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267 results

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Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2.
Schönherr H, Ayaz P, Taylor AM, Casaletto JB, Touré BB, Moustakas DT, Hudson BM, Valverde R, Zhao S, O'Hearn PJ, Foster L, Sharon DA, Garfinkle S, Giordanetto F, Lescarbeau A, Kurukulasuriya R, Gerami-Moayed N, Maglic D, Bruderek K, Naik G, Gunaydin H, Mader MM, Boezio AA, McLean TH, Chen R, Wang Y, Shaw DE, Watters J, Bergstrom DA. Schönherr H, et al. Among authors: shaw de. Proc Natl Acad Sci U S A. 2024 Feb 6;121(6):e2317756121. doi: 10.1073/pnas.2317756121. Epub 2024 Feb 1. Proc Natl Acad Sci U S A. 2024. PMID: 38300868 Free PMC article.
Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia.
Varkaris A, Pazolli E, Gunaydin H, Wang Q, Pierce L, Boezio AA, Bulku A, DiPietro L, Fridrich C, Frost A, Giordanetto F, Hamilton EP, Harris K, Holliday M, Hunter TL, Iskandar A, Ji Y, Larivée A, LaRochelle JR, Lescarbeau A, Llambi F, Lormil B, Mader MM, Mar BG, Martin I, McLean TH, Michelsen K, Pechersky Y, Puente-Poushnejad E, Raynor K, Rogala D, Samadani R, Schram AM, Shortsleeves K, Swaminathan S, Tajmir S, Tan G, Tang Y, Valverde R, Wehrenberg B, Wilbur J, Williams BR, Zeng H, Zhang H, Walters WP, Wolf BB, Shaw DE, Bergstrom DA, Watters J, Fraser JS, Fortin PD, Kipp DR. Varkaris A, et al. Among authors: shaw de. Cancer Discov. 2024 Feb 8;14(2):240-257. doi: 10.1158/2159-8290.CD-23-0944. Cancer Discov. 2024. PMID: 37916956 Free PMC article.
Low levels of endogenous anabolic androgenic steroids in females with severe asthma taking corticosteroids.
Yasinska V, Gómez C, Kolmert J, Ericsson M, Pohanka A, James A, Andersson LI, Sparreman-Mikus M, Sousa AR, Riley JH, Bates S, Bakke PS, Zounemat Kermani N, Caruso M, Chanez P, Fowler SJ, Geiser T, Howarth PH, Horváth I, Krug N, Montuschi P, Sanak M, Behndig A, Shaw DE, Knowles RG, Dahlén B, Maitland-van der Zee AH, Sterk PJ, Djukanovic R, Adcock IM, Chung KF, Wheelock CE, Dahlén SE, Wikström Jonsson E; U-BIOPRED Study Group. Yasinska V, et al. Among authors: shaw de. ERJ Open Res. 2023 Oct 2;9(5):00269-2023. doi: 10.1183/23120541.00269-2023. eCollection 2023 Sep. ERJ Open Res. 2023. PMID: 37868143 Free PMC article.
Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors.
Taylor AM, Williams BR, Giordanetto F, Kelley EH, Lescarbeau A, Shortsleeves K, Tang Y, Walters WP, Arrazate A, Bowman C, Brophy E, Chan EW, Deshmukh G, Greisman JB, Hunsaker TL, Kipp DR, Saenz Lopez-Larrocha P, Maddalo D, Martin IJ, Maragakis P, Merchant M, Murcko M, Nisonoff H, Nguyen V, Nguyen V, Orozco O, Owen C, Pierce L, Schmidt M, Shaw DE, Smith S, Therrien E, Tran JC, Watters J, Waters NJ, Wilbur J, Willmore L. Taylor AM, et al. Among authors: shaw de. J Med Chem. 2023 Oct 12;66(19):13384-13399. doi: 10.1021/acs.jmedchem.3c00483. Epub 2023 Sep 29. J Med Chem. 2023. PMID: 37774359
Functional dynamics and allosteric modulation of TRPA1.
Koldsø H, Jensen MØ, Jogini V, Shaw DE. Koldsø H, et al. Among authors: shaw de. Structure. 2023 Dec 7;31(12):1556-1566.e3. doi: 10.1016/j.str.2023.08.018. Epub 2023 Sep 19. Structure. 2023. PMID: 37729917 Free article.
Design and Synthesis of Inhibitors of the E3 Ligase SMAD Specific E3 Ubiquitin Protein Ligase 1 as a Treatment for Lung Remodeling in Pulmonary Arterial Hypertension.
Shaw DE, Smith N, Beerli R, Cotesta S, D'Alessandro PL, Edwards AM, Lattmann R, Lizos D, Pulz R, Rooney L, Sohal B, Rynn C, Taylor J, Troxler T, Williams G, Guth S, Rowlands D. Shaw DE, et al. J Med Chem. 2023 Jun 22;66(12):8130-8139. doi: 10.1021/acs.jmedchem.3c00229. Epub 2023 Jun 9. J Med Chem. 2023. PMID: 37294287
267 results