Scientific Publications and Presentations

Moleculin’s cutting edge technologies are the subject of over 100 peer-reviewed or society featured publications, including some of the most prestigious journals like Nature, Blood, Cancer Research and the British Journal of Cancer and institutions like AACR, ASCO, ASH and EHA.

Annamycin Bibliography


Liposomal Annamycin in Combination with Cytarabine for Treatment of Acute Myeloid Leukemia (AML) (MB-106 Study)
A. Wadolowska, C. Papayannidis, C. Sartor, G. Martinelli, I. Zacheo, G. Marconi, E. Lech-Maranda, B. Machalinski, S. Milczarek, S. Sica, J. Halka, C. Abbate, E. Wasyl, W. Priebe, JP Waymack, W. Dempke

Abstract LB180: Non-cardiotoxic properties of annamycin, a clinically evaluated anthracycline and potent
topoisomerase 2β poison

Zielinski, R., Grela, K., Cardenas-Zuniga, R., Skora, S., Fokt, I., Gagea, M., Dempke, W., and Priebe, W. 2024. Cancer Research 84 (7_Supplement): LB180-LB180.


Exploration of Annamycin Organotropism to Target Primary and Metastatic Liver Cancers
Zielinski, R., Grela, K., Peng, S., Felix, E., Cardenas-Zuniga, R., Grybowski, D., Skora, S., Fokt, I., and Priebe, W. 2023. Cancer Research 83 (7_Supplement): 4947-4947.

Re-Exploring the Anthracycline Chemical Space for Better Anti-Cancer Compounds
van Gelder, M. A., van der Zanden, S. Y., Vriends, M. B., Wagensveld, R. A., van der Marel, G. A., Codée, J. D., Overkleeft, H. S., Wander, D. P., and Neefjes, J. J. 2023. Journal of Medicinal Chemistry 66 (16): 11390-11398.

Preliminary Results from a Phase 1/2 Study of Liposomal Annamycin (L-ANN) in Combination with Cytarabin for the Treatment of Patients with Acute Myeloid Leukemia (AML) That Is Refractory to or Relapsed (r/r) after Induction Therapy
Papayannidis, C., Wadolowska, C., Sica, S., Machlinski, B., Lech-Maranda, E., Abbate, C., Wasyl, E., Waymack, P., Priebe, W., and Dempke, W. 2023. Blood 142: 5948.

Anthracycline-induced cardiotoxicity—are we about to clear this hurdle?
Dempke, W. C., Zielinski, R., Winkler, C., Silberman, S., Reuther, S., and Priebe, W. 2023. European Journal of Cancer 185: 94-104.

Annamycin Elicits Encouraging Responses in R/R Acute Myeloid Leukemia
Conroy, R. 2023. Cancer Network: 15


New approach to target metastatic colorectal cancer organotropism with L-Annamycin
Zielinski, R. J., Grela, K. G., Cardenas-Zuniga, R., Skora, S., Fokt, I., Felix, E., Grybowski, D., and Priebe, W. 2022. Cancer Research 82 (12_Supplement): 4048-4048.


Abstract P218: Annamycin, a novel non-cardiotoxic anthracycline with high activity against sarcomas metastatic to lungs
Zielinski, R., Grela, K., Cardenas-Zuniga, R., Skora, S., Fokt, I., Poimenidou, M., Lamhamedi-Cherradi, S.-E., Ludwig, J., and Priebe, W. 2021. Molecular Cancer Therapeutics 20 (12_Supplement): P218-P218.

Abstract PO-066: High uptake, retention, and in vivo activity of L-Annamycin in pancreatic cancer models
Kang, Y. a., Zielinski, R., Zuniga, R. C., Venugopal, R., Poimenidou, M., Remiszewski, M., Peng, S., Felix, E., Grela, K., and Skora, S. 2021. Cancer Research 81 (22_Supplement): PO-066-PO-066.


High efficacy of liposomal annamycin (L-ANN) in combination with cytarabine in syngeneic p53-null AML mouse model
Zal, T., Zielinski, R., Grela, K., Cardenas-Zuniga, R., Skora, S., Fokt, I., Zal, M. A., Andreeff, M., Gil, L., Priebe, W. and Shephard, R. 2020. Blood 136: 6-7.

High Efficacy of Liposomal Annamycin (L-ANN) in Combination with Cytarabine in Syngeneic p53-Null AML Mouse Model
Zal, T., Zielinski, R., Grela, K., Cardenas-Zuniga, R., Skora, S., Fokt, I., Zal, M.A., Andreev, M., Gil, L., Shephard, R., and Priebe, W., 2020. 62nd ASH Annual Meeting and Exposition, December 5-8, 2020.

AML-221: Liposomal Annamycin Overcomes MDR and Has No Cardiac Toxicity in Two Clinical Trials for the Second-Line Treatment of R/R AML
Shepard, R. 2020. Clinical Lymphoma Myeloma and Leukemia 20: S193.

AML-221: Liposomal Annamycin Overcomes MDR and Has No Cardiac Toxicity in Two Clinical Trials for the Second-Line Treatment of R/R AML
Shepard, R. 2020. Second SOHO Italian Conference, Rome, Italy.


Biodistribution and Efficacy of L-Annamycin in a Novel Imageable AML Mouse Model
Zielinski, R., Grela, K., Skora, S., Jacamo, R., Fokt, I., Sander, M., Remiszewski, M., Felix, E., Shanmugasundaram, M., Zal, M. A., Andreeff, M., Priebe, W., and Zal, T. 2019. Blood 134 (Supplement_1): 5150-5150.

Topoisomerase II inhibitors in AML: past, present, and future
Economides, M. P., McCue, D., Borthakur, G., and Pemmaraju, N. 2019. Expert Opin Pharmacother 20 (13): 1637-1644.


Liposomal Formulations in Clinical Use: An Updated Review
Bulbake, U., Doppalapudi, S., Kommineni, N., and Khan, W. 2017. Pharmaceutics 9 (2).


Phase I/II Trial of Nanomolecular Liposomal Annamycin in Adult Patients With Relapsed/Refractory Acute
Lymphoblastic Leukemia

Wetzler, M., Thomas, D. A., Wang, E. S., Shepard, R., Ford, L. A., Heffner, T. L., Parekh, S., Andreeff, M., O’Brien, S., and Kantarjian, H. M. 2013. Clinical Lymphoma Myeloma and Leukemia 13 (4): 430-434.


NFκB activation and drug sensitivity in human neoplastic cells treated with anthracyclines
Gruber, B. M., Anuszewska, E., Bubko, I., Kasprzycka-Guttman, T., Misiewicz, I., Skupinska, K., Fokt, I., Priebe, W., 2008. Acta Poloniae Pharmaceutica 65 (2): 267-271.


New therapeutic strategies for the treatment of acute lymphoblastic leukaemia
Pui, C. H., and Jeha, S. 2007. Nat Rev Drug Discov 6 (2): 149-65.

Effect of structural modification at the 4, 3′, and 2′ positions of doxorubicin on topoisomerase II poisoning, apoptosis, and cytotoxicity in human melanoma cells
Gruber, B. M., Anuszewska, E. L., Bubko, I., Goździk, A., Fokt, I., and Priebe, W. 2007. Archivum Immunologiae et Therapiae Experimentalis 55 (3): 193.

