| 词条 | Conformation–activity relationship |
| 释义 |
The conformation–activity relationship is the relationship between the biological activity and the chemical structure or conformational changes of a biomolecule. This terminology emphasizes the importance of dynamic conformational changes for the biological function, rather than the importance of static three-dimensional structure used in the analysis of structure activity relationships.[1] The conformational changes usually take place during intermolecular association, such as protein–protein interaction or protein–ligand binding. A binding partner changes the conformation of a biomolecule (e.g. a protein) to enable or disable its biochemical activity. Methods for analysis of conformation activity relationship vary from in silico[2] or using experimental methods such as X-ray crystallography and NMR where the conformation before and after activity can be compared statically or using dynamic methods such as multi-parametric surface plasmon resonance, dual polarisation interferometry or circular dichroism where the kinetics as well as degree of conformational change can be quantified. Experimental techniquesStaticStatic experimental techniques include X-ray crystallography and NMR. DynamicDynamic experimental techniques include multi-parametric surface plasmon resonance, Dual polarization interferometry, and circular dichroism. References1. ^{{cite journal|last1=Taylor|first1=RE|last2=Chen|first2=Y|last3=Beatty|first3=A|last4=Myles|first4=DC|last5=Zhou|first5=Y|title=Conformation-activity relationships in polyketide natural products: a new perspective on the rational design of epothilone analogues|journal=Journal of the American Chemical Society|volume=125|issue=1|pages=26–7|year=2003|pmid=12515494|doi=10.1021/ja028196l}} {{DEFAULTSORT:Conformation Activity Relationship}}2. ^{{cite journal|last1=Carotenuto|first1=Alfonso|last2=D'ursi|first2=Anna Maria|last3=Mulinacci|first3=Barbara|last4=Paolini|first4=Ilaria|last5=Lolli|first5=Francesco|last6=Papini|first6=Anna Maria|last7=Novellino|first7=Ettore|last8=Rovero|first8=Paolo|title=Conformation−Activity Relationship of Designed Glycopeptides as Synthetic Probes for the Detection of Autoantibodies, Biomarkers of Multiple Sclerosis|journal=Journal of Medicinal Chemistry|volume=49|pages=5072–9|year=2006|doi=10.1021/jm060117j|issue=17|pmid=16913697}} 1 : Medicinal chemistry |
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