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Discovery of isoquinoline sulfonamides as allosteric gyrase inhibitors with activity against fluoroquinolone-resistant bacteria.
Bakker AT, Kotsogianni I, Avalos M, Punt JM, Liu B, Piermarini D, Gagestein B, Slingerland CJ, Zhang L, Willemse JJ, Ghimire LB, van den Berg RJHBN, Janssen APA, Ottenhoff THM, van Boeckel CAA, van Wezel GP, Ghilarov D, Martin NI, van der Stelt M. Bakker AT, et al. Among authors: van boeckel caa. Nat Chem. 2024 Sep;16(9):1462-1472. doi: 10.1038/s41557-024-01516-x. Epub 2024 Jun 19. Nat Chem. 2024. PMID: 38898213 Free PMC article.
A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence.
Jiang M, Huizenga MCW, Wirt JL, Paloczi J, Amedi A, van den Berg RJBHN, Benz J, Collin L, Deng H, Di X, Driever WF, Florea BI, Grether U, Janssen APA, Hankemeier T, Heitman LH, Lam TW, Mohr F, Pavlovic A, Ruf I, van den Hurk H, Stevens AF, van der Vliet D, van der Wel T, Wittwer MB, van Boeckel CAA, Pacher P, Hohmann AG, van der Stelt M. Jiang M, et al. Among authors: van boeckel caa. Nat Commun. 2023 Dec 5;14(1):8039. doi: 10.1038/s41467-023-43606-3. Nat Commun. 2023. PMID: 38052772 Free PMC article.
Epi-Cyclophellitol Cyclosulfate, a Mechanism-Based Endoplasmic Reticulum α-Glucosidase II Inhibitor, Blocks Replication of SARS-CoV-2 and Other Coronaviruses.
Thaler M, Ofman TP, Kok K, Heming JJA, Moran E, Pickles I, Leijs AA, van den Nieuwendijk AMCH, van den Berg RJBHN, Ruijgrok G, Armstrong Z, Salgado-Benvindo C, Ninaber DK, Snijder EJ, van Boeckel CAA, Artola M, Davies GJ, Overkleeft HS, van Hemert MJ. Thaler M, et al. Among authors: van boeckel caa. ACS Cent Sci. 2024 Jul 25;10(8):1594-1608. doi: 10.1021/acscentsci.4c00506. eCollection 2024 Aug 28. ACS Cent Sci. 2024. PMID: 39220688 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: van boeckel caa. 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.
Comprehensive structure-activity-relationship of azaindoles as highly potent FLT3 inhibitors.
Grimm SH, Gagestein B, Keijzer JF, Liu N, Wijdeven RH, Lenselink EB, Tuin AW, van den Nieuwendijk AMCH, van Westen GJP, van Boeckel CAA, Overkleeft HS, Neefjes J, van der Stelt M. Grimm SH, et al. Among authors: van boeckel caa. Bioorg Med Chem. 2019 Mar 1;27(5):692-699. doi: 10.1016/j.bmc.2019.01.006. Epub 2019 Jan 14. Bioorg Med Chem. 2019. PMID: 30661740 Free article.
Identification and development of biphenyl substituted iminosugars as improved dual glucosylceramide synthase/neutral glucosylceramidase inhibitors.
Ghisaidoobe AT, van den Berg RJ, Butt SS, Strijland A, Donker-Koopman WE, Scheij S, van den Nieuwendijk AM, Koomen GJ, van Loevezijn A, Leemhuis M, Wennekes T, van der Stelt M, van der Marel GA, van Boeckel CA, Aerts JM, Overkleeft HS. Ghisaidoobe AT, et al. J Med Chem. 2014 Nov 13;57(21):9096-104. doi: 10.1021/jm501181z. Epub 2014 Oct 17. J Med Chem. 2014. PMID: 25250725
26 results