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Page 1
Mechanistic insights into a heterobifunctional degrader-induced PTPN2/N1 complex.
Hao Q, Rathinaswamy MK, Klinge KL, Bratkowski M, Mafi A, Baumgartner CK, Hamel KM, Veits GK, Jain R, Catalano C, Fitzgerald M, Hird AW, Park E, Vora HU, Henderson JA, Longenecker K, Hutchins CW, Qiu W, Scapin G, Sun Q, Stoll VS, Sun C, Li P, Eaton D, Stokoe D, Fisher SL, Nasveschuk CG, Paddock M, Kort ME. Hao Q, et al. Among authors: hutchins cw. Commun Chem. 2024 Aug 16;7(1):183. doi: 10.1038/s42004-024-01263-7. Commun Chem. 2024. PMID: 39152201 Free PMC article.
The PTPN2/PTPN1 inhibitor ABBV-CLS-484 unleashes potent anti-tumour immunity.
Baumgartner CK, Ebrahimi-Nik H, Iracheta-Vellve A, Hamel KM, Olander KE, Davis TGR, McGuire KA, Halvorsen GT, Avila OI, Patel CH, Kim SY, Kammula AV, Muscato AJ, Halliwill K, Geda P, Klinge KL, Xiong Z, Duggan R, Mu L, Yeary MD, Patti JC, Balon TM, Mathew R, Backus C, Kennedy DE, Chen A, Longenecker K, Klahn JT, Hrusch CL, Krishnan N, Hutchins CW, Dunning JP, Bulic M, Tiwari P, Colvin KJ, Chuong CL, Kohnle IC, Rees MG, Boghossian A, Ronan M, Roth JA, Wu MJ, Suermondt JSMT, Knudsen NH, Cheruiyot CK, Sen DR, Griffin GK, Golub TR, El-Bardeesy N, Decker JH, Yang Y, Guffroy M, Fossey S, Trusk P, Sun IM, Liu Y, Qiu W, Sun Q, Paddock MN, Farney EP, Matulenko MA, Beauregard C, Frost JM, Yates KB, Kym PR, Manguso RT. Baumgartner CK, et al. Among authors: hutchins cw. Nature. 2023 Oct;622(7984):850-862. doi: 10.1038/s41586-023-06575-7. Epub 2023 Oct 4. Nature. 2023. PMID: 37794185 Free PMC article.
Discovery of a Potent Chloroacetamide GPX4 Inhibitor with Bioavailability to Enable Target Engagement in Mice, a Potential Tool Compound for Inducing Ferroptosis In Vivo.
Randolph JT, O'Connor MJ, Han F, Hutchins CW, Siu YA, Cho M, Zheng Y, Hickson JA, Markley JL, Manaves V, Algire M, Baker KA, Chapman AM, Gopalakrishnan SM, Panchal SC, Foster-Duke K, Stolarik DF, Kempf-Grote A, Dammeier D, Fossey S, Sun Q, Sun C, Shen Y, Dart MJ, Kati WM, Lai A, Firestone AJ, Kort ME. Randolph JT, et al. Among authors: hutchins cw. J Med Chem. 2023 Mar 23;66(6):3852-3865. doi: 10.1021/acs.jmedchem.2c01415. Epub 2023 Mar 6. J Med Chem. 2023. PMID: 36877935
Discovery of Small Molecule Interleukin 17A Inhibitors with Novel Binding Mode and Stoichiometry: Optimization of DNA-Encoded Chemical Library Hits to In Vivo Active Compounds.
Ramos AL, Goedken ER, Frank KE, Argiriadi MA, Bazzaz S, Bian Z, Brown JTC, Centrella PA, Chen HJ, Disch JS, Donner PL, Duignan DB, Gikunju D, Greszler SN, Guié MA, Habeshian S, Hartl HE, Hein CD, Hutchins CW, Jetson R, Keefe AD, Khan H, Li HQ, Olszewski A, Ortiz Cardona BJ, Osuma A, Panchal SC, Phelan R, Qiu W, Shotwell JB, Shrestha A, Srikumaran M, Su Z, Sun C, Upadhyay AK, Wood MD, Wu H, Zhang R, Zhang Y, Zhao G, Zhu H, Webster MP. Ramos AL, et al. Among authors: hutchins cw. J Med Chem. 2024 Apr 25;67(8):6456-6494. doi: 10.1021/acs.jmedchem.3c02397. Epub 2024 Apr 4. J Med Chem. 2024. PMID: 38574366
CRISPR Screen Reveals BRD2/4 Molecular Glue-like Degrader via Recruitment of DCAF16.
Shergalis AG, Marin VL, Rhee DY, Senaweera S, McCloud RL, Ronau JA, Hutchins CW, McLoughlin S, Woller KR, Warder SE, Vasudevan A, Reitsma JM. Shergalis AG, et al. Among authors: hutchins cw. ACS Chem Biol. 2023 Feb 17;18(2):331-339. doi: 10.1021/acschembio.2c00747. Epub 2023 Jan 19. ACS Chem Biol. 2023. PMID: 36656921
Implications of the Conformationally Flexible, Macrocyclic Structure of the First-Generation, Direct-Acting Anti-Viral Paritaprevir on Its Solid Form Complexity and Chameleonic Behavior.
Sheikh AY, Mattei A, Miglani Bhardwaj R, Hong RS, Abraham NS, Schneider-Rauber G, Engstrom KM, Diwan M, Henry RF, Gao Y, Juarez V, Jordan E, DeGoey DA, Hutchins CW. Sheikh AY, et al. Among authors: hutchins cw. J Am Chem Soc. 2021 Oct 27;143(42):17479-17491. doi: 10.1021/jacs.1c06837. Epub 2021 Oct 12. J Am Chem Soc. 2021. PMID: 34637297
Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.
Fidanze SD, Liu D, Mantei RA, Hasvold LA, Pratt JK, Sheppard GS, Wang L, Holms JH, Dai Y, Aguirre A, Bogdan A, Dietrich JD, Marjanovic J, Park CH, Hutchins CW, Lin X, Bui MH, Huang X, Wilcox D, Li L, Wang R, Kovar P, Magoc TJ, Rajaraman G, Albert DH, Shen Y, Kati WM, McDaniel KF. Fidanze SD, et al. Among authors: hutchins cw. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1804-1810. doi: 10.1016/j.bmcl.2018.04.020. Epub 2018 Apr 11. Bioorg Med Chem Lett. 2018. PMID: 29678460
Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
McDaniel KF, Wang L, Soltwedel T, Fidanze SD, Hasvold LA, Liu D, Mantei RA, Pratt JK, Sheppard GS, Bui MH, Faivre EJ, Huang X, Li L, Lin X, Wang R, Warder SE, Wilcox D, Albert DH, Magoc TJ, Rajaraman G, Park CH, Hutchins CW, Shen JJ, Edalji RP, Sun CC, Martin R, Gao W, Wong S, Fang G, Elmore SW, Shen Y, Kati WM. McDaniel KF, et al. Among authors: hutchins cw. J Med Chem. 2017 Oct 26;60(20):8369-8384. doi: 10.1021/acs.jmedchem.7b00746. Epub 2017 Oct 12. J Med Chem. 2017. PMID: 28949521
44 results