Cytochrome P450-activated prodrugs
PR Ortiz de Montellano - Future medicinal chemistry, 2013 - Taylor & Francis
A prodrug is a compound that has negligible, or lower, activity against a specified
pharmacological target than one of its major metabolites. Prodrugs can be used to improve …
pharmacological target than one of its major metabolites. Prodrugs can be used to improve …
[BOOK][B] Chemical reagents for protein modification
RL Lundblad - 2004 - taylorfrancis.com
Revised and updated, Chemical Reagents for Protein Modification, Third Edition is an
encyclopedic work describing the many approaches to the site-specific modification of …
encyclopedic work describing the many approaches to the site-specific modification of …
Antiplatelet drug interactions
Mackenzie IS, Coughtrie MWH, MacDonald TM, Wei L.(Medicines Monitoring Unit (MEMO);
and Centre for Oncology & Molecular Medicine, Division of Medical Sciences, University of …
and Centre for Oncology & Molecular Medicine, Division of Medical Sciences, University of …
Cytochromes P450 catalyze both steps of the major pathway of clopidogrel bioactivation, whereas paraoxonase catalyzes the formation of a minor thiol metabolite …
PM Dansette, J Rosi, G Bertho… - Chemical research in …, 2012 - ACS Publications
The mechanism generally admitted for the bioactivation of the antithrombotic prodrug,
clopidogrel, is its two-step enzymatic conversion into a biologically active thiol metabolite …
clopidogrel, is its two-step enzymatic conversion into a biologically active thiol metabolite …
Clarifying the importance of CYP2C19 and PON1 in the mechanism of clopidogrel bioactivation and in vivo antiplatelet response
Aims It is thought that clopidogrel bioactivation and antiplatelet response are related to
cytochrome P450 2C19 (CYP2C19). However, a recent study challenged this notion by …
cytochrome P450 2C19 (CYP2C19). However, a recent study challenged this notion by …
Biotransformations leading to toxic metabolites: chemical aspect
AC Macherey, PM Dansette - The practice of medicinal chemistry, 2008 - Elsevier
Publisher Summary As drugs are usually foreign chemicals, history of concern for the
biotransformations of drugs leading to toxic metabolites formation is intrinsically linked to the …
biotransformations of drugs leading to toxic metabolites formation is intrinsically linked to the …
Spectroscopic and molecular docking studies on N, N-di-tert-butoxycarbonyl (Boc)-2-amino pyridine: A potential bioactive agent for lung cancer treatment
Potential energy surface scan was performed and the most stable molecular structure of the
N, N-di-tert-butoxycarbonyl (Boc)-2-amino pyridine (DBAP) molecule was predicted. The …
N, N-di-tert-butoxycarbonyl (Boc)-2-amino pyridine (DBAP) molecule was predicted. The …
The redox chemistry of sulfenic acids
AJ McGrath, GE Garrett, L Valgimigli… - Journal of the American …, 2010 - ACS Publications
A persistent triptycenyl sulfenic acid is used as a model for cysteine-derived and other
biologically relevant sulfenic acids in experiments which define their redox chemistry. EPR …
biologically relevant sulfenic acids in experiments which define their redox chemistry. EPR …
Overcoming clopidogrel resistance: discovery of vicagrel as a highly potent and orally bioavailable antiplatelet agent
J Shan, B Zhang, Y Zhu, B Jiao, W Zheng… - Journal of medicinal …, 2012 - ACS Publications
A series of optically active 2-hydroxytetrahydrothienopyridine derivatives were designed and
synthesized as prodrugs of clopidogrel thiolactone in order to overcome clopidogrel …
synthesized as prodrugs of clopidogrel thiolactone in order to overcome clopidogrel …
Sulfenic acids as reactive intermediates in xenobiotic metabolism
D Mansuy, PM Dansette - Archives of biochemistry and biophysics, 2011 - Elsevier
Sulfenic acid reactive intermediates are formed during the oxidation of cysteine residues of
proteins and play key roles in enzyme catalysis, redox homeostasis and regulation of cell …
proteins and play key roles in enzyme catalysis, redox homeostasis and regulation of cell …