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Page 1
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.
Ketcham JM, Harwood SJ, Aranda R, Aloiau AN, Bobek BM, Briere DM, Burns AC, Caddell Haatveit K, Calinisan A, Clarine J, Elliott A, Engstrom LD, Gunn RJ, Ivetac A, Jones B, Kuehler J, Lawson JD, Nguyen N, Parker C, Pearson KE, Rahbaek L, Saechao B, Wang X, Waters A, Waters L, Watkins AH, Olson P, Smith CR, Christensen JG, Marx MA. Ketcham JM, et al. Among authors: ivetac a. J Med Chem. 2024 Mar 28;67(6):4936-4949. doi: 10.1021/acs.jmedchem.4c00078. Epub 2024 Mar 13. J Med Chem. 2024. PMID: 38477582 Free PMC article.
Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits.
Smith CR, Kulyk S, Ahmad MUD, Arkhipova V, Christensen JG, Gunn RJ, Ivetac A, Ketcham JM, Kuehler J, Lawson JD, Thomas NC, Wang X, Marx MA. Smith CR, et al. Among authors: ivetac a. RSC Med Chem. 2022 Sep 27;13(12):1549-1564. doi: 10.1039/d2md00163b. eCollection 2022 Dec 14. RSC Med Chem. 2022. PMID: 36545438 Free PMC article.
Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X-Ray Cocrystallography.
Smith CR, Chen D, Christensen JG, Coulombe R, Féthière J, Gunn RJ, Hollander J, Jones B, Ketcham JM, Khare S, Kuehler J, Lawson JD, Marx MA, Olson P, Pearson KE, Ren C, Tsagris D, Ulaganathan T, Van't Veer I, Wang X, Ivetac A. Smith CR, et al. Among authors: ivetac a. J Med Chem. 2024 Jan 11;67(1):774-781. doi: 10.1021/acs.jmedchem.3c02140. Epub 2023 Dec 29. J Med Chem. 2024. PMID: 38156904 Free PMC article.
The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading.
Sudhakar N, Yan L, Qiryaqos F, Engstrom LD, Laguer J, Calinisan A, Hebbert A, Waters L, Moya K, Bowcut V, Vegar L, Ketcham JM, Ivetac A, Smith CR, Lawson JD, Rahbaek L, Clarine J, Nguyen N, Saechao B, Parker C, Elliott AJ, Vanderpool D, He L, Hover LD, Fernandez-Banet J, Coma S, Pachter JA, Hallin J, Marx MA, Briere DM, Christensen JG, Olson P, Haling J, Khare S. Sudhakar N, et al. Among authors: ivetac a. Mol Cancer Ther. 2024 Apr 19. doi: 10.1158/1535-7163.MCT-23-0870. Online ahead of print. Mol Cancer Ther. 2024. PMID: 38641404
Design and evaluation of achiral, non-atropisomeric 4-(aminomethyl)phthalazin-1(2H)-one derivatives as novel PRMT5/MTA inhibitors.
Smith CR, Aranda R, Christensen JG, Engstrom LD, Gunn RJ, Ivetac A, Ketcham JM, Kuehler J, David Lawson J, Marx MA, Olson P, Thomas NC, Wang X, Waters LM, Kulyk S. Smith CR, et al. Among authors: ivetac a. Bioorg Med Chem. 2022 Oct 1;71:116947. doi: 10.1016/j.bmc.2022.116947. Epub 2022 Jul 26. Bioorg Med Chem. 2022. PMID: 35926325 Free article.
Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction.
Ketcham JM, Haling J, Khare S, Bowcut V, Briere DM, Burns AC, Gunn RJ, Ivetac A, Kuehler J, Kulyk S, Laguer J, Lawson JD, Moya K, Nguyen N, Rahbaek L, Saechao B, Smith CR, Sudhakar N, Thomas NC, Vegar L, Vanderpool D, Wang X, Yan L, Olson P, Christensen JG, Marx MA. Ketcham JM, et al. Among authors: ivetac a. J Med Chem. 2022 Jul 28;65(14):9678-9690. doi: 10.1021/acs.jmedchem.2c00741. Epub 2022 Jul 14. J Med Chem. 2022. PMID: 35833726 Free PMC article.
Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers.
Smith CR, Aranda R, Bobinski TP, Briere DM, Burns AC, Christensen JG, Clarine J, Engstrom LD, Gunn RJ, Ivetac A, Jean-Baptiste R, Ketcham JM, Kobayashi M, Kuehler J, Kulyk S, Lawson JD, Moya K, Olson P, Rahbaek L, Thomas NC, Wang X, Waters LM, Marx MA. Smith CR, et al. Among authors: ivetac a. J Med Chem. 2022 Feb 10;65(3):1749-1766. doi: 10.1021/acs.jmedchem.1c01900. Epub 2022 Jan 18. J Med Chem. 2022. PMID: 35041419 Free article.
Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp3 character and an exquisite selectivity profile.
Bigi-Botterill SV, Ivetac A, Bradshaw EL, Cole D, Dougan DR, Ermolieff J, Halkowycz P, Johnson B, McBride C, Pickens J, Sabat M, Swann S. Bigi-Botterill SV, et al. Among authors: ivetac a. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127405. doi: 10.1016/j.bmcl.2020.127405. Epub 2020 Jul 12. Bioorg Med Chem Lett. 2020. PMID: 32738982 Free article.
Correction to "Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure".
Lanier M, Pickens J, Bigi SV, Bradshaw-Pierce EL, Chambers A, Cheruvallath ZS, Cole D, Dougan DR, Ermolieff J, Gibson T, Halkowycz P, Hirokawa A, Ivetac A, McBride C, Miura J, Nunez E, Sabat M, Tyhonas J, Wang H, Wang X, Swann S. Lanier M, et al. Among authors: ivetac a. ACS Med Chem Lett. 2017 Nov 8;8(12):1341. doi: 10.1021/acsmedchemlett.7b00457. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259759 Free PMC article.
1,2,4-Triazolo-[1,5-a]pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors With a Novel Monodentate Binding Interaction.
Ahmed S, Ayscough A, Barker GR, Canning HE, Davenport R, Downham R, Harrison D, Jenkins K, Kinsella N, Livermore DG, Wright S, Ivetac AD, Skene R, Wilkens SJ, Webster NA, Hendrick AG. Ahmed S, et al. Among authors: ivetac ad. J Med Chem. 2017 Jul 13;60(13):5663-5672. doi: 10.1021/acs.jmedchem.7b00352. Epub 2017 Jun 24. J Med Chem. 2017. PMID: 28594552
28 results