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Titolo:
COLORIMETRIC ASSAYS FOR EVALUATION OF THE MODE OF ACTION OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 NONNUCLEOSIDE REVERSE-TRANSCRIPTASE INHIBITORS
Autore:
SHAO X; RYTTING AS; EKSTRAND DHL; VRANG L; KALLANDER CFR; GRONOWITZ JS;
Indirizzi:
UPPSALA UNIV,BMC,RES UNIT REPLICAT ENZYMOL,DEPT MED GENET,BOX 589 S-75123 UPPSALA SWEDEN MEDIVIR S-14144 HUDDINGE SWEDEN CAVIDI TECH S-75183 UPPSALA SWEDEN CHINESE ACAD MED SCI,INST MED BIOTECHNOL,DEPT VIROL BEIJING 100050 PEOPLES R CHINA
Titolo Testata:
Antiviral chemistry & chemotherapy
fascicolo: 2, volume: 9, anno: 1998,
pagine: 167 - 176
SICI:
0956-3202(1998)9:2<167:CAFEOT>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
CARRIER-BOUND TEMPLATE; NONNUCLEOSIDE INHIBITORS; SELECTIVE-INHIBITION; HIV-1 REPLICATION; POTENT INHIBITOR; DERIVATIVES; SERIES; DIPYRIDODIAZEPINONE; PURIFICATION; RESOLUTION;
Keywords:
REVERSE TRANSCRIPTASE; RT ASSAYS; RT INHIBITORS; NONNUCLEOSIDE ANALOGS; CARRIER BOUND TEMPLATE/PRIMERS; HIV/AIDS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
34
Recensione:
Indirizzi per estratti:
Citazione:
X. Shao et al., "COLORIMETRIC ASSAYS FOR EVALUATION OF THE MODE OF ACTION OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 NONNUCLEOSIDE REVERSE-TRANSCRIPTASE INHIBITORS", Antiviral chemistry & chemotherapy, 9(2), 1998, pp. 167-176

Abstract

Four non-nucleoside reverse transcriptase (RT) inhibitors, 9-CI-TIBO rahydro-9-chloro-5-methyl-6-(3-methyl-2-butenyl)im 5,1-jk)(1,4)-benzodiazepin-2(1H)-thione)], nevi rapine 11-cyclopropyl-4-methyl-dipyrido[2,3-b:2',3'-e]-[1 ,4]diazepin-6-one), MSA-300 nyl)cyclopropyl]-N'-(5-chloropyrid-2-yl)-thiourea) and delavirdine ethanesulphonamido-1H-indol-2-yl-carbonyl)-4-[3-(1 -methylethylamino)pyridinyl] piperazine) were analysed for the mode of action of their inhibition of human immuno-deficiency virus type 1 (HIV-1) RT in three different assays utilizing a 96-well microtitre plate format, with solid-phase conjugated poly(ra) as template. These were: (i) direct RT assay for determination of IC50values of RT inhibitors; (ii) RT template/primer binding inhibition (BIG) assay, for measuring the effect of various substances on the RT activity binding to template/primer; (iii) RT protein ELISA, for measuring RT protein binding to template/primer with a monoclonal antibody reactive against a peptide in the RNase H region. MSA-300 and delavirdine gave the lowest IC50 values, ranging from 0.17 mu M to 0.24 mu M for MSA-300 and from 0.12 mu M to 0.38 mu M for delavirdine, whereas higher IC50 values of approximately 20 mu M were obtained for 9-CI-TIBO at all primer concentrations. None of the non-nucleoside substances hadinhibiting effects on the binding of template, primer, or template/primer to RT protein. Their inhibition of RT activity was not due to prevention of RT binding to template/primer. TIBO, nevirapine and delavirdine bound to RT reversibly and they bound more tightly to RT template/primer ternary than to RT template binary complex. MSA-300 showed a comparatively high affinity for the enzyme. The utility of the three assays in relation to screening and analysis of RT inhibitory substancesis discussed.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/09/20 alle ore 12:15:10