Treatment of Acute Lymphoblastic Leukemia
Apostolidou, E., Swords, R., Alvarado, Y., and Giles, F. J. 2007. Drugs 67 (15): 2153-2171.

Emerging therapeutic options for Philadelphia-positive acute lymphocytic leukemia
Alvarado, Y., Apostolidou, E., Swords, R., and Giles, F. J. 2007. Expert Opinion on Emerging Drugs 12 (1): 165-179.


Relationship between Topoisomerase II-DNA Cleavable Complexes, Apoptosis and Cytotoxic Activity of Anthracyclines in Human Cervix Carcinoma Cells
Gruber, B. M., Anuszewska, E. L., Bubko, I., Gozdzik, A., Priebe, W., and Fokt, I. 2005. Anticancer Research 25 (3B): 2193.


Enhanced topoisomerase II targeting by annamycin and related 4-demethoxy anthracycline analogues
Trevino, A. V., Woynarowska, B. A., Herman, T. S., Priebe, W., and Woynarowski, J. M. 2004. Molecular Cancer Therapeutics 3 (11): 1403.

A Computational Model for Anthracycline Binding to DNA:  Tuning Groove-Binding Intercalators for Specific Sequences
Cashman, D. J., and Kellogg, G. E. 2004. Journal of Medicinal Chemistry 47 (6): 1360-1374.


Phase II study of liposomal annamycin in the treatment of doxorubicin-resistant breast cancer
Booser, D. J., Esteva, F. J., Rivera, E., Valero, V., Esparza-Guerra, L., Priebe, W., and Hortobagyi, G. N. 2002. Cancer Chemotherapy and Pharmacology 50 (1): 6-8.


Effects of liposome-entrapped annamycin in human breast cancer cells: Interference with cell cycle progression and induction of apoptosis
Orlandi, L., Bertoli, G., Abolafio, G., Daidone, M. G., and Zaffaroni, N. 2001. Journal of Cellular Biochemistry 81 (1): 9-22.

Aronex Pharmaceuticals reports on annamycin phase I trial
2001. Expert Rev Anticancer Ther 1 (1): 4.


Phase I study of liposomal annamycin
Booser, D. J., Perez-Soler, R., Cossum, P., Esparza-Guerra, L., Wu, Q.-P., Zou, Y., Priebe, W., and Hortobagyi, G. N. 2000. Cancer Chemotherapy and Pharmacology 46 (5): 427-432


Comparison of annamycin to adriamycin in cardiac and MDR tumor cell systems
Kolonias, D., Podona, T., Savaraj, N., Gate, L., Cossum, P., and Lampidis, T. J. 1999.  Anticancer Res 19 (2a): 1277-83.


Modifications in high-density lipoprotein lipid composition and structure alter the plasma distribution of free and
liposomal annamycin

Wasan, K. M., Ng, S., and Cassidy, S. M. 1997. Journal of Pharmaceutical Sciences 86 (7): 872-875.

Blood and Plasma Lipoprotein Distribution and Gender Differences in the Plasma Pharmacokinetics of
Lipid-Associated Annamycin

Wasan, K. M., Kwong, M. 1997. Pharmacology & Toxicology 80 (6): 301-307.

Sugar—modified anthracyclines: a search for drugs able to overcome multidrug resistance
Priebe, W., Perez-Soler, R., in Carbohydrates in drug design, Z. Witczak, Editor. 1997, Taylor & Francis. p. 551-578.

Annamycin circumvents resistance mediated by the multidrug resistance-associated protein (MRP) in breast MCF-7 and small-cell lung UMCC-1 cancer cell lines selected for resistance to etoposide
Perez-Soler, R., Neamati, N., Zou, Y., Schneider, E., Doyle, L. A., Andreeff, M., Priebe, W., and Ling, Y.-H., International Journal of Cancer, 1997. 71(1): p. 35-41.


Lyophilized preliposomal formulation of the non-cross-resistant anthracycline annamycin: effect of surfactant on liposome formation, stability, and size
Zou, Y., Priebe, W., Perez-Soler, R., Cancer Chemotherapy and Pharmacology, 1996. 39(1): p. 103-108.

Differences in lipoprotein concentration and composition modify the plasma distribution of free and liposomal annamycin
Wasan, K.M., Morton, R.E., Pharm Res, 1996. 13(3): p. 462-8.

Characteristics of lipid-based formulations that influence their biological behavior in the plasma of patients
Wasan, K.M., Lopez-Berestein, G., Clin Infect Dis, 1996. 23(5): p. 1126-38.

Modifications in plasma lipoprotein concentration and lipid composition regulate the biological activity of hydrophobic drugs
Wasan, K.M., Journal of Pharmacological and Toxicological Methods, 1996. 36(1): p. 1-11.

The novel anthracycline annamycin is not affected by P-glycoprotein- related multidrug resistance: comparison with idarubicin and doxorubicin in HL-60 leukemia cell lines
Consoli, U., Priebe, W., Ling, Y.-H., Mahadevia, R., Griffin, M., Zhao, S., Perez-Soler, R., Andreeff, M., Blood, 1996. 88(2): p. 633-644.


“Preclinical toxicity of liposome-incorporated annamycin: selective bone marrow toxicity with lack of cardiotoxicity.”
Zou, Y., Priebe, W., Stephens, L., Perez-Soler, R., Clinical Cancer Research, 1995. 1(11): p. 1369.

Effect of vesicle size and lipid composition on the in vivo tumor selectivity and toxicity of the non-cross-resistant anthracycline annamycin incorporated in liposomes
Zou, Y., Ling, Y.-H., Reddy, S., Priebe, W., Perez-Soler, R., International Journal of Cancer, 1995. 61(5): p. 666-671.

Distribution of Free and Liposomal Annamycin within Human Plasma Is Regulated by Plasma Triglyceride Concentrations but Not by Lipid Transfer Protein
Wasan, K.M., Perez‐Soler, R., Journal of Pharmaceutical Sciences, 1995. 84(9): p. 1094-1100.

Partial circumvention of multi-drug resistance by annamycin is associated with comparable inhibition of DNA synthesis in the nuclear matrix of sensitive and resistant cells
Ling, Y.-H., Zou, Y., Priebe, W., Perez-Soler, R., International Journal of Cancer, 1995. 61(3): p. 402-408.

Mechanism of Action-Governed Design of Anthracycline Antibiotics: A “Turn-Off/Turn-On” Approach
Priebe, W., Current Pharmaceutical Design, 1995. 1: p. 51-68.


Antitumor Activity of Free and Liposome-entrapped Annamycin, a Lipophilic Anthracycline Antibiotic with Non-Cross-Resistance Properties
Zou, Y., Ling, Y.-H., Nguyen, V., Priebe, W., Perez-Soler, R., Cancer Research, 1994. 54(6): p. 1479.

The Use of Liposomes as Carriers of Lipophilic Anthracycline Antibiotics
Perez-soler, R., Ling, Y.-H., Zou, Y., Priebe, W., Journal of Liposome Research, 1994. 4(1): p. 555-573.

Cellular pharmacology of the partially non-cross-resistant anthracycline annamycin entrapped in liposomes in KB and
KB-V1 cells

Perez-Soler, R., Ling, Y.-H., Zou, Y., Priebe, W., Cancer Chemotherapy and Pharmacology, 1994. 34(2): p. 109-118.


