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Page 1
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: bergstrom da. 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.
RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across FGFR2 Alterations and Resistance Mutations.
Subbiah V, Sahai V, Maglic D, Bruderek K, Touré BB, Zhao S, Valverde R, O'Hearn PJ, Moustakas DT, Schönherr H, Gerami-Moayed N, Taylor AM, Hudson BM, Houde DJ, Pal D, Foster L, Gunaydin H, Ayaz P, Sharon DA, Goyal L, Schram AM, Kamath S, Sherwin CA, Schmidt-Kittler O, Jen KY, Ricard F, Wolf BB, Shaw DE, Bergstrom DA, Watters J, Casaletto JB. Subbiah V, et al. Among authors: bergstrom da. Cancer Discov. 2023 Sep 6;13(9):2012-2031. doi: 10.1158/2159-8290.CD-23-0475. Cancer Discov. 2023. PMID: 37270847 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: bergstrom da. 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.
Evaluating patient-derived colorectal cancer xenografts as preclinical models by comparison with patient clinical data.
Nunes M, Vrignaud P, Vacher S, Richon S, Lièvre A, Cacheux W, Weiswald LB, Massonnet G, Chateau-Joubert S, Nicolas A, Dib C, Zhang W, Watters J, Bergstrom D, Roman-Roman S, Bièche I, Dangles-Marie V. Nunes M, et al. Cancer Res. 2015 Apr 15;75(8):1560-6. doi: 10.1158/0008-5472.CAN-14-1590. Epub 2015 Feb 24. Cancer Res. 2015. PMID: 25712343
The Dolaflexin-based Antibody-Drug Conjugate XMT-1536 Targets the Solid Tumor Lineage Antigen SLC34A2/NaPi2b.
Bodyak ND, Mosher R, Yurkovetskiy AV, Yin M, Bu C, Conlon PR, Demady DR, DeVit MJ, Gumerov DR, Gurijala VR, Lee W, McGillicuddy D, Park PU, Poling LL, Protopova M, Qin L, Stevenson CA, Ter-Ovanesyan E, Uttard A, Xiao D, Xu J, Xu L, Bergstrom DA, Lowinger TB. Bodyak ND, et al. Among authors: bergstrom da. Mol Cancer Ther. 2021 May;20(5):896-905. doi: 10.1158/1535-7163.MCT-20-0183. Epub 2021 Mar 15. Mol Cancer Ther. 2021. PMID: 33722858
Dolaflexin: A Novel Antibody-Drug Conjugate Platform Featuring High Drug Loading and a Controlled Bystander Effect.
Yurkovetskiy AV, Bodyak ND, Yin M, Thomas JD, Clardy SM, Conlon PR, Stevenson CA, Uttard A, Qin L, Gumerov DR, Ter-Ovanesyan E, Bu C, Johnson AJ, Gurijala VR, McGillicuddy D, DeVit MJ, Poling LL, Protopopova M, Xu L, Zhang Q, Park PU, Bergstrom DA, Lowinger TB. Yurkovetskiy AV, et al. Among authors: bergstrom da. Mol Cancer Ther. 2021 May;20(5):885-895. doi: 10.1158/1535-7163.MCT-20-0166. Epub 2021 Mar 15. Mol Cancer Ther. 2021. PMID: 33722857
An accessible pharmacodynamic transcriptional biomarker for notch target engagement.
Tanis KQ, Podtelezhnikov AA, Blackman SC, Hing J, Railkar RA, Lunceford J, Klappenbach JA, Wei B, Harman A, Camargo LM, Shah S, Finney EM, Hardwick JS, Loboda A, Watters J, Bergstrom DA, Demuth T, Herman GA, Strack PR, Iannone R. Tanis KQ, et al. Among authors: bergstrom da. Clin Pharmacol Ther. 2016 Apr;99(4):370-80. doi: 10.1002/cpt.335. Epub 2016 Feb 17. Clin Pharmacol Ther. 2016. PMID: 26765077 Clinical Trial.
63 results