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Discovery and characterization of a specific inhibitor of serine-threonine kinase cyclin-dependent kinase-like 5 (CDKL5) demonstrates role in hippocampal CA1 physiology.
Castano A, Silvestre M, Wells CI, Sanderson JL, Ferrer CA, Ong HW, Lang Y, Richardson W, Silvaroli JA, Bashore FM, Smith JL, Genereux IM, Dempster K, Drewry DH, Pabla NS, Bullock AN, Benke TA, Ultanir SK, Axtman AD. Castano A, et al. Among authors: bullock an. Elife. 2023 Jul 25;12:e88206. doi: 10.7554/eLife.88206. Elife. 2023. PMID: 37490324 Free PMC article.
Toward target 2035: EUbOPEN - a public-private partnership to enable & unlock biology in the open.
Tredup C, Ackloo S, Beck H, Brown PJ, Bullock AN, Ciulli A, Dikic I, Edfeldt K, Edwards AM, Elkins JM, Farin HF, Fon EA, Gstaiger M, Günther J, Gustavsson AL, Häberle S, Isigkeit L, Huber KVM, Kotschy A, Krämer O, Leach AR, Marsden BD, Matsui H, Merk D, Montel F, Mulder MPC, Müller S, Owen DR, Proschak E, Röhm S, Stolz A, Sundström M, von Delft F, Willson TM, Arrowsmith CH, Knapp S. Tredup C, et al. Among authors: bullock an. RSC Med Chem. 2024 Nov 29. doi: 10.1039/d4md00735b. Online ahead of print. RSC Med Chem. 2024. PMID: 39618964 Free PMC article.
Covalent Inhibitors of KEAP1 with Exquisite Selectivity.
Fejes I, Markacz P, Tatai J, Rudas M, Dunkel P, Gyuris M, Nyerges M, Provost N, Duvivier V, Delerive P, Martiny V, Bristiel A, Vidal B, Richardson W, Rothweiler EM, Tranberg-Jensen J, Manning CE, Sweeney MN, Chalk R, Huber KVM, Bullock AN, Herner A, Seedorf K, Vinson C, Weber C, Kotschy A. Fejes I, et al. Among authors: bullock an. J Med Chem. 2024 Dec 12;67(23):21208-21222. doi: 10.1021/acs.jmedchem.4c02019. Epub 2024 Nov 21. J Med Chem. 2024. PMID: 39572012 Free PMC article.
Structure-Guided Conformational Restriction Leading to High-Affinity, Selective, and Cell-Active Tetrahydroisoquinoline-Based Noncovalent Keap1-Nrf2 Inhibitors.
Qin Y, Poulsen C, Narayanan D, Chan CB, Chen X, Montes BR, Tran KT, Mukminova E, Lin C, Gajhede M, Bullock AN, Olagnier D, Bach A. Qin Y, et al. Among authors: bullock an. J Med Chem. 2024 Nov 14;67(21):18828-18864. doi: 10.1021/acs.jmedchem.4c01221. Epub 2024 Oct 17. J Med Chem. 2024. PMID: 39418396
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: bullock an. 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.
Discovery of Two Highly Selective Structurally Orthogonal Chemical Probes for Activin Receptor-like Kinases 1 and 2.
Němec V, Remeš M, Beňovský P, Böck MC, Šranková E, Wong JF, Cros J, Williams E, Tse LH, Smil D, Ensan D, Isaac MB, Al-Awar R, Gomolková R, Ursachi VC, Fafílek B, Kahounová Z, Víchová R, Vacek O, Berger BT, Wells CI, Corona CR, Vasta JD, Robers MB, Krejci P, Souček K, Bullock AN, Knapp S, Paruch K. Němec V, et al. Among authors: bullock an. J Med Chem. 2024 Aug 8;67(15):12632-12659. doi: 10.1021/acs.jmedchem.4c00629. Epub 2024 Jul 18. J Med Chem. 2024. PMID: 39023313 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: bullock an. 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 of Conformationally Constrained ALK2 Inhibitors.
González-Álvarez H, Ensan D, Xin T, Wong JF, Zepeda-Velázquez CA, Cros J, Sweeney MN, Hoffer L, Kiyota T, Wilson BJ, Aman A, Roberts O, Isaac MB, Bullock AN, Smil D, Al-Awar R. González-Álvarez H, et al. Among authors: bullock an. J Med Chem. 2024 Mar 28;67(6):4707-4725. doi: 10.1021/acs.jmedchem.3c02308. Epub 2024 Mar 18. J Med Chem. 2024. PMID: 38498998 Free PMC article.
115 results