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Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.
Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha R, Rogers C, Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH. Chen P, et al. Among authors: chaikuad a. J Med Chem. 2016 Feb 25;59(4):1410-24. doi: 10.1021/acs.jmedchem.5b00209. Epub 2015 Apr 6. J Med Chem. 2016. PMID: 25799074 Free PMC article.
The ins and outs of selective kinase inhibitor development.
Müller S, Chaikuad A, Gray NS, Knapp S. Müller S, et al. Among authors: chaikuad a. Nat Chem Biol. 2015 Nov;11(11):818-21. doi: 10.1038/nchembio.1938. Nat Chem Biol. 2015. PMID: 26485069 No abstract available.
An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases.
Chaikuad A, Diharce J, Schröder M, Foucourt A, Leblond B, Casagrande AS, Désiré L, Bonnet P, Knapp S, Besson T. Chaikuad A, et al. J Med Chem. 2016 Nov 23;59(22):10315-10321. doi: 10.1021/acs.jmedchem.6b01083. Epub 2016 Nov 2. J Med Chem. 2016. PMID: 27766861
Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold.
Forster M, Chaikuad A, Dimitrov T, Döring E, Holstein J, Berger BT, Gehringer M, Ghoreschi K, Müller S, Knapp S, Laufer SA. Forster M, et al. Among authors: chaikuad a. J Med Chem. 2018 Jun 28;61(12):5350-5366. doi: 10.1021/acs.jmedchem.8b00571. Epub 2018 Jun 13. J Med Chem. 2018. PMID: 29852068
p63 uses a switch-like mechanism to set the threshold for induction of apoptosis.
Gebel J, Tuppi M, Chaikuad A, Hötte K, Schröder M, Schulz L, Löhr F, Gutfreund N, Finke F, Henrich E, Mezhyrova J, Lehnert R, Pampaloni F, Hummer G, Stelzer EHK, Knapp S, Dötsch V. Gebel J, et al. Among authors: chaikuad a. Nat Chem Biol. 2020 Oct;16(10):1078-1086. doi: 10.1038/s41589-020-0600-3. Epub 2020 Jul 27. Nat Chem Biol. 2020. PMID: 32719556
121 results