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Page 1
Strategic Fluorination to Achieve a Potent, Selective, Metabolically Stable, and Orally Bioavailable Inhibitor of CSNK2.
Ong HW, Yang X, Smith JL, Taft-Benz S, Howell S, Dickmander RJ, Havener TM, Sanders MK, Brown JW, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM. Ong HW, et al. Among authors: axtman ad. Molecules. 2024 Sep 2;29(17):4158. doi: 10.3390/molecules29174158. Molecules. 2024. PMID: 39275006 Free PMC article.
Discovery and Characterization of a Chemical Probe for Cyclin-Dependent Kinase-Like 2.
Bashore FM, Min SM, Chen X, Howell S, Rinderle CH, Morel G, Silvaroli JA, Wells CI, Bunnell BA, Drewry DH, Pabla NS, Ultanir SK, Bullock AN, Axtman AD. Bashore FM, et al. Among authors: axtman ad. ACS Med Chem Lett. 2024 Jul 3;15(8):1325-1333. doi: 10.1021/acsmedchemlett.4c00219. eCollection 2024 Aug 8. ACS Med Chem Lett. 2024. PMID: 39140040 Free PMC article.
More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication.
Ong HW, Yang X, Smith JL, Dickmander RJ, Brown JW, Havener TM, Taft-Benz S, Howell S, Sanders MK, Capener JL, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM. Ong HW, et al. Among authors: axtman ad. J Med Chem. 2024 Jul 25;67(14):12261-12313. doi: 10.1021/acs.jmedchem.4c00962. Epub 2024 Jul 3. J Med Chem. 2024. PMID: 38959455 Free PMC article.
Discovery and Characterization of a Chemical Probe for Cyclin-Dependent Kinase-Like 2.
Bashore FM, Min SM, Chen X, Howell S, Rinderle CH, Morel G, Silvaroli JA, Wells CI, Bunnell BA, Drewry DH, Pabla NS, Ultanir SK, Bullock AN, Axtman AD. Bashore FM, et al. Among authors: axtman ad. bioRxiv [Preprint]. 2024 May 14:2024.05.12.593776. doi: 10.1101/2024.05.12.593776. bioRxiv. 2024. Update in: ACS Med Chem Lett. 2024 Jul 03;15(8):1325-1333. doi: 10.1021/acsmedchemlett.4c00219 PMID: 38798634 Free PMC article. Updated. Preprint.
Discovery and optimization of narrow spectrum inhibitors of Tousled like kinase 2 (TLK2) using quantitative structure activity relationships.
Asquith CRM, East MP, Laitinen T, Alamillo-Ferrer C, Hartikainen E, Wells CI, Axtman AD, Drewry DH, Tizzard GJ, Poso A, Willson TM, Johnson GL. Asquith CRM, et al. Among authors: axtman ad. Eur J Med Chem. 2024 May 5;271:116357. doi: 10.1016/j.ejmech.2024.116357. Epub 2024 Apr 2. Eur J Med Chem. 2024. PMID: 38636130 Free PMC article.
Illumination of understudied ciliary kinases.
Flax RG, Rosston P, Rocha C, Anderson B, Capener JL, Durcan TM, Drewry DH, Prinos P, Axtman AD. Flax RG, et al. Among authors: axtman ad. Front Mol Biosci. 2024 Mar 8;11:1352781. doi: 10.3389/fmolb.2024.1352781. eCollection 2024. Front Mol Biosci. 2024. PMID: 38523660 Free PMC article. Review.
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: axtman ad. PLoS One. 2024 Feb 15;19(2):e0293548. doi: 10.1371/journal.pone.0293548. eCollection 2024. PLoS One. 2024. PMID: 38359047 Free PMC article.
49 results