Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
SCREENING DERIVATIZED PEPTIDE LIBRARIES FOR TIGHT-BINDING INHIBITORS TO CARBONIC-ANHYDRASE-II BY ELECTROSPRAY-IONIZATION MASS-SPECTROMETRY
Autore:
GAO JM; CHENG XH; CHEN RD; SIGAL GB; BRUCE JE; SCHWARTZ BL; HOFSTADLER SA; ANDERSON GA; SMITH RD; WHITESIDES GM;
Indirizzi:
HARVARD UNIV,DEPT CHEM,12 OXFORD ST CAMBRIDGE MA 02138 HARVARD UNIV,DEPT CHEM CAMBRIDGE MA 02138 PACIFIC NW NATL LAB,ENVIRONM MOL SCI LAB RICHLAND WA 99352
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 10, volume: 39, anno: 1996,
pagine: 1949 - 1955
SICI:
0022-2623(1996)39:10<1949:SDPLFT>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
BIOMOLECULES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
21
Recensione:
Indirizzi per estratti:
Citazione:
J.M. Gao et al., "SCREENING DERIVATIZED PEPTIDE LIBRARIES FOR TIGHT-BINDING INHIBITORS TO CARBONIC-ANHYDRASE-II BY ELECTROSPRAY-IONIZATION MASS-SPECTROMETRY", Journal of medicinal chemistry, 39(10), 1996, pp. 1949-1955

Abstract

This paper describes the use of electrospray ionization-mass spectrometry (ESI-MS) to screen two libraries of soluble compounds to search for tight binding inhibitors for carbonic anhydrase II (EC 4.2.1.1). The two libraries, H2NO2SC6H4C(O)NH-AA(1)-AA(2)-C(O)NHCH2CH2CO2H (1), where AA(1) and AA(2) are L-amino acids (library size: 289 compounds) orD-amino acids (256 compounds), were constructed by attaching tripeptides to the carboxyl group of 4-carboxybenzenesulfonamide. Screening ofboth libraries yielded, as the tightest binding inhibitor, compound 1(AA(1) = AA(2) = L-Leu; binding constant K-b = 1.4 X 10(8) M(-1)). The ability of ESI-MS to estimate simultaneously the relative binding affinities of a protein to soluble ligands in a library, if general, should be useful in drug development.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 10/07/20 alle ore 18:07:04