Organ distribution and tumor uptake of annamycin, a new anthracycline derivative with high affinity for lipid membranes, entrapped in multilamellar vesicles
Zou, Y., Priebe W., Ling, Y.-H., Perez-Soler, R., Cancer Chemotherapy and Pharmacology, 1993. 32(3): p. 190-196.

Quantitative Analysis of the Lipophilic Doxorubicin Analogue Annamycin in Plasma and Tissue Samples by
Reversed-Phase Chromatography

Zou, Y., Hayman, A., Priebe W., Perez-Soler, R., Journal of Pharmaceutical Sciences, 1993. 82(11): p. 1151-1154.

Design and tumor targeting of anthracyclines able to overcome multidrug resistance: A double-advantage approach
Priebe, W., Perez-Soler, R., Pharmacology & Therapeutics, 1993. 60(2): p. 215-234.

Intrinsic cytotoxicity and reversal of multidrug-resistance by monensin in KB parent and MDR cells
Ling, Y.-H., Priebe, W., Perez-Soler, R.,Int J Oncol, 1993. 3(5): p. 971-977.

In Vitro Cytotoxicity, Cellular Pharmacology, and DNA Lesions Induced by Annamycin, an Anthracycline Derivative with High Affinity for Lipid Membranes
Ling, Y.-H., Priebe, W., Yang, L-Y., Burke, T., Pommier, Y., Perez-Soler, R., Cancer Research, 1993. 53(7): p. 1583.

Apoptosis Induced by Anthracycline Antibiotics in P388 Parent and Multidrug-resistant Cells
Ling, Y.-H., Priebe, W., Perez-Soler, R., Cancer Research, 1993. 53(8): p. 1845.


Anthracycline Antibiotics with High Liposome Entrapment: Structural Features and Biological Activity
Perez-Soler, R., Priebe, W., Cancer Research, 1990. 50(14): p. 4260.

WP1066 Bibliography


Elevated Wall Tension Initiates Interleukin-6 Expression and Abdominal Aortic Dilation
Akerman, A. W., R. E. Stroud, R. W. Barrs, R. T. Grespin, L. T. McDonald, R. A. C. LaRue, R. Mukherjee, J. S. Ikonomidis, J. A. Jones and J. M. J. A. o. v. s. Ruddy (2018). 46: 193-204.

Interleukin-6 Promotes Proliferation but Inhibits Tenogenic Differentiation via the Janus Kinase/Signal Transducers and Activators of Transcription 3 (JAK/STAT3) Pathway in Tendon-Derived Stem Cells
Chen, S., G. Deng, K. Li, H. Zheng, G. Wang, B. Yu, K. J. M. s. m. i. m. j. o. e. Zhang and c. research (2018). 4: 1567.

Stat3/Oct-4/c-Myc signal circuit for regulating stemness-mediated doxorubicin resistance of triple-negative breast cancer cells and inhibitory effects of WP1066
Cheng, C.-C., L.-H. Shi, X.-J. Wang, S.-X. Wang, X.-Q. Wan, S.-R. Liu, Y.-F. Wang, Z. Lu, L.-H. Wang and Y. J. I. j. o. o. Ding (2018). 53(1): 339-348.

Combinatorial Drug Testing in 3D Microtumors Derived from GBM Patient-Derived Xenografts Reveals Cytotoxic Synergy in Pharmacokinomics-informed Pathway Interactions
Gilbert, A. N., J. C. Anderson, C. W. Duarte, R. S. Shevin, C. P. Langford, R. Singh, G. Y. Gillespie and C. D. J. S. r. Willey (2018)

Thymoquinone Augments Cisplatin-Induced Apoptosis on Esophageal Carcinoma Through Mitigating the Activation of JAK2/STAT3 Pathway
Hu, X., J. Ma, V. Vikash, J. Li, D. Wu, Y. Liu, J. Zhang, W. J. D. d. Dong and sciences (2018). 63(1): 126-134.

Edaravone ameliorates experimental autoimmune thyroiditis in rats through HO-1-dependent STAT3/PI3K/Akt pathway
Li, H., J. Min, X. Mao, X. Wang, Y. Yang and Y. J. A. j. o. t. r. Chen (2018). 10(7): 2037.

Study of Kinase Inhibitor WP1066 on the STAT3/JAK2 of Prostate Stromal Cells
Li, Y., J. Li, Q. Wei, Z. Zhang, J. Wu and A. J. S. d. x. x. b. Y. x. b. J. o. S. U. M. s. e. Wang (2018). 48(1): 65-68.

An RNAi-mediated screen identifies novel targets for next-generation antiepileptic drugs based on increased expression of the homeostatic regulator pumilio
Lin, W.-H., M. He, Y. N. Fan and R. A. J. J. o. n. Baines (2018). 32(2): 106-117.

Nesfatin-1 functions as a switch for phenotype transformation and proliferation of VSMCs in hypertensive vascular remodeling
Lu, Q.-B., H.-P. Wang, Z.-H. Tang, H. Cheng, Q. Du, Y.-B. Wang, W.-B. Feng, K.-X. Li, W.-W. Cai and L.-Y. J. B. e. B. A.-M. B. o. D. Qiu (2018). 1864(6): 2154-2168.

Effects of Interleukin-6 on posterior capsular opacification
Ma, B., L. Yang, R. Jing, J. Liu, Y. Quan, Q. Hui, J. Li, L. Qin and C. J. E. e. r. Pei (2018). 172: 94-103.

Impact of STAT3 phosphorylation in glioblastoma stem cells radiosensitization and patient outcome
Masliantsev, K., B. Pinel, A. Balbous, P.-O. Guichet, G. Tachon, S. Milin, J. Godet, M. Duchesne, A. Berger and C. J. O. Petropoulos (2018). 9(3): 3968.

STAT3/HOTAIR signaling axis regulates HNSCC growth in an EZH2-dependent manner
Sun, S., Y. Wu, W. Guo, F. Yu, L. Kong, Y. Ren, Y. Wang, X. Yao, C. Jing and C. J. C. C. R. Zhang (2018)

Cancer cell-intrinsic PD-1 and implications in combinatorial immunotherapy
Xu, J., H. Yao, H. Wang, C. Li and J.-Y. J. F. i. i. Fang (2018). 9: 1774.

Astrocyte elevated gene‐1 promotes invasion and epithelial–mesenchymal transition in bladder cancer cells through activation of signal transducer and activator of transcription 3
Yang, X., L. Shi, C. Yi, Y. Yang, L. Chang and D. J. I. J. o. U. Song (2018). 25(2): 157-163.

Dual-functionality of RASSF1A overexpression in A375 cells is mediated by activation of IL-6/STAT3 regulatory loop
Yi, M., W. Wang, S. Chen, Y. Peng, J. Li, J. Cai, Y. Zhou, Q. Peng, Y. Ban and Z. J. M. b. r. Zeng (2018). 45(5): 1277-1287.


Large Amino Acid Transporter 1 Selective Liposomes of l-DOPA Functionalized Amphiphile for Combating Glioblastoma.
Bhunia, S., V. Vangala, D. Bhattacharya, H. G. Ravuri, M. Kuncha, S. Chakravarty, R. Sistla and A. J. M. p. Chaudhuri (2017). 14(11): 3834-3847.

