Organophosphorus chemicals: potent inhibitors of the human metabolism of steroid hormones and xenobiotics.

Drug Metab Rev

Department of Environmental and Molecular Toxicology, North Carolina State University, Raleigh, North 27695, USA.

Published: June 2006

Although it has been known for some time that organophosphate chemicals containing the P = S moiety are irreversible inhibitors of cytochrome P450, this knowledge has not been generally applied to the human metabolism of xenobiotics. Recent studies have demonstrated that organophosphate insecticides containing this moiety are potent inhibitors of the metabolism of both xenobiotics and endogenous substrates by human liver microsomes and by specific human cytochrome P450 isoforms.

Download full-text PDF

Source
http://dx.doi.org/10.1080/03602530600569984DOI Listing

Publication Analysis

Top Keywords

potent inhibitors
8
human metabolism
8
cytochrome p450
8
metabolism xenobiotics
8
organophosphorus chemicals
4
chemicals potent
4
human
4
inhibitors human
4
metabolism steroid
4
steroid hormones
4

Similar Publications

The COVID-19 pandemic began in March 2020 and has affected many countries and infected over a million people. It has had a serious impact on people's physical and mental health, daily life and the global economy. Today, many drugs show limited efficacy in the treatment of COVID-19 and studies to develop effective drugs continue.

View Article and Find Full Text PDF

Designing an anticancer Pd(II) complex as poly(ADP-ribose) polymerase 1 inhibitor.

Int J Biol Macromol

January 2025

School of Biological and Food Engineering, Guangxi Science & Technology Normal University, Laibin, Guangxi 546199, China. Electronic address:

Targeting DNA repair mechanisms, particularly PARP-1 inhibition, has emerged as a promising strategy for developing anticancer therapies. we designed and synthesized two 2-thiazolecarboxaldehyde thiosemicarbazone palladium(II) complexes (C1 and C2), and evaluated their anti-cancer activities. These Pd(II) complexes exhibited potent PARP-1 enzyme inhibition and demonstrated considerable antiproliferative activity against various cancer cell lines.

View Article and Find Full Text PDF

Tyrosinase is a rate-limiting enzyme for melanogenesis and abnormal melanin production can be controlled by utilizing tyrosinase inhibitory substances. To develop potent and safe inhibitors of tyrosinase, complex tannins a narrowly distributed plant polyphenols were prepared from the fruit peel of Euryale ferox (EPTs) and then structurally characterized, as well as investigated for their inhibitory effects and the involved mechanisms against tyrosinase activity and melanogenesis. The structures of EPTs were established to consist of 63.

View Article and Find Full Text PDF

Synthesis and biological assessment of BUB1B inhibitors for the treatment of clear cell renal cell carcinoma.

Eur J Med Chem

January 2025

Science for Life Laboratory, KTH - Royal Institute of Technology, Stockholm, SE, 17165, Sweden; Centre for Host-Microbiome Interactions, Faculty of Dentistry, Oral & Craniofacial Sciences, King's College London, London, SE1 9RT, UK. Electronic address:

Clear cell renal cell carcinoma (ccRCC) presents substantial therapeutic challenges due to its molecular heterogeneity, limited response to conventional therapies, and widespread drug resistance. Recent advancements in molecular research have identified novel targets, such as BUB1B, which has been identified through global transcriptomic profiling and gene co-expression network analysis as critical in ccRCC progression. In this study, we synthesized 40 novel derivatives of TG-101209 to modulate BUB1B expression and activity, leading to the induction of apoptosis in Caki-1 cells.

View Article and Find Full Text PDF

3-Fluoroneuraminosyl fluorides are invaluable probes for studying the catalytic mechanism of sialidases (neuraminidases), and as sialidase inhibitors. Significantly, when a C-3 equatorial fluorine is installed on a C-4 functionalised N-acylneuraminic acid (Neu)-based template, the compounds are potent and selective inhibitors of both influenza and parainfluenza sialidases, and of virus replication. Typically, the reported syntheses of 3-fluoroneuraminosyl fluorides involve either an enzymatic or a chemical synthesis that have uncontrolled stereoselectivity in the introduction of fluorine at C-3 of Neu and consequently yield a mixture of C-3 ax and C-3 eq fluoro derivatives.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!