Identification of selective neuropeptide Y2 peptide agonists

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 2, 2007, Pages 538-541

  DeCarr, Lynn B ^a   Buckholz, Thomas M ^a   Coish, Philip D G ^a   Fathi, Zahra ^a   Fisk, Stephen E ^a   Mays, Michelle R ^a   O'Connor, Stephen J ^a   Lumb, Kevin J ^a  

^a BAYER CORPORATION   (United States)

Author keywords

NPY; NPY2; Obesity; Peptide; PYY

Indexed keywords

AMINOBENZOIC ACID DERIVATIVE; NEUROPEPTIDE Y RECEPTOR AGONIST; NEUROPEPTIDE Y1 RECEPTOR; NEUROPEPTIDE Y2 RECEPTOR; NEUROPEPTIDE Y5 RECEPTOR; PEPTIDE YY;

AMINO TERMINAL SEQUENCE; APPETITE; ARTICLE; BINDING AFFINITY; DRUG IDENTIFICATION; DRUG POTENCY; PROTEIN MODIFICATION;

BINDING, COMPETITIVE; CELL LINE; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; EATING; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HUMANS; INDICATORS AND REAGENTS; PEPTIDE YY; RECEPTORS, NEUROPEPTIDE Y;

EID: 33846092678     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.10.007     Document Type: Article

References (29)

