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Page 1
Structure-Based Discovery of a Series of Covalent, Orally Bioavailable, and Selective BFL1 Inhibitors.
Palisse A, Cheung T, Blokhuis A, Cogswell T, Martins BS, Riemens R, Schellekens R, Battocchio G, Jansen C, Cottee MA, Ornell K, Sacchetto C, Leon L, van Hoek-Emmelot M, Bostock M, Brauer BL, Beaumont K, Lucas SCC, Ahmed S, Blackwell JH, Börjesson U, Gohlke A, Gramatikov IMT, Hargreaves D, van Hoeven V, Kantae V, Kupcova L, Milbradt AG, Seneviratne U, Su N, Vales J, Wang H, White MJ, Kinzel O. Palisse A, et al. Among authors: kantae v. J Med Chem. 2024 Dec 26;67(24):22055-22079. doi: 10.1021/acs.jmedchem.4c01995. Epub 2024 Dec 6. J Med Chem. 2024. PMID: 39641779
Structure-Based Optimization of a Series of Covalent, Cell Active Bfl-1 Inhibitors.
Lucas SCC, Blackwell JH, Börjesson U, Hargreaves D, Milbradt AG, Bostock MJ, Ahmed S, Beaumont K, Cheung T, Demanze S, Gohlke A, Guerot C, Haider A, Kantae V, Kauffman GW, Kinzel O, Kupcova L, Lainchbury MD, Lamb ML, Leon L, Palisse A, Sacchetto C, Storer RI, Su N, Thomson C, Vales J, Chen Y, Hu X. Lucas SCC, et al. Among authors: kantae v. J Med Chem. 2024 Sep 26;67(18):16455-16479. doi: 10.1021/acs.jmedchem.4c01288. Epub 2024 Sep 18. J Med Chem. 2024. PMID: 39291659
Development of a Series of Pyrrolopyridone MAT2A Inhibitors.
Atkinson SJ, Bagal SK, Argyrou A, Askin S, Cheung T, Chiarparin E, Coen M, Collie IT, Dale IL, De Fusco C, Dillman K, Evans L, Feron LJ, Foster AJ, Grondine M, Kantae V, Lamont GM, Lamont S, Lynch JT, Nilsson Lill S, Robb GR, Saeh J, Schimpl M, Scott JS, Smith J, Srinivasan B, Tentarelli S, Vazquez-Chantada M, Wagner D, Walsh JJ, Watson D, Williamson B. Atkinson SJ, et al. Among authors: kantae v. J Med Chem. 2024 Mar 28;67(6):4541-4559. doi: 10.1021/acs.jmedchem.3c01860. Epub 2024 Mar 11. J Med Chem. 2024. PMID: 38466661
Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl-b Inhibitors.
Mfuh AM, Boerth JA, Bommakanti G, Chan C, Chinn AJ, Code E, Fricke PJ, Giblin KA, Gohlke A, Hansel C, Hariparsad N, Hughes SJ, Jin M, Kantae V, Kavanagh SL, Lamb ML, Lane J, Moore R, Puri T, Quinn TR, Reddy I, Robb GR, Robbins KJ, Gancedo Rodrigo M, Schimpl M, Singh B, Singh M, Tang H, Thomson C, Walsh JJ, Ware J, Watson IDG, Ye MW, Wrigley GL, Zhang AX, Zhang Y, Grimster NP. Mfuh AM, et al. Among authors: kantae v. J Med Chem. 2024 Jan 25;67(2):1500-1512. doi: 10.1021/acs.jmedchem.3c02083. Epub 2024 Jan 16. J Med Chem. 2024. PMID: 38227216
Structure-Activity Relationship Studies of α-Ketoamides as Inhibitors of the Phospholipase A and Acyltransferase Enzyme Family.
Zhou J, Mock ED, Al Ayed K, Di X, Kantae V, Burggraaff L, Stevens AF, Martella A, Mohr F, Jiang M, van der Wel T, Wendel TJ, Ofman TP, Tran Y, de Koster N, van Westen GJP, Hankemeier T, van der Stelt M. Zhou J, et al. Among authors: kantae v. J Med Chem. 2020 Sep 10;63(17):9340-9359. doi: 10.1021/acs.jmedchem.0c00522. Epub 2020 Aug 13. J Med Chem. 2020. PMID: 32787138 Free PMC article.
Discovery of a NAPE-PLD inhibitor that modulates emotional behavior in mice.
Mock ED, Mustafa M, Gunduz-Cinar O, Cinar R, Petrie GN, Kantae V, Di X, Ogasawara D, Varga ZV, Paloczi J, Miliano C, Donvito G, van Esbroeck ACM, van der Gracht AMF, Kotsogianni I, Park JK, Martella A, van der Wel T, Soethoudt M, Jiang M, Wendel TJ, Janssen APA, Bakker AT, Donovan CM, Castillo LI, Florea BI, Wat J, van den Hurk H, Wittwer M, Grether U, Holmes A, van Boeckel CAA, Hankemeier T, Cravatt BF, Buczynski MW, Hill MN, Pacher P, Lichtman AH, van der Stelt M. Mock ED, et al. Among authors: kantae v. Nat Chem Biol. 2020 Jun;16(6):667-675. doi: 10.1038/s41589-020-0528-7. Epub 2020 May 11. Nat Chem Biol. 2020. PMID: 32393901 Free PMC article.
Resurrecting the phoenix: When an assay fails.
Srinivasan B, Kantae V, Robinson J. Srinivasan B, et al. Among authors: kantae v. Med Res Rev. 2020 Sep;40(5):1776-1793. doi: 10.1002/med.21670. Epub 2020 Apr 13. Med Res Rev. 2020. PMID: 32285494 Review.
Identification of α,β-Hydrolase Domain Containing Protein 6 as a Diacylglycerol Lipase in Neuro-2a Cells.
van Esbroeck ACM, Kantae V, Di X, van der Wel T, den Dulk H, Stevens AF, Singh S, Bakker AT, Florea BI, Stella N, Overkleeft HS, Hankemeier T, van der Stelt M. van Esbroeck ACM, et al. Among authors: kantae v. Front Mol Neurosci. 2019 Nov 26;12:286. doi: 10.3389/fnmol.2019.00286. eCollection 2019. Front Mol Neurosci. 2019. PMID: 31849602 Free PMC article.
21 results