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Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones.
Deng X, Elkins JM, Zhang J, Yang Q, Erazo T, Gomez N, Choi HG, Wang J, Dzamko N, Lee JD, Sim T, Kim N, Alessi DR, Lizcano JM, Knapp S, Gray NS. Deng X, et al. Among authors: knapp s. Eur J Med Chem. 2013;70:758-67. doi: 10.1016/j.ejmech.2013.10.052. Epub 2013 Oct 29. Eur J Med Chem. 2013. PMID: 24239623 Free PMC article.
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: knapp s. 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.
Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF.
Bennett J, Fedorov O, Tallant C, Monteiro O, Meier J, Gamble V, Savitsky P, Nunez-Alonso GA, Haendler B, Rogers C, Brennan PE, Müller S, Knapp S. Bennett J, et al. Among authors: knapp s. J Med Chem. 2016 Feb 25;59(4):1642-7. doi: 10.1021/acs.jmedchem.5b00458. Epub 2015 May 20. J Med Chem. 2016. PMID: 25974391 Free PMC article.
Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.
Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers C, Parikh M, Taylor A, Samas B, O'Mahony A, Berg E, Pallares G, Torrey AD, Treiber DK, Samardjiev IJ, Nasipak BT, Padilla-Benavides T, Wu Q, Imbalzano AN, Nickerson JA, Bunnage ME, Müller S, Knapp S, Owen DR. Gerstenberger BS, et al. Among authors: knapp s. J Med Chem. 2016 May 26;59(10):4800-11. doi: 10.1021/acs.jmedchem.6b00012. Epub 2016 May 3. J Med Chem. 2016. PMID: 27115555 Free PMC article.
Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis.
Myrianthopoulos V, Gaboriaud-Kolar N, Tallant C, Hall ML, Grigoriou S, Brownlee PM, Fedorov O, Rogers C, Heidenreich D, Wanior M, Drosos N, Mexia N, Savitsky P, Bagratuni T, Kastritis E, Terpos E, Filippakopoulos P, Müller S, Skaltsounis AL, Downs JA, Knapp S, Mikros E. Myrianthopoulos V, et al. Among authors: knapp s. J Med Chem. 2016 Oct 13;59(19):8787-8803. doi: 10.1021/acs.jmedchem.6b00355. Epub 2016 Sep 27. J Med Chem. 2016. PMID: 27617704 Free PMC article.
Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors.
Popp TA, Tallant C, Rogers C, Fedorov O, Brennan PE, Müller S, Knapp S, Bracher F. Popp TA, et al. Among authors: knapp s. J Med Chem. 2016 Oct 13;59(19):8889-8912. doi: 10.1021/acs.jmedchem.6b00774. Epub 2016 Sep 27. J Med Chem. 2016. PMID: 27673482
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. Among authors: knapp s. 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
Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies.
Igoe N, Bayle ED, Fedorov O, Tallant C, Savitsky P, Rogers C, Owen DR, Deb G, Somervaille TC, Andrews DM, Jones N, Cheasty A, Ryder H, Brennan PE, Müller S, Knapp S, Fish PV. Igoe N, et al. Among authors: knapp s. J Med Chem. 2017 Jan 26;60(2):668-680. doi: 10.1021/acs.jmedchem.6b01583. Epub 2017 Jan 9. J Med Chem. 2017. PMID: 28068087 Free article.
1,281 results