STAT3 balances myocyte hypertrophy vis-à-vis autophagy in response to Angiotensin II by modulating the AMPKα/mTOR axis
Chen, L., L. Zhao, A. Samanta, S. M. Mahmoudi, T. Buehler, A. Cantilena, R. J. Vincent, M. Girgis, J. Breeden and S. J. P. o. Asante (2017). 12(7): e0179835.

Leukemia inhibitory factor (LIF) withdrawal activates mTOR signaling pathway in mouse embryonic stem cells through the MEK/ERK/TSC2 pathway
Cherepkova, M. Y., G. S. Sineva, V. A. J. C. d. Pospelov and disease (2017). 7(1): e2050.

Comparison of three cell-based drug screening platforms for HSV-1 infection
D’aiuto, L., K. Williamson, P. Dimitrion, J. McNulty, C. E. Brown, C. B. Dokuburra, A. J. Nielsen, W. J. Lin, P. Piazza and M. E. J. A. r. Schurdak (2017). 142: 136-140.

WP1066 suppresses macrophage cell death induced by inflammasome agonists independently of its inhibitory effect on STAT3
Honda, S., D. Sadatomi, Y. Yamamura, K. Nakashioya, S. Tanimura and K. J. C. s. Takeda (2017). 108(3): 520-527.

IL-27 modulates chemokine production in TNF-α-stimulated human oral epithelial cells
Hosokawa, Y., I. Hosokawa, K. Ozaki, T. J. C. P. Matsuo and Biochemistry (2017). 43(3): 1198-1206.

IL-29 Enhances CXCL10 Production in TNF-α-stimulated Human Oral Epithelial Cells
Hosokawa, Y., I. Hosokawa, S. Shindo, K. Ozaki and T. J. I. i. Matsuo (2017). 46(6): 615-624.

Survivin inhibitor YM155 induces mitochondrial dysfunction, autophagy, DNA damage and apoptosis in Bcl‐xL silenced glioma cell lines
Jane, E. P., D. R. Premkumar, P. A. Sutera, J. M. Cavaleri and I. F. J. M. c. Pollack (2017). 56(4): 1251-1265.

Adipose stromal cells from visceral and subcutaneous fat facilitate migration of ovarian cancer cells via IL-6/JAK2/STAT3 pathway
Kim, B., H. S. Kim, S. Kim, G. Haegeman, B. K. Tsang, D. N. Dhanasekaran, Y. S. J. C. r. Song and t. o. j. o. K. C. Association (2017). 49(2): 338.

Irisin reverses the IL-6 induced epithelial-mesenchymal transition in osteosarcoma cell migration and invasion through the STAT3/Snail signaling pathway
Kong, G., Y. Jiang, X. Sun, Z. Cao, G. Zhang, Z. Zhao, Y. Zhao, Q. Yu and G. J. O. r. Cheng (2017). 38(5): 2647-2656.

The prenylflavonoid Icaritin enhances osteoblast proliferation and function by signal transducer and activator of transcription factor 3 (STAT-3) regulation of CXC chemokine receptor type 4 (CXCR4) expression
Lim, R., L. Li, N. Chew and E. J. B. Yong (2017). 105: 122-133.

Stat3 inhibitor abrogates the expression of PD-1 ligands on lymphoma cell lines.
Ma, C., H. Horlad, C. Pan, H. Yano, K. Ohnishi, Y. Fujiwara, M. Matsuoka, A. Lee, T. Niidome, R. J. J. o. c. Yamanaka and e. hematopathology (2017). 57(1): 21-25.

Combination of cationic dexamethasone derivative and STAT3 inhibitor (WP1066) for aggressive melanoma: a strategy for repurposing a phase I clinical trial drug
Sau, S., S. K. Mondal, S. K. Kashaw, A. K. Iyer, R. J. M. Banerjee and c. biochemistry (2017). 436(1-2): 119-136.

Molecular mechanisms of 3, 3′ 4, 4′, 5-pentachlorobiphenyl-induced epithelial-mesenchymal transition in human hepatocellular carcinoma cells
Song, L., L. Guo, Z. J. T. Li and a. pharmacology (2017). 322: 75-88.

In vivo and ex vivo cetuximab sensitivity assay using three-dimensional primary culture system to stratify KRAS mutant colorectal cancer
Tashiro, T., H. Okuyama, H. Endo, K. Kawada, Y. Ashida, M. Ohue, Y. Sakai and M. J. P. o. Inoue (2017). 12(3): e0174151.

Chemokine CCL2-CCR2 signaling induces neuronal cell death via STAT3 activation and IL-1β production after status epilepticus
Tian, D.-S., J. Peng, M. Murugan, L. Feng, J.-L. Liu, U. B. Eyo, L.-J. Zhou, R. Mogilevsky, W. Wang and L.-J. J. J. o. N. Wu (2017). 0315-0317.

STAT3 inhibition by WP1066 suppresses the growth and invasiveness of bladder cancer cells
Tsujita, Y., A. Horiguchi, S. Tasaki, M. Isono, T. Asano, K. Ito, T. Asano, Y. Mayumi and T. J. O. r. Kushibiki (2017). 38(4): 2197-2204.

WP1066, a small molecule inhibitor of the JAK/STAT3 pathway, inhibits ceramide glucosyltransferase activity
Tsurumaki, H., H. Katano, K. Sato, R. Imai, S. Niino, Y. Hirabayashi, S. J. B. Ichikawa and b. r. communications (2017). 491(2): 265-270.

IL-6 promotes epithelial-to-mesenchymal transition of human peritoneal mesothelial cells possibly through the JAK2/STAT3 signaling pathway
Xiao, J., Y. Gong, Y. Chen, D. Yu, X. Wang, X. Zhang, Y. Dou, D. Liu, G. Cheng and S. J. A. J. o. P.-R. P. Lu (2017). 313(2): F310-F318.

SERPINB1 ameliorates acute lung injury in liver transplantation through ERK1/2-mediated STAT3-dependent HO-1 induction
Yao, W., H. Li, G. Luo, X. Li, C. Chen, D. Yuan, X. Chi, Z. Xia, Z. J. F. R. B. Hei and Medicine (2017). 108: 542-553.

Exogenous MSCs ameliorate hypoxia/reoxygenation injury in renal tubular epithelial cells through JAK/STAT signaling pathway-mediated regulation of HMGB
Zhang, L., Y. Wang, J. Ma, X. Lai, J. Fang, G. Li, L. Xu, G. Pan and Z. J. A. j. o. t. r. Chen (2017). 9(5): 2412.

Overexpression of Human Papillomavirus Type 16 Oncoproteins Enhances Epithelial‐Mesenchymal Transition via STAT3 Signaling Pathway in Non-Small Cell Lung Cancer Cells
Zhang, W., X. Wu, L. Hu, Y. Ma, Z. Xiu, B. Huang, Y. Feng, X. J. O. R. F. P. Tang and C. C. Therapeutics (2017). 25(5): 843-852.


WP1066 exhibits antitumor efficacy in nasal‑type natural killer/T-cell lymphoma cells through downregulation of the STAT3 signaling pathway
Geng, L., X. Li, X. Zhou, X. Fang, D. Yuan and X. J. O. r. Wang (2016). 36(5): 2868-2874.

STAT3 signaling pathway regulates glioma stem cells induced host macrophage malignance
Hong, L., J. Ma, H. Zhu, H. Cai, J. Dong, M. Li, Q. Huang and A. J. T. C. R. Wang (2016). 5(6): 805-816.

