Chen, Chao published the artcileUse of Phenoxyaniline Analogues To Generate Biochemical Insights into the Interactio n of Polybrominated Diphenyl Ether with CYP2B Enzymes, Formula: C6H3ClFNO2, the publication is Biochemistry (2018), 57(5), 817-826, database is CAplus and MEDLINE.
Human hepatic cytochromes P 450 (CYP) are integral to xenobiotic metabolism CYP2B6 is a major catalyst of biotransformation of environmental toxicants including polybrominated di-Ph ethers (PBDEs). CYP2B substrates tend to contain halogen atoms, but the biochem. basis for this selectivity and for species specific determinants of metabolism has not been identified. Spectral binding titrations and inhibition studies were performed to investigate interactions of rat CYP2B1, rabbit CYP2B4, and CYP2B6 with a series of phenoxyaniline (POA) congeners that are analogs of PBDEs. For most congeners, there was less than 3-fold difference between the spectral binding constants (KS) and IC50 values. In contrast, large discrepancies between these values were observed for POA and 3-chloro-4-phenoxyaniline. CYP2B1 was the most sensitive enzyme to POA congeners, so the Val-363 residue from that enzyme was introduced into CYP2B4 or CYP2B6. This substitution partially altered the protein-ligand interaction profiles to make them more similar to that of CYP2B1. Addition of cytochrome P 450 oxidoreductase (POR) to titrations of CYP2B6 with POA or 2’4’5’TCPOA decreased the affinity of both ligands for the enzyme. Addition of cytochrome b5 (cyt b5) to a recombinant enzyme system containing POR and CYP2B6 increased the POA IC50 value and decreased the 2’4’5’TCPOA IC50 value. Overall, the inconsistency between KS and IC50 values for POA vs. 2’4’5’TCPOA is largely due to the effects of redox partner binding. These results provide insight into the biochem. basis of di-Ph ether binding to human CYP2B6 and changes in CYP2B6 mediated metabolism dependent on POA congener and redox partner identity.
Biochemistry published new progress about 350-30-1. 350-30-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Nitro Compound,Benzene, name is 3-Chloro-4-fluoronitrobenzene, and the molecular formula is C6H3ClFNO2, Formula: C6H3ClFNO2.
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