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Your search keyword '"van der Stelt, Mario"' showing total 8 results
Start Over Author "van der Stelt, Mario" Publisher royal society of chemistry
8 results on '"van der Stelt, Mario"'

3. Novel activity-based probes for N-acylethanolamine acid amidase.

Author

Petracca, Rita, Romeo, Elisa, Baggelaar, Marc P., Artola, Marta, Pontis, Silvia, Ponzano, Stefano, Overkleeft, Herman S., van der Stelt, Mario, and Piomelli, Daniele

Subjects
AMIDASES, ANALGESICS, ANTI-inflammatory agents
Abstract

The cysteine hydrolase, N-acylethanolamine acid amidase (NAAA) is a promising target for analgesic and anti-inflammatory drugs. Here, we describe the development of two unprecedented NAAA-reactive activity-based probes as research tools for application in the discovery of new inhibitors and for the in-depth characterization of NAAA in its cellular environment. [ABSTRACT FROM AUTHOR]

Published
2017
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7. Development of an acid ceramidase activity-based probe.

Author

Ouairy, Cécile M. J., Ferraz, Maria J., Boot, Rolf G., Baggelaar, Marc P., van der Stelt, Mario, Appelman, Monique, van der Marel, Gijsbert A., Florea, Bogdan I., Aerts, Johannes M. F. G., and Overkleeft, Herman S.

Subjects
ACID ceramidase, GLYCOSPHINGOLIPIDS, MOLECULAR probes, METABOLISM, HYDROLYSIS, FREE fatty acids, FARBER disease
Abstract

Acid ceramidase is responsible for the ultimate step in the catabolism of (glyco)sphingolipids by hydrolysis of ceramide into sphingosine and free fatty acid. Deficiency in acid ceramidase is the molecular basis of Farber disease. Here we report the synthesis and characterization of an activity-based acid ceramidase probe. [ABSTRACT FROM AUTHOR]

Published
2015
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8. Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe.

Author

Gazzi T, Brennecke B, Atz K, Korn C, Sykes D, Forn-Cuni G, Pfaff P, Sarott RC, Westphal MV, Mostinski Y, Mach L, Wasinska-Kalwa M, Weise M, Hoare BL, Miljuš T, Mexi M, Roth N, Koers EJ, Guba W, Alker A, Rufer AC, Kusznir EA, Huber S, Raposo C, Zirwes EA, Osterwald A, Pavlovic A, Moes S, Beck J, Nettekoven M, Benito-Cuesta I, Grande T, Drawnel F, Widmer G, Holzer D, van der Wel T, Mandhair H, Honer M, Fingerle J, Scheffel J, Broichhagen J, Gawrisch K, Romero J, Hillard CJ, Varga ZV, van der Stelt M, Pacher P, Gertsch J, Ullmer C, McCormick PJ, Oddi S, Spaink HP, Maccarrone M, Veprintsev DB, Carreira EM, Grether U, and Nazaré M

Abstract

Despite its essential role in the (patho)physiology of several diseases, CB 2 R tissue expression profiles and signaling mechanisms are not yet fully understood. We report the development of a highly potent, fluorescent CB 2 R agonist probe employing structure-based reverse design. It commences with a highly potent, preclinically validated ligand, which is conjugated to a silicon-rhodamine fluorophore, enabling cell permeability. The probe is the first to preserve interspecies affinity and selectivity for both mouse and human CB 2 R. Extensive cross-validation (FACS, TR-FRET and confocal microscopy) set the stage for CB 2 R detection in endogenously expressing living cells along with zebrafish larvae. Together, these findings will benefit clinical translatability of CB 2 R based drugs., Competing Interests: The authors have no conflicts to declare., (This journal is © The Royal Society of Chemistry.)

Published
2022
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