Inhibition of Signal Transducer and Activator of Transcription 3 (STAT 3) reduces neonatal hypoxic‐ischaemic brain damage.
Hristova, M., E. Rocha‐Ferreira, X. Fontana, L. Thei, R. Buckle, M. Christou, S. Hompoonsup, N. Gostelow, G. Raivich and D. J. J. o. n. Peebles (2016). 136(5): 981-994.

ALDH1A1 induces resistance to CHOP in diffuse large B-cell lymphoma through activation of the JAK2/STAT3 pathway
Jiang, J., Y. Liu, Y. Tang, L. Li, R. Zeng, S. Zeng, M. J. O. Zhong and therapy (2016). 9: 5349.

Progression and inflammation of human myeloid leukemia induced by ambient PM2. 5 exposure
Jin, X.-T., M.-L. Chen, R.-J. Li, Q. An, L. Song, Y. Zhao, H. Xiao, L. Cheng and Z.-Y. J. A. o. t. Li (2016). 90(8): 1929-1938.

B cell translocation gene 2 (Btg2) is regulated by Stat3 signaling and inhibits adipocyte differentiation
Kim, S., J.-W. Hong, K. W. J. M. Park and c. biochemistry (2016). 413(1-2): 145-153.

The STAT-3 inhibitor WP1066 promotes oral squamous cell carcinoma invasiveness by cisplatin in vitro
Kong, L., A. Liu, X. Zhou, Y. Ren, Y. Huang, S. Liu and L. J. T. M. J. Zhang (2016). 44(1): 38-42.

Docosahexaenoic acid inhibits 12-O-tetradecanoylphorbol-13-acetate-induced fascin-1-dependent breast cancer cell migration by suppressing the PKCδ-and Wnt-1/β-catenin-mediated pathways
Lii, C.-K., J.-W. Chang, J.-J. Chen, H.-W. Chen, K.-L. Liu, S.-L. Yeh, T.-S. Wang, S.-H. Liu, C.-H. Tsai and C.-C. J. O. Li (2016). 7(18): 25162.

Dexmedetomidine acts via the JAK2/STAT3 pathway to attenuate isoflurane-induced neurocognitive deficits in senile mice
Si, Y., Y. Zhang, L. Han, L. Chen, Y. Xu, F. Sun, M. Ji, J. Yang and H. J. P. o. Bao (2016). 11(10): e0164763.

Irisin reverses platelet derived growth factor-BB-induced vascular smooth muscle cells phenotype modulation through STAT3 signaling pathway
Song, H., J. Xu, N. Lv, Y. Zhang, F. Wu, H. Li, L. Shao, Q. Mu, F. Wang, D. J. B. Tang and b. r. communications (2016). 479(2): 139-145.

The hepatocyte growth factor antagonist NK4 inhibits indoleamine-2, 3-dioxygenase expression via the c-Met-phosphatidylinositol 3-kinase-AKT signaling pathway
Wang, D., Y. Saga, N. Sato, T. Nakamura, O. Takikawa, H. MIzUKAMI, S. MATSUbARA and H. J. I. j. o. o. Fujiwara (2016). 48(6): 2303-2309.

Overexpression of RPS27a contributes to enhanced chemoresistance of CML cells to imatinib by the transactivated STAT3
Wang, H., B. Xie, Y. Kong, Y. Tao, G. Yang, M. Gao, H. Xu, F. Zhan, J. Shi and Y. J. O. Zhang (2016). 7(14): 18638.

miR-182-5p induced by STAT3 activation promotes glioma tumorigenesis
Xue, J., A. Zhou, Y. Wu, S.-A. Morris, K. Lin, S. Amin, R. Verhaak, G. Fuller, K. Xie and A. B. J. C. r. Heimberger (2016). 76(14): 4293-4304.

Delayed administration of WP1066, an STAT3 inhibitor, ameliorates radiation-induced lung injury in mice
Yu, J., X. Yuan, Y. Liu, K. Zhang, J. Wang, H. Zhang and F. J. L. Liu (2016). 194(1): 67-74.


IL-21 induces antiviral microRNA-29 in CD4 T cells to limit HIV-1 infection
Adoro, S., J. R. Cubillos-Ruiz, X. Chen, M. Deruaz, V. D. Vrbanac, M. Song, S. Park, T. T. Murooka, T. E. Dudek and A. D. Luster (2015). Nature Communications 6:7562.

IL10, TGF Beta1, and IFN Gamma Modulate Intracellular Signaling Pathways and Cytokine Production to Control Toxoplasma gondii Infection in BeWo Trophoblast Cells
Barbosa, B. F., J. B. Lopes-Maria, A. O. Gomes, M. B. Angeloni, A. S. Castro, P. S. Franco, M. L. Fermino, M. C. Roque-Barreira, F. Ietta and O. A. Martins-Filho (2015). Biology of Reproduction 92(3):82, 1-13.

Molecular Heterogeneity in a Patient-Derived Glioblastoma Xenoline Is Regulated by Different Cancer Stem Cell Populations
Garner, J. M., D. W. Ellison, D. Finkelstein, D. Ganguly, Z. Du, M. Sims, C. H. Yang, R. B. Interiano, A. M. Davidoff and L. M. Pfeffer (2015). PloS ONE 10(12): e0125838

Progression and inflammation of human myeloid leukemia induced by ambient PM2. 5 exposure
Jin, X.-T., M.-L. Chen, R.-J. Li, Q. An, L. Song, Y. Zhao, H. Xiao, L. Cheng and Z.-Y. Li (2015). Archives of Toxicology: pp1-10.

STAT3 Regulates Lytic Activation of Kaposi’s Sarcoma-Associated Herpesvirus
King, C. A., X. Li, A. Barbachano-Guerrero and S. Bhaduri-McIntosh (2015). Journal of Virology 89(22): 11347-11355.

Sorafenib sensitizes glioma cells to the BH3 mimetic ABT-737 by targeting MCL1 in a STAT3-dependent manner
Kiprianova, I., J. Remy, N. Milosch, I. V. Mohrenz, V. Seifert, A. Aigner and D. Kögel (2015). Neoplasia 17(7): 564-573.

Stat3 orchestrates interaction between endothelial and tumor cells and inhibition of Stat3 suppresses brain metastasis of breast cancer cells
Lee, H.-T., J. Xue, P.-C. Chou, A. Zhou, P. Yang, C. A. Conrad, K. D. Aldape, W. Priebe, C. Patterson and R. Sawaya (2015). Oncotarget 6(12): 10016-10029.

The STAT3 inhibitor WP1066 synergizes with vorinostat to induce apoptosis of mantle cell lymphoma cells
Lu, K., N. Chen, X.-x. Zhou, X.-l. Ge, L.-l. Feng, P.-p. Li, X.-y. Li, L.-y. Geng and X. Wang (2015). Biochemical and Biophysical Research Communications 464(1): 292-298.

The STAT3 inhibitor WP1066 reverses the resistance of chronic lymphocytic leukemia cells to histone deacetylase inhibitors induced by interleukin-6
Lu, K., X.-s. Fang, L.-l. Feng, Y.-j. Jiang, X.-x. Zhou, X. Liu, P.-p. Li, N. Chen, M. Ding and N. Wang (2015). Cancer Letters 359(2): 250-258.

Bromine Atom Interactions in Biologically Active Acrylamide Derivatives
Malinska, M., I. Fokt, W. Priebe and K. Wozniak (2015). Crystal Growth & Design 15(6): 2632-2642.