1. Small C.J., and Bloom S.R. Expert Opin. Investig. Drugs 14 (2005) 647
2. Batterham R.L., Cowley M.A., Small C.J., Herzog H., Cohen M.A., Dakin C.L., Wren A.M., Brynes A.E., Low M.J., Ghatei M.A., Cone R.D., and Bloom S.R. Nature 418 (2002) 650
3. Batterham R.L., Cohen M.A., Ellis S.M., Le Roux C.W., Withers D.J., Frost G.S., Ghatei M.A., and Bloom S.R. N. Eng. J. Med. 349 (2003) 941
4. Challis B.G., Pinnock S.B., Coll A.P., Carter R.N., Dickson S.L., and O'Rahilly S. Biochem. Biophys. Res. Commun. 311 (2003) 915
5. Cox J.E., and Randich A. Peptides 25 (2004) 985
6. Pittner R.A., Moore C.X., Bhavsar S.P., Gedulin B.R., Smith P.A., Jodka C.M., Parkes D.G., Paterniti J.R., Srivastava V.P., and Young A.A. Int. J. Obes. Relat. Metab. Disord. 28 (2004) 963
7. Chelikani P.K., Haver A.C., and Reidelberger R.D. Endocrinology 146 (2005) 879
8. Degen L., Oesch S., Casanova M., Graf S., Ketterer S., Drewe J., and Beglinger C. Gastroenterology 129 (2005) 1430
9. Koegler F.H., Enriori P.J., Billes S.K., Takahashi D.L., Martin M.S., Clark R.L., Evans A.E., Grove K.L., Cameron J.L., and Cowley M.A. Diabetes 54 (2005) 3198
10. Moran T.H., Smedh U., Kinzig K.P., Scott K.A., Knipp S., and Ladenheim E.E. Am. J. Physiol. Regul. Integr. Comp. Physiol. 288 (2005) R384
11. Sileno A.P., Brandt G.C., Spann B.M., and Quay S.C. Int. J. Obes. 30 (2006) 68
12. Abbott C.R., Small C.J., Kennedy A.R., Neary N.M., Sajedi A., Ghatei M.A., and Bloom S.R. Brain Res. 1043 (2005) 139
13. Gerald C., Walker M.W., Criscione L., Gustafson E.L., Batzl-Hartmann C., Smith K.E., Vaysse P., Durkin M.M., Laz T.M., Linemeyer D.L., Schaffhauser A.O., Whitebread S., Hofbauer K.G., Taber R.I., Branchek T.A., and Weinshank R.L. Nature 382 (1996) 168
14. Mullins D., Kirby D., Hwa J., Guzzi M., Rivier J., and Parker E. Mol. Pharmacol. 60 (2001) 534
15. Cabrele C., and Beck-Sickinger A.G. J. Pept. Sci. 6 (2000) 97
16. Balasubramaniam A. Curr. Pharm. Des. 9 (2003) 1165
17. Balasubramaniam A., Servin A.L., Rigel D.F., Rouyer-Fessard C.R., and Laburthe M. Pept. Res. 1 (1988) 32
18. Beck-Sickinger A.G., Hoffmann E., Gaida W., Grouzmann E., Dürr H., and Jung G. Bioorg. Med. Chem. Lett. 3 (1993) 937
19. Rist B., Zerbe O., Ingenhoven N., Scapozza L., Peers C., Vaughan P.F., McDonald R.L., Wieland H.A., and Beck-Sickinger A.G. FEBS Lett. 394 (1996) 169
20. 18 HPLC and identity was confirmed with electrospray mass spectrometry.
21. 125I]-labeled human PYY (Perkin-Elmer), 200 μg wheatgerm agglutinin beads (Amersham), and membrane (10 μg) in a final volume of 200 μl. Nonspecific binding was defined with 1 μM PYY. Plates were incubated for 30 min at room temperature while shaking, removed from shaker, and kept at room temperature for an additional 2.5 h. The amount of radioactivity in the samples was quantified with a Wallac 1450 Microbeta Trilux liquid scintillation counter (Perkin-Elmer). Data were fit to a single-site binding model with Prism 3.03 (GraphPad Software).
22. 35S]GTPγS incorporated into KAN-TS membranes was quantified with a Wallac 1450 Microbeta Trilux liquid scintillation counter (Perkin-Elmer). Data were fit to a single-site binding model with Prism 3.03 (GraphPad Software).
23. 125I]-labeled PYY (Perkin-Elmer), and membrane (20-30 μg) in a final volume of 200 μl for 2 h at room temperature. Nonspecific binding was defined with 1 μM PYY. Following incubation, total content of the wells was transferred to Millipore HV plates (pretreated with 0.1% BSA), rapidly filtered, and washed thrice with 200 μl ice-cold binding buffer. Filter plates were air-dried, 15-20 μl scintillant added (Microscint O, Perkin-Elmer Life Sciences), and radioactivity quantified with a Wallac 1450 Microbeta Trilux liquid scintillation counter (Perkin-Elmer Life Sciences). Data were fit to a single-site binding model with Prism 3.03 (GraphPad Software).
24. 125I]-labeled human PYY (Perkin- Elmer), and membrane (10 μg) in a final volume of 200 μl for 2 h at room temperature. Nonspecific binding was defined with 1 μM PYY. Following the incubation, total content of the wells was transferred to Millipore HV plates (pretreated with 0.1% BSA and aspirated prior to transfer), rapidly filtered, and washed thrice with 200 μl ice-cold binding buffer. Filter plates were then air-dried, 15-20 μl scintillant added (Microscint O), and radioactivity quantified with a Wallac 1450 Microbeta Trilux liquid scintillation counter (Perkin-Elmer Life Sciences). Data were fit to a single-site binding model with Prism 3.03 (GraphPad Software).
25. Kurtzhals P., Havelund S., Jonassen I., Kiehr B., Larsen U.D., Ribel U., and Markussen J. Biochem. J. 312 (1995) 725
26. Harris J.M., and Chess R.B. Nat. Rev. Drug Disc. 2 (2003) 214
27. Rimland J.M., Seward E.P., Humbert Y., Ratti E., Trist D.G., and North R.A. Mol. Pharmacol. 49 (1996) 387
28. Larhammar D., Blomqvist A.G., Yee F., Jazin E., Yoo H., and Wahlested C. J. Biol. Chem. 267 (1992) 10935
29. Hu Y., Bloomquist B.T., Cornfield L.J., DeCarr L.B., Flores-Riveros J.R., Friedman L., Jiang P., Lewis-Higgins L., Sadlowski Y., Schaefer J., Velazquez N., and McCaleb M.L. J. Biol. Chem. 271 (1996) 26315