Monthly Archives: March 2013

How Are Fragments Optimized? A Retrospective Analysis of 145 Fragment Optimizations JMC 2013

Posted on March 27, 2013 by admetchemist

György G. Ferenczy and György M. Keserű,  J. Med. Chem. Article ASAP

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“Detoxication” differs from “Detoxification”

Posted on March 21, 2013 by admetchemist

According to Wikipedia Two common patterns associated with Detoxication: A drug with potent pharmacological activity is converted to a major metabolite with markedly reduced or no pharmacological activity (e.g., Pentobarbital and Hydroxypentobarbital) A drug is converted to a metabolite with roughly equivalent or slightly … Continue reading →

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The role of biotransformation enzymes in the development of renal injury and urothelial cancer caused by aristolochic acid: urgent questions and difficult answers. 2009

Posted on March 20, 2013 by admetchemist

Stiborova M., Frei E., Arlt V.M., Schmeiser H.H. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):5-11. Enzymes may be involved in the bioactivation of AA include NAD(P)H:quinone oxidoreductase (NQO1), followed by cytochrome P450 (CYP) 1A1/2 in hepatic microsomes, and NADPH:CYP reductase … Continue reading →

Posted in 1A1, 1A2, Aristolochic Acid, Bioactivation, Biotransformation, Carcinogens, Cyclooxygenase (COX), NADPH P450 Reductase (NPR), NADPH Quninone Oxidoreductase | Tagged , , , | 3 Comments

Aristolochic Acid Nephropathy: Harbinger of a Global Iatrogenic Disease by Arthur P. Grollman 2013

Posted on March 19, 2013 by admetchemist

Grollman, A. P., Environ Mol Mutagen. 2013 Jan; 54(1):1-7 Aristolochic acids are carcinogenic, mutagenic, and nephrotoxic compounds that cause Balkan endemic nephropathy and “Chinese herbs nephropathy”.

Posted in Aristolochic Acid, Carcinogens, Disease, DNA Adducts, Nephropathy, Toxicity | Tagged , , , , , , | Leave a comment

Effect of Solvents on the Time-Dependent Inhibition of CYP3A4 and the Biotransformation of AZD3839 in Human Liver Microsomes and Hepatocytes, AstraZeneca DMD 2013

Posted on March 13, 2013 by admetchemist

Aasa, J. et al. Drug Metab. Dispos. 2013 Jan;41(1):159-169. Given the fact that M23 was observed in hepatocyte incubations, but not in microsomal incubations. AZD3839 might be a substrate for aldehyde oxidase and the oxidation very likely occurred on pyrimidine ring.    

Posted in Drug Drug Interaction (DDI), Drug Metabolism, Solvent Effects, Time-dependent Inhibition (TDI) | Tagged , , | Leave a comment