Enhanced miR-210 expression promotes the pathogenesis of endometriosis through activation of signal transducer and activator of transcription
Okamoto, M., K. Nasu, W. Abe, Y. Aoyagi, Y. Kawano, K. Kai, M. Moriyama and H. Narahara (2015). Human Reproduction 30(3): 632-641.

Overcoming Chemoresistance of Pediatric Ependymoma by Inhibition of STAT3 Signaling
Phi, J. H., S.-A. Choi, S.-K. Kim, K.-C. Wang, J. Y. Lee and D. G. Kim (2015). Translational Oncology 8(5): 376-386.

FL3, a Synthetic Flavagline and Ligand of Prohibitins, Protects Cardiomyocytes via STAT3 from Doxorubicin Toxicity
Qureshi, R., O. Yildirim, A. Gasser, C. Basmadjian, Q. Zhao, J.-P. Wilmet, L. Désaubry and C. G. Nebigil (2015). PloS ONE 10(11): e0141826.

JAK/STAT pathway regulation of GABA A receptor expression after differing severities of experimental TBI
Raible, D. J., L. C. Frey, Y. C. Del Angel, J. Carlsen, D. Hund, S. J. Russek, B. Smith and A. R. Brooks-Kayal (2015). Experimental Neurology 271: 445-456.

Coculture with astrocytes reduces the radiosensitivity of glioblastoma stem‐like cells and identifies additional targets for radiosensitization.
Rath, B. H., A. Wahba, K. Camphausen and P. J. Tofilon (2015). Cancer Medicine 4(11): 1705-1716.

Cochinchina Momordica Seed Suppresses Proliferation and Metastasis in Human Lung Cancer Cells by Regulating Multiple Molecular Targets.
Shen, Y., L. Meng, H. Sun, Y. Zhu and H. Liu (2015). The American Journal of Chinese Medicine 43(01): 149-166.

Targeting STAT3/miR-21 axis inhibits epithelial-mesenchymal transition via regulating CDK5 in head and neck squamous cell carcinoma
Sun, S.-S., X. Zhou, Y.-Y. Huang, L.-P. Kong, M. Mei, W.-Y. Guo, M.-H. Zhao, Y. Ren, Q. Shen and L. Zhang (2015). Molecular Cancer 14(1): 1.

Delayed Administration of WP1066, an STAT3 Inhibitor, Ameliorates Radiation-Induced Lung Injury in Mice
Yu, J., X. Yuan, Y. Liu, K. Zhang, J. Wang, H. Zhang and F. Liu (2015). Lung, Epub ahead of print, doi:10.1007/s000408-015-9821-8.

Suppression of autophagy augments the radiosensitizing effects of STAT3 inhibition on human glioma cells
Yuan, X., J. Du, S. Hua, H. Zhang, C. Gu, J. Wang, L. Yang, J. Huang, J. Yu and F. Liu (2015). Experimental Cell Research 330(2): 267-276.

Inhibition of Signal Transducer and Activator of Transcription 3 (STAT3) reduces neonatal hypoxic‐ischemic brain damage
Hristova, M., E. Rocha‐Ferreira, X. Fontana, L. Thei, R. Buckle, M. Christou, S. Hompoonsup, N. Gostelow, G. Raivich and D. Peebles (2015). Journal of Neurochemistry. doi: 10.1111/jnc.13490


Preclinical characterization of signal transducer and activator of transcription 3 small molecule inhibitors for primary and metastatic brain cancer therapy
Assi, H. H., C. Paran, N. VanderVeen, J. Savakus, R. Doherty, E. Petruzzella, J. D. Hoeschele, H. Appelman, L. Raptis and T. Mikkelsen (2014). Journal of Pharmacology and Experimental Therapeutics 349(3): 458-46

Inhibition of STAT3 activity re-activates anti-tumor immunity but fails to restore the immunogenicity of tumor cells in a B-cell lymphoma model
Cao, Y., X. Zhou, M. Zhou, D. Xu, Q. Ma, P. Zhang, X. Huang, Q. Li, D. Ma and J. Zhou (2014). Cancer Biology & Therapy 15(9): 1153-1162.

A ROS/STAT3/HIF‐1α signaling cascade mediates EGF‐induced TWIST1 expression and prostate cancer cell invasion
Cho, K. H., M. J. Choi, K. J. Jeong, J. J. Kim, M. H. Hwang, S. C. Shin, C. G. Park and H. Y. Lee (2014). The Prostate 74(5): 528-536.

Hypoxia and STAT3 signalling interactions regulate pro-inflammatory pathways in rheumatoid arthritis
Gao, W., J. McCormick, M. Connolly, E. Balogh, D. J. Veale and U. Fearon (2014). Annals of the Rheumatic Diseases: 74(6), 1275-83.

The effect of STAT3 inhibition on status epilepticus and subsequent spontaneous seizures in the pilocarpine model of acquired epilepsy
Grabenstatter, H., Y. C. Del Angel, J. Carlsen, M. Wempe, A. White, M. Cogswell, S. Russek and A. Brooks-Kayal (2014).Neurobiology of Disease 62: 73-85.

Targeting miR-21 to treat psoriasis
Guinea-Viniegra, J., M. Jiménez, H. B. Schonthaler, R. Navarro, Y. Delgado, M. J. Concha-Garzón, E. Tschachler, S. Obad, E. Daudén and E. F. Wagner (2014). Science Translational Medicine 6(225): 225re1/1-225re1/8.

Increased STAT1 signaling in endocrine-resistant breast cancer
Huang, R., D. Faratian, A. H. Sims, D. Wilson, J. S. Thomas, D. J. Harrison and S. P. Langdon (2014). PloS ONE 9(4): e94226/11.

Signal transducer and activator of transcription-3 inhibitor WP1066 affects human tongue squamous cell carcinoma proliferation and apoptosis in vitro and in vivo
Huang, Y., X. Zhou, A. Liu, S. Li, X. Wang and L. Zhang (2014). Chinese Journal of Stomatology 49(5): 308-313.

Inhibition of the JAK2/STAT3 pathway reduces gastric cancer growth in vitro and in vivo
Judd, L. M., T. R. Menheniott, H. Ling, C. B. Jackson, M. Howlett, A. Kalantzis, W. Priebe and A. S. Giraud (2014). PLoS ONE 9(5): e95993.

Therapeutic targets in subependymoma
Kong, L.-Y., J. Wei, A. S. Haider, B. D. Liebelt, X. Ling, C. A. Conrad, G. N. Fuller, N. B. Levine, W. Priebe and R. Sawaya (2014). Journal of Neuroimmunology 277(1): 168-175.

Analogs of Cinnamic Acid Benzyl Amide As Nonclassical Inhibitors of Activated JAK2 Kinase
Mielecki, M., M. Milner-Krawczyk, K. Grzelak, D. Mielecki, K. A Krzysko, B. Lesyng and W. Priebe (2014). Current Cancer Drug Targets 14(7): 638-651.

Inhibitor of signal transducer and activator of transcription 3 (STAT3) suppresses ovarian cancer growth, migration and invasion and enhances the effect of cisplatin in vitro
Tang, Y., Z. Sun, W. Wu, J. Xing, Y. He, D. Xin and P. Han (2014). Genetics and Molecular Research: GMR 14(1): 2450-2460.

