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Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist.
Balıkçı E, Marques AMC, Bauer LG, Seupel R, Bennett J, Raux B, Buchan K, Simelis K, Singh U, Rogers C, Ward J, Cheng C, Szommer T, Schützenhofer K, Elkins JM, Sloman DL, Ahel I, Fedorov O, Brennan PE, Huber KVM. Balıkçı E, et al. Among authors: brennan pe. J Med Chem. 2024 May 9;67(9):7245-7259. doi: 10.1021/acs.jmedchem.4c00072. Epub 2024 Apr 18. J Med Chem. 2024. PMID: 38635563 Free PMC article.
Characterization of covalent inhibitors that disrupt the interaction between the tandem SH2 domains of SYK and FCER1G phospho-ITAM.
Bashore FM, Katis VL, Du Y, Sikdar A, Wang D, Bradshaw WJ, Rygiel KA, Leisner TM, Chalk R, Mishra S, Williams CA, Gileadi O, Brennan PE, Wiley JC, Gockley J, Cary GA, Carter GW, Young JE, Pearce KH, Fu H; Emory-Sage-SGC TREAT-AD Center; Axtman AD. Bashore FM, et al. Among authors: brennan pe. PLoS One. 2024 Feb 15;19(2):e0293548. doi: 10.1371/journal.pone.0293548. eCollection 2024. PLoS One. 2024. PMID: 38359047 Free PMC article.
Regulation of inositol 5-phosphatase activity by the C2 domain of SHIP1 and SHIP2.
Bradshaw WJ, Kennedy EC, Moreira T, Smith LA, Chalk R, Katis VL, Benesch JLP, Brennan PE, Murphy EJ, Gileadi O. Bradshaw WJ, et al. Among authors: brennan pe. Structure. 2024 Apr 4;32(4):453-466.e6. doi: 10.1016/j.str.2024.01.005. Epub 2024 Feb 2. Structure. 2024. PMID: 38309262 Free article.
Discovery of FERM domain protein-protein interaction inhibitors for MSN and CD44 as a potential therapeutic approach for Alzheimer's disease.
Du Y, Bradshaw WJ, Leisner TM, Annor-Gyamfi JK, Qian K, Bashore FM, Sikdar A, Nwogbo FO, Ivanov AA, Frye SV, Gileadi O, Brennan PE, Levey AI; Emory-Sage-SGC TREAT-AD Center; Axtman AD, Pearce KH, Fu H, Katis VL. Du Y, et al. Among authors: brennan pe. J Biol Chem. 2023 Dec;299(12):105382. doi: 10.1016/j.jbc.2023.105382. Epub 2023 Oct 21. J Biol Chem. 2023. PMID: 37866628 Free PMC article.
Characterization of covalent inhibitors that disrupt the interaction between the tandem SH2 domains of SYK and FCER1G phospho-ITAM.
Bashore FM, Katis VL, Du Y, Sikdar A, Wang D, Bradshaw WJ, Rygiel KA, Leisner TM, Chalk R, Mishra S, Williams AC, Gileadi O, Brennan PE, Wiley JC, Gockley J, Cary GA, Carter GW, Young JE, Pearce KH, Fu H; Emory-Sage-SGC TREAT-AD Center; Axtman AD. Bashore FM, et al. Among authors: brennan pe. bioRxiv [Preprint]. 2023 Jul 29:2023.07.28.551026. doi: 10.1101/2023.07.28.551026. bioRxiv. 2023. Update in: PLoS One. 2024 Feb 15;19(2):e0293548. doi: 10.1371/journal.pone.0293548. PMID: 37547005 Free PMC article. Updated. Preprint.
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