Matches in SemOpenAlex for { <https://semopenalex.org/work/W1964754125> ?p ?o ?g. }
Showing items 1 to 78 of
78
with 100 items per page.
- W1964754125 endingPage "16829" @default.
- W1964754125 startingPage "16821" @default.
- W1964754125 abstract "NSC 613863 (R)-(+) and NSC 613862 (S)-(-) (CI980) are two chiral isomers of ethyl 5-amino 2-methyl-1,2-dihydro-3-phenylpyrido[3,4-b]pyrazin-7-yl carbamate which have potent antitubulin activity. The S-isomer is a more potent antimitotic compound than the R-isomer, and the two isomers differ markedly in binding to tubulin [Leynadier, D., Peyrot, V., Sarrazin, M., Briand, C., Andreu, J. M., Rener, G. A., & Temple, C., Jr. (1993) Biochemistry 32, 10675-10682]. To understand the origin of such differences, we studied the interactions of three R- and S-isomer structural analogs which differ in C2 (the chiral carbon), i.e., C179, NSC 337238, and NSC 330770. C179 is a methylated dehydrogenated achiral compound. It bound to tubulin with an apparent affinity Ka of (2.29 +/- 0.17) x 10(4) M-1, inhibited tubulin polymerization in vitro at a half-inhibitory concentration (IC50) of 100 microM, and presented no GTPase activity. The substitution of -CH3 by -H leads to the NSC 337238 compound. It bound to tubulin with a higher affinity [Ka = (2.62 +/- 0.35) x 10(5) M-1] and inhibited tubulin polymerization at a lower concentration (IC50 = 14 microM). It presented no GTPase activity and induced the formation of abnormal polymers at a protein critical concentration (Cr) of 2 mg mL-1. NSC 330770, a demethylated hydrogenated molecule, interacted strongly with tubulin [Ka = (3.30 +/- 0.56) x 10(6) M-1].(ABSTRACT TRUNCATED AT 250 WORDS)" @default.
- W1964754125 created "2016-06-24" @default.
- W1964754125 creator A5003828462 @default.
- W1964754125 creator A5003846685 @default.
- W1964754125 creator A5015918801 @default.
- W1964754125 creator A5023113393 @default.
- W1964754125 creator A5047219507 @default.
- W1964754125 date "1995-12-01" @default.
- W1964754125 modified "2023-09-25" @default.
- W1964754125 title "Differential Effects of Ethyl 5-Amino-2-methyl-1,2-dihydro-3-phenylpyrido[3,4-b]pyrazin-7-yl Carbamate Analogs Modified at Position C2 on Tubulin Polymerization, Binding, and Conformational Changes" @default.
- W1964754125 doi "https://doi.org/10.1021/bi00051a033" @default.
- W1964754125 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/8527458" @default.
- W1964754125 hasPublicationYear "1995" @default.
- W1964754125 type Work @default.
- W1964754125 sameAs 1964754125 @default.
- W1964754125 citedByCount "12" @default.
- W1964754125 countsByYear W19647541252016 @default.
- W1964754125 countsByYear W19647541252017 @default.
- W1964754125 crossrefType "journal-article" @default.
- W1964754125 hasAuthorship W1964754125A5003828462 @default.
- W1964754125 hasAuthorship W1964754125A5003846685 @default.
- W1964754125 hasAuthorship W1964754125A5015918801 @default.
- W1964754125 hasAuthorship W1964754125A5023113393 @default.
- W1964754125 hasAuthorship W1964754125A5047219507 @default.
- W1964754125 hasConcept C178790620 @default.
- W1964754125 hasConcept C185592680 @default.
- W1964754125 hasConcept C202751555 @default.
- W1964754125 hasConcept C20418707 @default.
- W1964754125 hasConcept C2777752497 @default.
- W1964754125 hasConcept C2779303437 @default.
- W1964754125 hasConcept C3019471444 @default.
- W1964754125 hasConcept C44228677 @default.
- W1964754125 hasConcept C45803636 @default.
- W1964754125 hasConcept C515207424 @default.
- W1964754125 hasConcept C521977710 @default.
- W1964754125 hasConcept C55493867 @default.
- W1964754125 hasConcept C71240020 @default.
- W1964754125 hasConcept C84425145 @default.
- W1964754125 hasConcept C86803240 @default.
- W1964754125 hasConcept C95444343 @default.
- W1964754125 hasConceptScore W1964754125C178790620 @default.
- W1964754125 hasConceptScore W1964754125C185592680 @default.
- W1964754125 hasConceptScore W1964754125C202751555 @default.
- W1964754125 hasConceptScore W1964754125C20418707 @default.
- W1964754125 hasConceptScore W1964754125C2777752497 @default.
- W1964754125 hasConceptScore W1964754125C2779303437 @default.
- W1964754125 hasConceptScore W1964754125C3019471444 @default.
- W1964754125 hasConceptScore W1964754125C44228677 @default.
- W1964754125 hasConceptScore W1964754125C45803636 @default.
- W1964754125 hasConceptScore W1964754125C515207424 @default.
- W1964754125 hasConceptScore W1964754125C521977710 @default.
- W1964754125 hasConceptScore W1964754125C55493867 @default.
- W1964754125 hasConceptScore W1964754125C71240020 @default.
- W1964754125 hasConceptScore W1964754125C84425145 @default.
- W1964754125 hasConceptScore W1964754125C86803240 @default.
- W1964754125 hasConceptScore W1964754125C95444343 @default.
- W1964754125 hasIssue "51" @default.
- W1964754125 hasLocation W19647541251 @default.
- W1964754125 hasLocation W19647541252 @default.
- W1964754125 hasOpenAccess W1964754125 @default.
- W1964754125 hasPrimaryLocation W19647541251 @default.
- W1964754125 hasRelatedWork W1593539367 @default.
- W1964754125 hasRelatedWork W1953369462 @default.
- W1964754125 hasRelatedWork W1964754125 @default.
- W1964754125 hasRelatedWork W1994399889 @default.
- W1964754125 hasRelatedWork W2009711715 @default.
- W1964754125 hasRelatedWork W2030004024 @default.
- W1964754125 hasRelatedWork W2052556436 @default.
- W1964754125 hasRelatedWork W2057768106 @default.
- W1964754125 hasRelatedWork W2059052337 @default.
- W1964754125 hasRelatedWork W2166585705 @default.
- W1964754125 hasVolume "34" @default.
- W1964754125 isParatext "false" @default.
- W1964754125 isRetracted "false" @default.
- W1964754125 magId "1964754125" @default.
- W1964754125 workType "article" @default.