Matches in SemOpenAlex for { <https://semopenalex.org/work/W1986572036> ?p ?o ?g. }
Showing items 1 to 73 of
73
with 100 items per page.
- W1986572036 endingPage "117a" @default.
- W1986572036 startingPage "117a" @default.
- W1986572036 abstract "Calmodulin (CaM) is a Ca2+-sensing protein essential to eukaryotic signal transduction pathways. It has two homologous domains (N and C), each binding two Ca2+ ions. The anti-psychotic drug trifluoperazine (TFP; Stelazine) is a CaM antagonist known to bind hydrophobic clefts of CaM that are exposed upon Ca2+ binding. Equilibrium Ca2+ titrations monitored by changes in steady-state fluorescence of intrinsic Phe and Tyr residues were used to evaluate the effect of TFP on the Ca2+ affinity of full length CaM (CaM1–148), N-domain (CaM1–80) and C-domain (CaM76–148) over a range of TFP:CaM ratios. Low levels of TFP (1:1, 2:1 ratios) decreased the Ca2+ affinity of CaM. TFP had the greatest effect on Ca2+ binding to sites III and IV, in the C-domain of CaM1–148, but affected both domains. At an 8:1 ratio of TFP:CaM, the effect reversed and the Ca2+ affinity of CaM increased. 1H-15N-HSQC NMR showed that resonances assigned to apo and Ca2+-saturated C-domain were the most perturbed during TFP titration, while a smaller subset of N-domain resonances were affected. The stoichiometry of TFP binding to apo-CaM1–148 was determined to be 2:1, and 4:1 for (Ca2+)4-CaM. Crystallographic structures of TFP bound to (Ca2+)4-CaM1–148 indicate two possible orientations of TFP when bound in 1:1 vs 2:1 and 4:1 TFP:CaM ratios. A new structure of a (Ca2+)2-CaM76–148 -TFP complex showed the trifluoromethyl group of TFP in both positions seen previously; distinct conformation of Met 144 correlated with orientation of TFP. NMR of apo-CaM76–148 will be used to determine whether apo CaM-TFP complex adopts the semi-open conformation of apo CaM bound to a myosin peptide." @default.
- W1986572036 created "2016-06-24" @default.
- W1986572036 creator A5032108955 @default.
- W1986572036 creator A5075658499 @default.
- W1986572036 date "2009-02-01" @default.
- W1986572036 modified "2023-09-28" @default.
- W1986572036 title "Interactions of the Anti-Psychotic Drug Trifluoperazine with Calmodulin" @default.
- W1986572036 doi "https://doi.org/10.1016/j.bpj.2008.12.514" @default.
- W1986572036 hasPublicationYear "2009" @default.
- W1986572036 type Work @default.
- W1986572036 sameAs 1986572036 @default.
- W1986572036 citedByCount "0" @default.
- W1986572036 crossrefType "journal-article" @default.
- W1986572036 hasAuthorship W1986572036A5032108955 @default.
- W1986572036 hasAuthorship W1986572036A5075658499 @default.
- W1986572036 hasBestOaLocation W19865720361 @default.
- W1986572036 hasConcept C107824862 @default.
- W1986572036 hasConcept C120009192 @default.
- W1986572036 hasConcept C12554922 @default.
- W1986572036 hasConcept C139719470 @default.
- W1986572036 hasConcept C162324750 @default.
- W1986572036 hasConcept C166342909 @default.
- W1986572036 hasConcept C170493617 @default.
- W1986572036 hasConcept C179104552 @default.
- W1986572036 hasConcept C181199279 @default.
- W1986572036 hasConcept C184866935 @default.
- W1986572036 hasConcept C185592680 @default.
- W1986572036 hasConcept C204983608 @default.
- W1986572036 hasConcept C2775891158 @default.
- W1986572036 hasConcept C29688787 @default.
- W1986572036 hasConcept C55493867 @default.
- W1986572036 hasConcept C71240020 @default.
- W1986572036 hasConcept C8010536 @default.
- W1986572036 hasConcept C86803240 @default.
- W1986572036 hasConceptScore W1986572036C107824862 @default.
- W1986572036 hasConceptScore W1986572036C120009192 @default.
- W1986572036 hasConceptScore W1986572036C12554922 @default.
- W1986572036 hasConceptScore W1986572036C139719470 @default.
- W1986572036 hasConceptScore W1986572036C162324750 @default.
- W1986572036 hasConceptScore W1986572036C166342909 @default.
- W1986572036 hasConceptScore W1986572036C170493617 @default.
- W1986572036 hasConceptScore W1986572036C179104552 @default.
- W1986572036 hasConceptScore W1986572036C181199279 @default.
- W1986572036 hasConceptScore W1986572036C184866935 @default.
- W1986572036 hasConceptScore W1986572036C185592680 @default.
- W1986572036 hasConceptScore W1986572036C204983608 @default.
- W1986572036 hasConceptScore W1986572036C2775891158 @default.
- W1986572036 hasConceptScore W1986572036C29688787 @default.
- W1986572036 hasConceptScore W1986572036C55493867 @default.
- W1986572036 hasConceptScore W1986572036C71240020 @default.
- W1986572036 hasConceptScore W1986572036C8010536 @default.
- W1986572036 hasConceptScore W1986572036C86803240 @default.
- W1986572036 hasIssue "3" @default.
- W1986572036 hasLocation W19865720361 @default.
- W1986572036 hasOpenAccess W1986572036 @default.
- W1986572036 hasPrimaryLocation W19865720361 @default.
- W1986572036 hasRelatedWork W1507922729 @default.
- W1986572036 hasRelatedWork W1965607587 @default.
- W1986572036 hasRelatedWork W1999108200 @default.
- W1986572036 hasRelatedWork W2006122354 @default.
- W1986572036 hasRelatedWork W2010105235 @default.
- W1986572036 hasRelatedWork W2034512339 @default.
- W1986572036 hasRelatedWork W2060848457 @default.
- W1986572036 hasRelatedWork W2100807528 @default.
- W1986572036 hasRelatedWork W2137662714 @default.
- W1986572036 hasRelatedWork W1906689289 @default.
- W1986572036 hasVolume "96" @default.
- W1986572036 isParatext "false" @default.
- W1986572036 isRetracted "false" @default.
- W1986572036 magId "1986572036" @default.
- W1986572036 workType "article" @default.