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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 der gracht amf. 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.
Chemical Control over T-Cell Activation in Vivo Using Deprotection of trans-Cyclooctene-Modified Epitopes.
van der Gracht AMF, de Geus MAR, Camps MGM, Ruckwardt TJ, Sarris AJC, Bremmers J, Maurits E, Pawlak JB, Posthoorn MM, Bonger KM, Filippov DV, Overkleeft HS, Robillard MS, Ossendorp F, van Kasteren SI. van der Gracht AMF, et al. ACS Chem Biol. 2018 Jun 15;13(6):1569-1576. doi: 10.1021/acschembio.8b00155. Epub 2018 May 11. ACS Chem Biol. 2018. PMID: 29733186 Free PMC article.
When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists.
Vilums M, Zweemer AJ, Barmare F, van der Gracht AM, Bleeker DC, Yu Z, de Vries H, Gross R, Clemens J, Krenitsky P, Brussee J, Stamos D, Saunders J, Heitman LH, IJzerman AP. Vilums M, et al. Eur J Med Chem. 2015 Mar 26;93:121-34. doi: 10.1016/j.ejmech.2015.01.063. Epub 2015 Feb 2. Eur J Med Chem. 2015. PMID: 25666912