Characterization of binding properties of monoglyceride lipase inhibitors by a versatile fluorescence-based technique

Analytical Biochemistry

Volumn 399, Issue 1, 2010, Pages 132-134

  Savinainen, Juha R ^a   Yoshino, Megumi ^a   Minkkilä, Anna ^a   Nevalainen, Tapio ^a   Laitinen, Jarmo T ^a  

^a UNIVERSITY OF EASTERN FINLAND   (Finland)

Author keywords

[No Author keywords available]

Indexed keywords

AMINO ACIDS; BINDING ENERGY; FLUORESCENCE;

2-ARACHIDONOYL GLYCEROLS; BINDING PROPERTIES; DOSE-DEPENDENT; ENDOCANNABINOID; HIGH THROUGHPUT SCREENING METHODS; MONOGLYCERIDES; MULTIPLE BINDING SITES; REFERENCE COMPOUNDS;

BINDING SITES;

4 NITROPHENYL 4 [DIBENZO[D][1,3]DIOXOL 5 YL (HYDROXY)METHYL]PIPERADINE 1 CARBOXYLATE; 5 ETHOXY 3 (3 PHENOXYPHENYL) 1,3,4 OXADIAZOL 2(3H) ONE; 5 METHOXY 3 (3 PHENOXYPHENYL) 1,3,4 OXADIAZOL 2(3H) ONE; ACYLGLYCEROL LIPASE; ACYLGLYCEROL LIPASE INHIBITOR; ARACHIDONOYLTRIFLUOROMETHYLKETONE; ATM 113; ATM 114; CAY 10499; ENZYME INHIBITOR; JZL 184; METHYLARACHIDONYL FLUOROPHOSPHONATE; N ARACHIDONYLMALEIMIDE; UNCLASSIFIED DRUG;

ARTICLE; BINDING KINETICS; BINDING SITE; CONCENTRATION RESPONSE; CONTROLLED STUDY; FLUORESCENCE ANALYSIS; HIGH THROUGHPUT SCREENING; PRIORITY JOURNAL;

EID: 77649184344     PISSN: 00032697     EISSN: 10960309     Source Type: Journal    
DOI: 10.1016/j.ab.2009.12.009     Document Type: Article

References (11)

1. Saario S.M., Laitinen J.T. Therapeutic potential of endocannabinoid-hydrolysing enzyme inhibitors. Basic Clin. Pharmacol. Toxicol. 2007, 101:287-293.
2. Wang Y., Chanda P., Jones P.G., Kennedy J.F. A fluorescence-based assay for monoacylglycerol lipase compatible with inhibitor screening. Assay Drug Dev. Technol. 2008, 6:387-393.
3. Sun W.C., Gee K.R., Haugland R.P. Synthesis of novel fluorinated coumarins: excellent UV-light excitable fluorescent dyes. Bioorg. Med. Chem. Lett. 1998, 8:3107-3110.
4. Minkkilä A., Savinainen J.R., Käsnänen H., Xhaard H., Nevalainen T., Laitinen J.T., Poso A., Leppänen J., Saario S.M. Screening of various hormone-sensitive lipase inhibitors as endocannabinoid-hydrolyzing enzyme inhibitors. ChemMedChem 2009, 4:1253-1259.
5. Long J.Z., Nomura D.K., Cravatt B.F. Characterization of monoacylglycerol lipase inhibition reveals differences in central and peripheral endocannabinoid metabolism. Chem. Biol. 2009, 16:744-753.
6. Ben Ali Y., Chahinian H., Petry S., Muller G., Lebrun R., Verger R., Carrière F., Mandrich L., Rossi M., Manco G., Sarda L., Abousalham A. Use of an inhibitor to identify members of the hormone-sensitive lipase family. Biochemistry 2006, 45:14183-14191.
7. Saario S.M., Savinainen J.R., Laitinen J.T., Jarvinen T., Niemi R. Monoglyceride lipase-like enzymatic activity is responsible for hydrolysis of 2-arachidonoylglycerol in rat cerebellar membranes. Biochem. Pharmacol. 2004, 67:1381-1387.
8. Saario S.M., Salo O.M., Nevalainen T., Poso A., Laitinen J.T., Jarvinen T., Niemi R. Characterization of the sulfhydryl-sensitive site in the enzyme responsible for hydrolysis of 2-arachidonoyl-glycerol in rat cerebellar membranes. Chem. Biol. 2005, 12:649-656.
9. Scoichet B.K. Interpreting steep dose-response curves in early inhibitor discovery. J. Med. Chem. 2006, 29:7274-7277.
10. Matuszak N., Muccioli G.G., Labar G., Lambert D.M. Synthesis and in vitro evaluation of N-substituted maleimide derivatives as selective monoglyceride lipase inhibitors. J. Med. Chem. 2009, 52:7410-7420.
11. Muccioli G.G., Labar G., Lambert D.M. CAY10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious MGL assay. ChemBioChem 2008, 9:2704-2710.