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CD47-blocking Antibody ZL-1201 Promotes Tumor-associated Macrophage Phagocytic Activity and Enhances the Efficacy of the Therapeutic Antibodies and Chemotherapy.
Cao A, Yi J, Tang X, Szeto CW, Wu R, Wan B, Fang X, Li S, Wang L, Wang L, Li J, Ye Q, Huang T, Hsu K, Kabbarah O, Zhou H. Cao A, et al. Among authors: huang t. Cancer Res Commun. 2022 Nov 10;2(11):1404-1417. doi: 10.1158/2767-9764.CRC-22-0266. eCollection 2022 Nov. Cancer Res Commun. 2022. PMID: 36970051 Free PMC article.
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
Rew Y, Du X, Eksterowicz J, Zhou H, Jahchan N, Zhu L, Yan X, Kawai H, McGee LR, Medina JC, Huang T, Chen C, Zavorotinskaya T, Sutimantanapi D, Waszczuk J, Jackson E, Huang E, Ye Q, Fantin VR, Sun D. Rew Y, et al. Among authors: huang t, huang e. J Med Chem. 2018 Sep 13;61(17):7767-7784. doi: 10.1021/acs.jmedchem.8b00743. Epub 2018 Aug 23. J Med Chem. 2018. PMID: 30091920
ZL-1211 Exhibits Robust Antitumor Activity by Enhancing ADCC and Activating NK Cell-mediated Inflammation in CLDN18.2-High and -Low Expressing Gastric Cancer Models.
Konno H, Lin T, Wu R, Dai X, Li S, Wang G, Chen M, Li W, Wang L, Sun BC, Luo Z, Huang T, Chen Y, Zhang J, Ye Q, Bellovin D, Wan B, Kang L, Szeto C, Hsu K, Kabbarah O. Konno H, et al. Among authors: huang t. Cancer Res Commun. 2022 Sep 7;2(9):937-950. doi: 10.1158/2767-9764.CRC-22-0216. eCollection 2022 Sep. Cancer Res Commun. 2022. PMID: 36922936 Free PMC article.
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
Du X, Eksterowicz J, Zhou H, Rew Y, Zhu L, Yan X, Medina JC, Huang T, Chen X, Sutimantanapi D, Jahchan N, Kong W, Sun J, Zavorotinskaya T, Ye Q, Fantin VR, Sun D. Du X, et al. Among authors: huang t. J Med Chem. 2019 Jul 25;62(14):6751-6764. doi: 10.1021/acs.jmedchem.9b00711. Epub 2019 Jul 5. J Med Chem. 2019. PMID: 31274313
Orally Bioavailable Small-Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression through Blockade of Adenosine Production.
Du X, Moore J, Blank BR, Eksterowicz J, Sutimantanapi D, Yuen N, Metzger T, Chan B, Huang T, Chen X, Chen Y, Duong F, Kong W, Chang JH, Sun J, Zavorotinskaya T, Ye Q, Junttila MR, Ndubaku C, Friedman LS, Fantin VR, Sun D. Du X, et al. Among authors: huang t. J Med Chem. 2020 Sep 24;63(18):10433-10459. doi: 10.1021/acs.jmedchem.0c01086. Epub 2020 Sep 9. J Med Chem. 2020. PMID: 32865411
Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists.
Lucas BS, Aaron W, An S, Austin RJ, Brown M, Chan H, Chong A, Hungate R, Huang T, Jiang B, Johnson MG, Kaizerman JA, Lee G, McMinn DL, Orf J, Powers JP, Rong M, Toteva MM, Uyeda C, Wickramasinghe D, Xu G, Ye Q, Zhong W. Lucas BS, et al. Among authors: huang t. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3618-22. doi: 10.1016/j.bmcl.2010.04.110. Epub 2010 Apr 28. Bioorg Med Chem Lett. 2010. PMID: 20493695
Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines.
Kaizerman JA, Aaron W, An S, Austin R, Brown M, Chong A, Huang T, Hungate R, Jiang B, Johnson MG, Lee G, Lucas BS, Orf J, Rong M, Toteva MM, Wickramasinghe D, Xu G, Ye Q, Zhong W, McMinn DL. Kaizerman JA, et al. Among authors: huang t. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4607-10. doi: 10.1016/j.bmcl.2010.06.006. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20594845
Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit.
Brown ML, Aaron W, Austin RJ, Chong A, Huang T, Jiang B, Kaizerman JA, Lee G, Lucas BS, McMinn DL, Orf J, Rong M, Toteva MM, Xu G, Ye Q, Zhong W, Degraffenreid MR, Wickramasinghe D, Powers JP, Hungate R, Johnson MG. Brown ML, et al. Among authors: huang t. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5206-9. doi: 10.1016/j.bmcl.2011.07.052. Epub 2011 Jul 23. Bioorg Med Chem Lett. 2011. PMID: 21840217
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