Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2

P Lafite, S Dijols, D Buisson, AC Macherey… - Bioorganic & medicinal …, 2006 - Elsevier
The active site topology, substrate specificity, and biological roles of the human cytochrome
P450 CYP2J2, which is mainly expressed in the cardiovascular system, are poorly known …

Selective, competitive and mechanism-based inhibitors of human cytochrome P450 2J2

P Lafite, S Dijols, DC Zeldin, PM Dansette… - Archives of biochemistry …, 2007 - Elsevier
Twenty five derivatives of the drugs terfenadine and ebastine have been designed,
synthesized and evaluated as inhibitors of recombinant human CYP2J2. Compound 14 …

Unusual regioselectivity and active site topology of human cytochrome P450 2J2

P Lafite, F André, DC Zeldin, PM Dansette… - Biochemistry, 2007 - ACS Publications
The oxidation of six derivatives of terfenadone by recombinant human CYP2J2 (CYP=
cytochrome P450) was studied by high-performance liquid chromatography coupled to mass …

Inhibition and inactivation of human CYP2J2: implications in cardiac pathophysiology and opportunities in cancer therapy

A Karkhanis, Y Hong, ECY Chan - Biochemical Pharmacology, 2017 - Elsevier
Extrahepatic cytochrome P450 enzymes (CYP450) are pivotal in the metabolism of
endogenous substrates and xenobiotics. CYP2J2 is a major cardiac CYP450 and primarily …

Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors

S Ren, J Zeng, Y Mei, JZH Zhang, SF Yan, J Fei… - Drug Metabolism and …, 2013 - ASPET
Cytochrome P450 (CYP) 2J2 is one of the human CYPs involved in phase I xenobiotics
metabolism. It is mainly expressed in extrahepatic tissues, including intestine and …

Inhibitors of cytochrome P450 (CYP) 1B1

R Dutour, D Poirier - European Journal of Medicinal Chemistry, 2017 - Elsevier
Abstract Human cytochrome P450 1B1 (CYP1B1) is involved in the metabolism of various
drugs. This enzyme catalyzes the hydroxylation of aryl compounds, thus generating more …

LKY-047: first selective inhibitor of cytochrome P450 2J2

NM Phuc, Z Wu, O Yuseok, JH Lee, S Oh… - Drug Metabolism and …, 2017 - ASPET
Highly selective cytochrome P450 CYP2J2 (CYP2J2) inhibitors suitable for reaction
phenotyping are currently not available.(7 S)-(+)-(4-Nitro-phenyl)-acrylic acid, 8, 8-dimethyl …

[HTML][HTML] New perspectives of CYP1B1 inhibitors in the light of molecular studies

R Mikstacka, Z Dutkiewicz - Processes, 2021 - mdpi.com
Human cytochrome P450 1B1 (CYP1B1) is an extrahepatic heme-containing
monooxygenase. CYP1B1 contributes to the oxidative metabolism of xenobiotics, drugs, and …

[HTML][HTML] Molecular determinant of substrate binding and specificity of cytochrome P450 2J2

L Xu, LY Chen - Scientific Reports, 2020 - nature.com
Abstract Cytochrome P450 2J2 (CYP2J2) is responsible for the epoxidation of endogenous
arachidonic acid, and is involved in the metabolism of exogenous drugs. To date, no crystal …

Cytochrome P450s in the development of target-based anticancer drugs

K Purnapatre, SK Khattar, KS Saini - Cancer letters, 2008 - Elsevier
Enzymes of the cytochrome P450 (CYP) superfamily are the major determinants of half-life
and execute pharmacological effects of many therapeutic drugs. In new drug discovery …