Regulation of PSMB5 Protein and β Subunits of Mammalian Proteasome by Constitutively Activated Signal Transducer and Activator of Transcription 3 (STAT3): potential role in bortezomib-mediated anticancer therapy
Vangala, J. R., S. Dudem, N. Jain and S. V. Kalivendi (2014). Journal of Biological Chemistry 289(18): 12612-12622.

STAT3 inhibitor WP1066 as a novel therapeutic agent for bCCI neuropathic pain rats
Xue, Z.-j., L. Shen, Z.-y. Wang, S.-y. Hui, Y.-g. Huang and C. Ma (2014). Brain Research 1583: 79-88.

Induction of Murine Macrophage M2 Polarization by Cigarette Smoke Extract via the JAK2/STAT3 Pathway
Yuan, F., X. Fu, H. Shi, G. Chen, P. Dong and W. Zhang (2014). PLoS ONE 9(9): e107063

Effect of Angiotensin II on STAT3 mediated atrial structural remodeling
Zheng, L., M. Zhang, J. Xue, Y. Li, Y. Nan, M. Li, J. Wang and X. Du (2014). European Review for Medical and Pharmacological Sciences 18(16): 2365-2377.

JAK2/STAT3 targeted therapy suppresses tumor invasion via disruption of the EGFRvIII/JAK2/STAT3 axis and associated focal adhesion in EGFRvIII-expressing glioblastoma
Zheng, Q., L. Han, Y. Dong, J. Tian, W. Huang, Z. Liu, X. Jia, T. Jiang, J. Zhang and X. Li (2014).Zheng, Q., L. Han, Y. Dong, J. Tian, W. Huang, Z. Liu, X. Jia, T. Jiang, J. Zhang and X. Li (2014). Neuro-Oncology 16(9): 1229-1243.

STAT3 inhibitor WP1066 attenuates miRNA-21 to suppress human oral squamous cell carcinoma growth in vitro and in vivo
Zhou, X., Y. Ren, A. Liu, L. Han, K. Zhang, S. Li, P. Li, P. Li, C. Kang and X. Wang (2014). Oncology Reports 31(5): 2173-2180.

WP1066 Sensitizes Oral Squamous Cell Carcinoma Cells to Cisplatin by Targeting STAT3/miR-21 axis
Zhou, X., Y. Ren, A. Liu, R. Jin, Q. Jiang, Y. Huang, L. Kong, X. Wang and Zhang (2014). Scientific Reports 4: 7461


Effect of the STAT3 inhibitor STX-0119 on the proliferation of cancer stem-like cells derived from recurrent glioblastoma
Ashizawa, T., H. Miyata, et al. (2013). International Journal of Oncology 43(1): 219-227.

Inflammatory effects of resistin on human smooth muscle cells: Up-regulation of fractalkine and its receptor, CX3CR1 expression by TLR4 and Gi-protein pathways
Gan, A. M., E. D. Butoi, et al. (2013). Cell and Tissue Research 351(1): 161-174.

STAT3 as a therapeutic target for Epstein-Barr virus (EBV) – associated nasopharyngeal carcinoma
Ho, Y., S. W. Tsao, et al. (2013). Cancer Letters 330(2): 141-149.

Deficiency of Erbin induces resistance of cervical cancer cells to anoikis in a STAT3-dependent manner
Hu, Y., H. Chen, et al. (2013). Oncogenesis 2 (e53): 1-12.

The hyaluronic acid receptor CD44 coordinates normal and metaplastic gastric epithelial progenitor cell proliferation
Khurana, S. S., T. E. Riehl, et al. (2013). Journal of Biological Chemistry 288(22): 16085-16097.

Stat3-targeted therapies overcome the acquired resistance to vemurafenib in melanomas
Liu, F., J. Cao, et al. (2013). Journal of Investigative Dermatology 133(8): 2041-2049.

Identification of novel host-targeted compounds that protect from anthrax lethal toxin-induced cell death
Slater, L. H., E. C. Hett, et al. (2013). ACS Chem Biol 8(4): 812-822.

Angiotensin-converting enzyme 2 attenuates oxidative stress and VSMC proliferation via the JAK2/STAT3/SOCS3 and profilin-1/MAPK signaling pathways
Song, B., H. Jin, et al. (2013). Regulatory Peptides 185: 44-51.

On-target JAK2/STAT3 inhibition slows disease progression in orthotopic xenografts of human glioblastoma brain tumor stem cells
Stechishin, O. D., H. A. Luchman, et al. (2013). Neuro-Oncology 15(2): 198-207.


microRNA‐124 Regulates Cardiomyocyte Differentiation of Bone Marrow‐Derived Mesenchymal Stem Cells Via Targeting STAT3 Signaling
Cai, B., J. Li, et al. (2012). Stem Cells 30(8): 1746-1755.

Inhibition of STAT3 signaling prevents vascular smooth muscle cell proliferation and neointima formation
Daniel, J. M., J. Dutzmann, et al. (2012). Basic Research in Cardiology 107(3): 261.

The tumor microenvironment expression of p-STAT3 influences the efficacy of cyclophosphamide with WP1066 in murine melanoma models
Hatiboglu, M. A., L. Y. Kong, et al. (2012). International Journal of Cancer 131(1): 8-17.

Delta-opioid receptor activation promotes mesenchymal stem cell survival via PKC/STAT3 signaling pathway
Higuchi, S., M. Ii, et al. (2012). Circulation Journal 76(1): 204-212.

Upregulation of CXCR4 is functionally crucial for maintenance of stemness in drug-resistant non-small cell lung cancer cells
Jung, M., J. Rho, et al. (2012). Oncogene 32(2): 209-221.

Suicide Gene Reveals the Myocardial Neovascularization Role of Mesenchymal Stem Cells Overexpressing CXCR4 (MSCCXCR4)
Liang, J., W. Huang, et al. (2012). PloS ONE 7(9): e46158.

Leukemia Inhibitory Factor-Induced Stat3 Signaling Suppresses Fibroblast Growth Factor 1-Induced Erk1/2 Activation to Inhibit the Downstream Differentiation in Mouse Embryonic Stem Cells
Liu, J.-W., Y.-C. Hsu, et al. (2012). Stem Cells and Development 22(8): 1190-1197.

Sphingosine-1-phosphate enhances satellite cell activation in dystrophic muscles through a S1PR2/STAT3 signaling pathway
Loh, K. C., W. I. Leong, et al. (2012). PloS ONE 7(5): doi:10.1371/journal.pone.0037218.

Induction of Bv8 Expression by granulocyte colony-stimulating factor in CD11b+Gr1+ cells: Key role of Stat3 signaling
Qu, X., G. Zhuang, et al. (2012). Journal of Biological Chemistry 287(23): 19574-19584.

Synthetic lethal screening with small-molecule inhibitors provides a pathway to rational combination therapies for melanoma
Roller, D. G., M. Axelrod, et al. (2012). Molecular Cancer Therapeutics 11(11): 2505-2515.

Low amino acids affect expression of 11β-HSD2 in BeWo cells through leptin-activated JAK-STAT and MAPK pathways
Shang, Y., X. Yang, et al. (2012). Amino Acids 42(5): 1879-1887.

STAT5 in Human Basophils: IL-3 Is Required for Its FceRI-Mediated Phosphorylation
Verweij, M. M., V. Sabato, et al. (2012). Cytometry Part B (Clinical Cytometry) 82B(2): 101-106.


