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Page 1
Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1.
Cherney EC, Zhang L, Nara S, Zhu X, Gullo-Brown J, Maley D, Lin TA, Hunt JT, Huang C, Yang Z, Darienzo C, Discenza L, Ranasinghe A, Grubb M, Ziemba T, Traeger SC, Li X, Johnston K, Kopcho L, Fereshteh M, Foster K, Stefanski K, Fargnoli J, Swanson J, Brown J, Delpy D, Seitz SP, Borzilleri R, Vite G, Balog A. Cherney EC, et al. Among authors: zhu x. ACS Med Chem Lett. 2021 Jan 28;12(2):288-294. doi: 10.1021/acsmedchemlett.0c00668. eCollection 2021 Feb 11. ACS Med Chem Lett. 2021. PMID: 33603977 Free PMC article.
[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.
Shan W, Balog A, Nation A, Zhu X, Chen J, Cvijic ME, Geng J, Rizzo CA, Spires T Jr, Attar RM, Obermeier M, Traeger S, Dai J, Zhang Y, Galella M, Trainor G, Vite GD, Gavai AV. Shan W, et al. Among authors: zhu x. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5707-5711. doi: 10.1016/j.bmcl.2016.10.059. Epub 2016 Oct 21. Bioorg Med Chem Lett. 2016. PMID: 27836399
Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form.
Nelp MT, Kates PA, Hunt JT, Newitt JA, Balog A, Maley D, Zhu X, Abell L, Allentoff A, Borzilleri R, Lewis HA, Lin Z, Seitz SP, Yan C, Groves JT. Nelp MT, et al. Among authors: zhu x. Proc Natl Acad Sci U S A. 2018 Mar 27;115(13):3249-3254. doi: 10.1073/pnas.1719190115. Epub 2018 Mar 12. Proc Natl Acad Sci U S A. 2018. PMID: 29531094 Free PMC article.
Discovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy.
Zhang L, Cherney EC, Zhu X, Lin TA, Gullo-Brown J, Maley D, Johnston-Allegretto K, Kopcho L, Fereshteh M, Huang C, Li X, Traeger SC, Dhar G, Anandam A, Mahankali S, Padmanabhan S, Rajanna P, Murali V, Mariappan T, Borzilleri R, Vite G, Hunt JT, Balog A. Zhang L, et al. Among authors: zhu x. ACS Med Chem Lett. 2021 Mar 2;12(3):494-501. doi: 10.1021/acsmedchemlett.1c00014. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33738077 Free PMC article.
Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors.
Cherney EC, Zhang L, Guo W, Huang A, Williams D, Seitz S, Shan W, Zhu X, Gullo-Brown J, Maley D, Lin TA, Hunt JT, Huang C, Yang Z, D'Arienzo CJ, Discenza LN, Ranasinghe A, Grubb MF, Traeger SC, Li X, Johnston KA, Kopcho L, Fereshteh M, Foster KA, Stefanski K, Delpy D, Dhar G, Anandam A, Mahankali S, Padmanabhan S, Rajanna P, Murali V, Mariappan TT, Pattasseri S, Nimje RY, Hong Z, Kempson J, Rampulla R, Mathur A, Gupta A, Borzilleri R, Vite G, Balog A. Cherney EC, et al. Among authors: zhu x. ACS Med Chem Lett. 2021 Jun 16;12(7):1143-1150. doi: 10.1021/acsmedchemlett.1c00236. eCollection 2021 Jul 8. ACS Med Chem Lett. 2021. PMID: 34267885 Free PMC article.
Discovery of Non-Nucleotide Small-Molecule STING Agonists via Chemotype Hybridization.
Cherney EC, Zhang L, Lo J, Huynh T, Wei D, Ahuja V, Quesnelle C, Schieven GL, Futran A, Locke GA, Lin Z, Monereau L, Chaudhry C, Blum J, Li S, Fereshteh M, Li-Wang B, Gangwar S, Pan C, Chong C, Zhu X, Posy SL, Sack JS, Zhang P, Ruzanov M, Harner M, Akhtar F, Schroeder GM, Vite G, Fink B. Cherney EC, et al. Among authors: zhu x. J Med Chem. 2022 Feb 24;65(4):3518-3538. doi: 10.1021/acs.jmedchem.1c01986. Epub 2022 Feb 2. J Med Chem. 2022. PMID: 35108011
Discovery of KT-474─a Potent, Selective, and Orally Bioavailable IRAK4 Degrader for the Treatment of Autoimmune Diseases.
Zheng X, Ji N, Campbell V, Slavin A, Zhu X, Chen D, Rong H, Enerson B, Mayo M, Sharma K, Browne CM, Klaus CR, Li H, Massa G, McDonald AA, Shi Y, Sintchak M, Skouras S, Walther DM, Yuan K, Zhang Y, Kelleher J, Liu G, Luo X, Mainolfi N, Weiss MM. Zheng X, et al. Among authors: zhu x. J Med Chem. 2024 Oct 24;67(20):18022-18037. doi: 10.1021/acs.jmedchem.4c01305. Epub 2024 Aug 16. J Med Chem. 2024. PMID: 39151120 Free PMC article. Clinical Trial.
Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B-Cell Lymphoma.
Weiss MM, Zheng X, Ji N, Browne CM, Campbell V, Chen D, Enerson B, Fei X, Huang X, Klaus CR, Li H, Mayo M, McDonald AA, Paul A, Rong H, Sharma K, Shi Y, Slavin A, Walther DM, Yuan K, Zhang Y, Zhu X, Kelleher J, Walker D, Mainolfi N. Weiss MM, et al. Among authors: zhu x. J Med Chem. 2024 Jul 11;67(13):10548-10566. doi: 10.1021/acs.jmedchem.3c01823. Epub 2024 Jun 26. J Med Chem. 2024. PMID: 38920289
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