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Page 1
Inhibiting peptidylarginine deiminases (PAD1-4) by targeting a Ca2+ dependent allosteric binding site.
Dakin LA, Xing L, Hall J, Ding W, Vajdos FF, Pelker JW, Ramsey S, Balbo P, Sahasrabudhe PV, Banker ME, Choi WY, Wright SW, Chang JS, Curto JM, Davoren JE, Drozda SE, Fennell KF, Futatsugi K, Kortum S, Lee KL, Liu S, Lovering F, Nicki JA, Trujillo JI, Vincent F, Schnute ME. Dakin LA, et al. Among authors: chang js. Nat Commun. 2025 May 16;16(1):4579. doi: 10.1038/s41467-025-59919-4. Nat Commun. 2025. PMID: 40379660 Free PMC article.
Identification of type-II inhibitors using kinase structures.
Lovering F, McDonald J, Whitlock GA, Glossop PA, Phillips C, Bent A, Sabnis Y, Ryan M, Fitz L, Lee J, Chang JS, Han S, Kurumbail R, Thorarensen A. Lovering F, et al. Among authors: chang js. Chem Biol Drug Des. 2012 Nov;80(5):657-64. doi: 10.1111/j.1747-0285.2012.01443.x. Epub 2012 Sep 3. Chem Biol Drug Des. 2012. PMID: 22759374
Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: chang js. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
Rational approach to highly potent and selective apoptosis signal-regulating kinase 1 (ASK1) inhibitors.
Lovering F, Morgan P, Allais C, Aulabaugh A, Brodfuehrer J, Chang J, Coe J, Ding W, Dowty H, Fleming M, Frisbie R, Guzova J, Hepworth D, Jasti J, Kortum S, Kurumbail R, Mohan S, Papaioannou N, Strohbach JW, Vincent F, Lee K, Zapf CW. Lovering F, et al. Eur J Med Chem. 2018 Feb 10;145:606-621. doi: 10.1016/j.ejmech.2017.12.041. Epub 2017 Dec 15. Eur J Med Chem. 2018. PMID: 29348070
Structural basis of the acyl-transfer mechanism of human GPAT1.
Johnson ZL, Ammirati M, Wasilko DJ, Chang JS, Noell S, Foley TL, Yoon H, Smith K, Asano S, Hales K, Wan M, Yang Q, Piotrowski MA, Farley KA, Gilbert T, Aschenbrenner LM, Fennell KF, Dutra JK, Xu M, Guo C, Varghese AE, Bellenger J, Quinn A, Am Ende CW, West GM, Griffor MC, Bennett D, Calabrese M, Steppan CM, Han S, Wu H. Johnson ZL, et al. Among authors: chang js. Nat Struct Mol Biol. 2023 Jan;30(1):22-30. doi: 10.1038/s41594-022-00884-7. Epub 2022 Dec 15. Nat Struct Mol Biol. 2023. PMID: 36522428
Discovery, Characterization, and Structure of a Cell Active PAD2 Inhibitor Acting through a Novel Allosteric Mechanism.
Byrnes LJ, Choi WY, Balbo P, Banker ME, Chang J, Chen S, Cheng X, Cong Y, Culp J, Di H, Griffor M, Hall J, Meng X, Morgan B, Mousseau JJ, Nicki J, O'Connell T, Ramsey S, Shaginian A, Shanker S, Trujillo J, Wan J, Vincent F, Wright SW, Vajdos F. Byrnes LJ, et al. ACS Chem Biol. 2024 Oct 18;19(10):2186-2197. doi: 10.1021/acschembio.4c00397. Epub 2024 Sep 24. ACS Chem Biol. 2024. PMID: 39316753
Preclinical characterization of the Omicron XBB.1.5-adapted BNT162b2 COVID-19 vaccine.
Modjarrad K, Che Y, Chen W, Wu H, Cadima CI, Muik A, Maddur MS, Tompkins KR, Martinez LT, Cai H, Ramos M, Mensah S, Cumbia B, Falcao L, McKeen AP, Chang JS, Fennell KF, Huynh KW, McLellan TJ, Sahasrabudhe PV, Chen W, Cerswell M, Garcia MA, Li S, Sharma R, Li W, Dizon KP, Duarte S, Gillett F, Smith R, Illenberger DM, Efferen KS, Vogel AB, Anderson AS, Şahin U, Swanson KA. Modjarrad K, et al. Among authors: chang js. NPJ Vaccines. 2024 Nov 20;9(1):229. doi: 10.1038/s41541-024-01013-9. NPJ Vaccines. 2024. PMID: 39567521 Free PMC article.
Peptidylarginine Deiminase (PAD) Inhibitor Optimization through Displacement of a Trapped Water Molecule.
Schnute ME, Chinigo GM, Futatsugi K, Yamaguchi M, Bagley SW, Banker ME, Chang JS, Chen MZ, Choi WY, Corbett MS, Drozda SE, Ebner DC, Garcia-Irizarry C, Hicklin R, Hoy S, Jiao W, Kortum S, Lee KL, Limburg DC, Lovering F, Moreno A, Mousseau JJ, Pan S, Parikh MD, Pelker JW, Ramsey S, Reilly U, Rescourio G, Schmitt DC, Simpson B, Skrzypek GJ, Smaltz DJ, Taylor AP, Torella R, Trujillo JI, Vajdos FF, Wepy JA, Wright SW, Blakemore DC, Vincent F, Clerin VM. Schnute ME, et al. Among authors: chang js. ACS Med Chem Lett. 2025 Jul 9;16(8):1662-1669. doi: 10.1021/acsmedchemlett.5c00372. eCollection 2025 Aug 14. ACS Med Chem Lett. 2025. PMID: 40832545
1,727 results