Matches in SemOpenAlex for { <https://semopenalex.org/work/W2891752511> ?p ?o ?g. }
Showing items 1 to 69 of
69
with 100 items per page.
- W2891752511 endingPage "S30" @default.
- W2891752511 startingPage "S30" @default.
- W2891752511 abstract "HSA is an important plasma protein responsible for transport of drug molecules. Coumarin derivatives play critical role as anticancer, antidiabetic and antiparkinson agents. In our lab we have synthesized coumarin-based pharmacophore, di(2-picolyl)amine-3(bromoacetyl) coumarin (ligand-L) endowed with anticancer activity. Anticancer agents binding mode of HSA provides valuable pharmacological information and is a structural guidance in synthesizing new drugs with greater efficacy. Thus, binding mechanism of ligand-L with HSA was explored using spectroscopic and molecular docking techniques. UV–Vis spectroscopy demonstrates hyperchromism in the absorbance spectra of HSA on addition of ligand-L suggesting interaction of ligand-L with HSA. Fluorescence spectroscopy indicates quenching in the fluorescence of HSA in the presence of ligand-L confirming the complex formation and this binding follows static mechanism. Steady state fluorescence spectroscopy revealed high binding affinity between ligand-L and HSA with a 1:1 stoichiometry. Thermodynamic parameters obtained by ITC suggest that the interaction between ligand-L and HSA is mainly driven by van der Waals forces and hydrogen bonds, and the negative value of ΔG is an indication of spontaneous binding process. Competitive binding and molecular docking experiments showed that the binding site of ligand-L mainly resides in sub-domain IIA of HSA. CD experiments revealed no significant conformational changes in the secondary structure of HSA on binding of ligand-L. We also found that esterase-like activity of HSA was not affected by ligand-L. In conclusion, this study demonstrates binding mechanism of ligand-L with HSA, and the binding did not induce conformational changes in HSA. This study is likely to provide better understanding of transport and delivery of ligand-L via HSA. Overall, it will provide insights into pharmacokinetic properties of ligand-L and designing new ligand-L based derivatives with greater efficacy." @default.
- W2891752511 created "2018-09-27" @default.
- W2891752511 creator A5006871265 @default.
- W2891752511 date "2018-10-01" @default.
- W2891752511 modified "2023-09-25" @default.
- W2891752511 title "The discovery of innovative medicines with the Right Safety to increase R&D productivity" @default.
- W2891752511 doi "https://doi.org/10.1016/j.toxlet.2018.06.1132" @default.
- W2891752511 hasPublicationYear "2018" @default.
- W2891752511 type Work @default.
- W2891752511 sameAs 2891752511 @default.
- W2891752511 citedByCount "0" @default.
- W2891752511 crossrefType "journal-article" @default.
- W2891752511 hasAuthorship W2891752511A5006871265 @default.
- W2891752511 hasConcept C107824862 @default.
- W2891752511 hasConcept C112887158 @default.
- W2891752511 hasConcept C116569031 @default.
- W2891752511 hasConcept C121332964 @default.
- W2891752511 hasConcept C158711907 @default.
- W2891752511 hasConcept C159110408 @default.
- W2891752511 hasConcept C170493617 @default.
- W2891752511 hasConcept C178790620 @default.
- W2891752511 hasConcept C178910836 @default.
- W2891752511 hasConcept C185592680 @default.
- W2891752511 hasConcept C2778597219 @default.
- W2891752511 hasConcept C32909587 @default.
- W2891752511 hasConcept C41685203 @default.
- W2891752511 hasConcept C55493867 @default.
- W2891752511 hasConcept C62520636 @default.
- W2891752511 hasConcept C71240020 @default.
- W2891752511 hasConcept C71924100 @default.
- W2891752511 hasConcept C91881484 @default.
- W2891752511 hasConceptScore W2891752511C107824862 @default.
- W2891752511 hasConceptScore W2891752511C112887158 @default.
- W2891752511 hasConceptScore W2891752511C116569031 @default.
- W2891752511 hasConceptScore W2891752511C121332964 @default.
- W2891752511 hasConceptScore W2891752511C158711907 @default.
- W2891752511 hasConceptScore W2891752511C159110408 @default.
- W2891752511 hasConceptScore W2891752511C170493617 @default.
- W2891752511 hasConceptScore W2891752511C178790620 @default.
- W2891752511 hasConceptScore W2891752511C178910836 @default.
- W2891752511 hasConceptScore W2891752511C185592680 @default.
- W2891752511 hasConceptScore W2891752511C2778597219 @default.
- W2891752511 hasConceptScore W2891752511C32909587 @default.
- W2891752511 hasConceptScore W2891752511C41685203 @default.
- W2891752511 hasConceptScore W2891752511C55493867 @default.
- W2891752511 hasConceptScore W2891752511C62520636 @default.
- W2891752511 hasConceptScore W2891752511C71240020 @default.
- W2891752511 hasConceptScore W2891752511C71924100 @default.
- W2891752511 hasConceptScore W2891752511C91881484 @default.
- W2891752511 hasLocation W28917525111 @default.
- W2891752511 hasOpenAccess W2891752511 @default.
- W2891752511 hasPrimaryLocation W28917525111 @default.
- W2891752511 hasRelatedWork W1971679563 @default.
- W2891752511 hasRelatedWork W1975644494 @default.
- W2891752511 hasRelatedWork W1981883043 @default.
- W2891752511 hasRelatedWork W2011420991 @default.
- W2891752511 hasRelatedWork W2022128949 @default.
- W2891752511 hasRelatedWork W2035922710 @default.
- W2891752511 hasRelatedWork W2088829158 @default.
- W2891752511 hasRelatedWork W2169871851 @default.
- W2891752511 hasRelatedWork W2744776933 @default.
- W2891752511 hasRelatedWork W4316928435 @default.
- W2891752511 hasVolume "295" @default.
- W2891752511 isParatext "false" @default.
- W2891752511 isRetracted "false" @default.
- W2891752511 magId "2891752511" @default.
- W2891752511 workType "article" @default.