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Discovery of a Potent and Selective CDKL5/GSK3 Chemical Probe That Is Neuroprotective.
Ong HW, Liang Y, Richardson W, Lowry ER, Wells CI, Chen X, Silvestre M, Dempster K, Silvaroli JA, Smith JL, Wichterle H, Pabla NS, Ultanir SK, Bullock AN, Drewry DH, Axtman AD. Ong HW, et al. Among authors: bullock an. ACS Chem Neurosci. 2023 May 3;14(9):1672-1685. doi: 10.1021/acschemneuro.3c00135. Epub 2023 Apr 21. ACS Chem Neurosci. 2023. PMID: 37084253 Free PMC article.
Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor.
Kim HG, Tan L, Weisberg EL, Liu F, Canning P, Choi HG, Ezell SA, Wu H, Zhao Z, Wang J, Mandinova A, Griffin JD, Bullock AN, Liu Q, Lee SW, Gray NS. Kim HG, et al. Among authors: bullock an. ACS Chem Biol. 2013 Oct 18;8(10):2145-50. doi: 10.1021/cb400430t. Epub 2013 Aug 13. ACS Chem Biol. 2013. PMID: 23899692 Free PMC article.
Target 2035 - update on the quest for a probe for every protein.
Müller S, Ackloo S, Al Chawaf A, Al-Lazikani B, Antolin A, Baell JB, Beck H, Beedie S, Betz UAK, Bezerra GA, Brennan PE, Brown D, Brown PJ, Bullock AN, Carter AJ, Chaikuad A, Chaineau M, Ciulli A, Collins I, Dreher J, Drewry D, Edfeldt K, Edwards AM, Egner U, Frye SV, Fuchs SM, Hall MD, Hartung IV, Hillisch A, Hitchcock SH, Homan E, Kannan N, Kiefer JR, Knapp S, Kostic M, Kubicek S, Leach AR, Lindemann S, Marsden BD, Matsui H, Meier JL, Merk D, Michel M, Morgan MR, Mueller-Fahrnow A, Owen DR, Perry BG, Rosenberg SH, Saikatendu KS, Schapira M, Scholten C, Sharma S, Simeonov A, Sundström M, Superti-Furga G, Todd MH, Tredup C, Vedadi M, von Delft F, Willson TM, Winter GE, Workman P, Arrowsmith CH. Müller S, et al. Among authors: bullock an. RSC Med Chem. 2021 Dec 3;13(1):13-21. doi: 10.1039/d1md00228g. eCollection 2022 Jan 27. RSC Med Chem. 2021. PMID: 35211674 Free PMC article.
Development of an ALK2-biased BMP type I receptor kinase inhibitor.
Mohedas AH, Xing X, Armstrong KA, Bullock AN, Cuny GD, Yu PB. Mohedas AH, et al. Among authors: bullock an. ACS Chem Biol. 2013;8(6):1291-302. doi: 10.1021/cb300655w. Epub 2013 Apr 30. ACS Chem Biol. 2013. PMID: 23547776 Free PMC article.
BTB domain mutations perturbing KCTD15 oligomerisation cause a distinctive frontonasal dysplasia syndrome.
Miller KA, Cruz Walma DA, Pinkas DM, Tooze RS, Bufton JC, Richardson W, Manning CE, Hunt AE, Cros J, Hartill V, Parker MJ, McGowan SJ, Twigg SRF, Chalk R, Staunton D, Johnson D, Wilkie AOM, Bullock AN. Miller KA, et al. Among authors: bullock an. J Med Genet. 2024 Apr 19;61(5):490-501. doi: 10.1136/jmg-2023-109531. J Med Genet. 2024. PMID: 38296633 Free PMC article.
Still in Search for an EAAT Activator: GT949 Does Not Activate EAAT2, nor EAAT3 in Impedance and Radioligand Uptake Assays.
van Veggel L, Mocking TAM, Sijben HJ, Liu R, Gorostiola González M, Dilweg MA, Royakkers J, Li A, Kumar V, Dong YY, Bullock A, Sauer DB, Diliën H, van Westen GJP, Schreiber R, Heitman LH, Vanmierlo T. van Veggel L, et al. ACS Chem Neurosci. 2024 Apr 3;15(7):1424-1431. doi: 10.1021/acschemneuro.3c00731. Epub 2024 Mar 13. ACS Chem Neurosci. 2024. PMID: 38478848 Free PMC article.
Development of a Selective Dual Discoidin Domain Receptor (DDR)/p38 Kinase Chemical Probe.
Röhm S, Berger BT, Schröder M, Chatterjee D, Mathea S, Joerger AC, Pinkas DM, Bufton JC, Tjaden A, Kovooru L, Kudolo M, Pohl C, Bullock AN, Müller S, Laufer S, Knapp S. Röhm S, et al. Among authors: bullock an. J Med Chem. 2021 Sep 23;64(18):13451-13474. doi: 10.1021/acs.jmedchem.1c00868. Epub 2021 Sep 10. J Med Chem. 2021. PMID: 34506142
A new class of small molecule inhibitor of BMP signaling.
Sanvitale CE, Kerr G, Chaikuad A, Ramel MC, Mohedas AH, Reichert S, Wang Y, Triffitt JT, Cuny GD, Yu PB, Hill CS, Bullock AN. Sanvitale CE, et al. Among authors: bullock an. PLoS One. 2013 Apr 30;8(4):e62721. doi: 10.1371/journal.pone.0062721. Print 2013. PLoS One. 2013. PMID: 23646137 Free PMC article.
Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors.
Zhang T, Kwiatkowski N, Olson CM, Dixon-Clarke SE, Abraham BJ, Greifenberg AK, Ficarro SB, Elkins JM, Liang Y, Hannett NM, Manz T, Hao M, Bartkowiak B, Greenleaf AL, Marto JA, Geyer M, Bullock AN, Young RA, Gray NS. Zhang T, et al. Among authors: bullock an. Nat Chem Biol. 2016 Oct;12(10):876-84. doi: 10.1038/nchembio.2166. Epub 2016 Aug 29. Nat Chem Biol. 2016. PMID: 27571479 Free PMC article.
110 results