Suppression of Stat3 activity sensitizes gefitinib-resistant non small cell lung cancer cells
Chiu, H. C., D. L. Chou, et al. (2011). Biochemical Pharmacology 81(11): 1263-1270.

Oncostatin M-enhanced vascular endothelial growth factor expression in human vascular smooth muscle cells involves PI3K-, p38 MAPK-, Erk1/2- and STAT1/STAT3-dependent pathways and is attenuated by interferon-γ
Demyanets, S., C. Kaun, et al. (2011). Basic Research in Cardiology 106(2): 217-231.

Transactivated EGFR mediates alpha(1)-AR-induced STAT3 activation and cardiac hypertrophy
Li, Y., H. Zhang, et al. (2011). Am J Physiol Heart Circ Physiol 301(5): H1941-1951.

Hepatocyte growth factor suppresses the anticancer effect of irinotecan by decreasing the level of active metabolite in HepG2 cells
Okumura, M., T. Iwakiri, et al. (2011). Biochemical Pharmacology 82(11): 1720-1730.

Tyrphostin-like compounds with ubiquitin modulatory activity as possible therapeutic agents for multiple myeloma
Peng, Z., A. Pal, et al. (2011). Bioorganic & Medicinal Chemistry 19(23): 7194-7204.

Inhibition of STAT3 reverses alkylator resistance through modulation of the AKT and beta-catenin signaling pathways
Wang, Y., L. Chen, et al. (2011). Oncol Rep 26(5): 1173-1180.

Two small molecule compounds, LLL12 and FLLL32, exhibit potent inhibitory activity on STAT3 in human rhabdomyosarcoma cells
Wei, C. C., S. Ball, et al. (2011). International Journal of Oncology 38(1): 279-285.

Hypoxia potentiates glioma-mediated immunosuppression
Wei, J., A. Wu, et al. (2011). PloS ONE 6(1).


The small molecule curcumin analog FLLL32 induces apoptosis in melanoma cells via STAT3 inhibition and retains the cellular response to cytokines with anti-tumor activity
Bill, M. A., J. R. Fuchs, et al. (2010). Molecular Cancer 9: 165.

STAT3 inhibitor WP1066 as a novel therapeutic agent for renal cell carcinoma
Horiguchi, A., T. Asano, et al. (2010). British Journal of Cancer 102(11): 1592-1599.

The Role of Tregs in Glioma-Mediated Immunosuppression: Potential Target for Intervention
Humphries, W., J. Wei, et al. (2010). Neurosurgery Clinics of North America 21(1): 125-137.

Intratumoral mediated immunosuppression is prognostic in genetically engineered murine models of glioma and correlates to immunotherapeutic responses
Kong, L. Y., A. S. Wu, et al. (2010). Clinical Cancer Research 16(23): 5722-5733.

A novel small molecule, LLL12, inhibits STAT3 phosphorylation and activities and exhibits potent growth-suppressive activity in human cancer cells
Lin, L., B. Hutzen, et al. (2010). Neoplasia (New York, NY) 12(1): 39.

Inhibition of JAK/STAT signaling pathway prevents high-glucose-induced increase in endothelin-1 synthesis in human endothelial cells
Manea, S.-A., A. Manea, et al. (2010). Cell and Tissue Research 340(1): 71-79.

Activation of host tissue trophic factors through JAK-STAT3 signaling: A mechanism of mesenchymal stem cell-mediated cardiac repair
Shabbir, A., D. Zisa, et al. (2010). American Journal of Physiology – Heart and Circulatory Physiology 299(5): H1428-H1438.

Glioblastoma cancer-initiating cells inhibit T-cell proliferation and effector responses by the signal transducers and activators of transcription 3 pathway
Wei, J., J. Barr, et al. (2010). Molecular Cancer Therapeutics 9(1): 67-78.


The role of tregs in human glioma patients and their inhibition with a novel STAT-3 inhibitor
Heimberger, A. B., L. Y. Kong, et al. (2009). Clinical Neurosurgery 56: 98-106.

A novel phosphorylated STAT3 inhibitor enhances T cell cytotoxicity against melanoma through inhibition of regulatory T cells
Kong, L. Y., J. Wei, et al. (2009). Cancer Immunol Immunother 58(7): 1023-1032.

Therapeutic suppression of constitutive and inducible JAK\STAT activation in head and neck squamous cell carcinoma
Kupferman, M. E., A. Jayakumar, et al. (2009). Journal of Experimental Therapeutics and Oncology 8(2): 117-127.

Leptin attenuates cardiac apoptosis after chronic ischaemic injury
McGaffin, K. R., B. Zou, et al. (2009). Cardiovascular Research 83(2): 313-324.

Targeted therapy for advanced prostate cancer: Looking through new lenses
Vogiatzi, P., M. Cassone, et al. (2009). Drug News and Perspectives 22(10): 593-601.


A novel inhibitor of signal transducers and activators of transcription 3 activation is efficacious against established central nervous system melanoma and inhibits regulatory T cells
Kong, L. Y., M. K. Abou-Ghazal, et al. (2008). Clinical Cancer Research 14(18): 5759-5768.

WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation
Verstovsek, S., T. Manshouri, et al. (2008). Clinical Cancer Research 14(3): 788-796.

The JAK kinases: Not just another kinase drug discovery target
Wilks, A. F. (2008). Seminars in Cell and Developmental Biology 19(4): 319-328.


WP1066 disrupts janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells
Ferrajoli, A., S. Faderl, et al. (2007). Cancer Research 67(23): 11291-11299.

A novel small molecule inhibitor of signal transducers and activators of transcription 3 reverses immune tolerance in malignant glioma patients
Hussain, S. F., L. Y. Kong, et al. (2007). Cancer Research 67(20): 9630-9636.

A novel inhibitor of the STAT3 pathway induces apoptosis in malignant glioma cells both in vitro and in vivo
Iwamaru, A., S. Szymanski, et al. (2007). Oncogene 26(17): 2435-2444.

Activation of integrin-linked kinase is a critical prosurvival pathway induced in leukemic cells by bone marrow-derived stromal cells
Tabe, Y., L. Jin, et al. (2007). Cancer Research 67(2): 684-694.

Roles of mTOR and STAT3 in autophagy induced by telomere 3′ overhang-specific DNA oligonucleotides.
Yokoyama, T., Y. Kondo, et al. (2007). Autophagy 3(5): 496-498.

WP1122 Bibliography


EXTH-07. Design And Evaluation Of WP1122, An Inhibitor Of Glycolysis With Increased CNS Update
Felix, E., I. Fokt, J. Arumugam, M. Krasinski, M. Tai Khuong, R. Zielinski, S. Skora, V. Radjendirane and W. Priebe (2018). Neuro-Oncology 20(suppl_6): vi86-vi86.

Deglycosylation of PD-L1 by 2-deoxyglucose reverses PARP inhibitor-induced immunosuppression in triple-negative breast cancer
Shao, B., C.-W. Li, S.-O. Lim, L. Sun, Y.-J. Lai, J. Hou, C. Liu, C.-W. Chang, Y. Qiu and J.-M. J. A. j. o. c. r. Hsu (2018). 8(9): 1837.

WP1122: Novel Therapy for CNS Malignancies
Conrad, C. National Brain Tumor Society

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