A series of 3-(2-aminocarbonyl-4-phenoxymethylphenyl)propanoic acid analogs were synthesized and evaluated for their EP3 antagonist activity in the presence of additive serum albumin. Several compounds were biologically evaluated for their in vivo efficacy with respect to the PGE(2)-induced uterine contraction in pregnant rats as well as their pharmacokinetics. The discovery process of these potent and selective EP3 antagonists and their structure activity relationship are also presented.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.bmc.2009.11.023 | DOI Listing |
Nucleic Acids Res
January 2025
Department of Physics, 845 W Taylor St, University of Illinois Chicago, Chicago, IL 60607, USA.
Altered DNA dynamics at lesion sites are implicated in how DNA repair proteins sense damage within genomic DNA. Using laser temperature-jump (T-jump) spectroscopy combined with cytosine-analog Förster Resonance Energy Transfer (FRET) probes that sense local DNA conformations, we measured the intrinsic dynamics of DNA containing 3 base-pair mismatches recognized in vitro by Rad4 (yeast ortholog of XPC). Rad4/XPC recognizes diverse lesions from environmental mutagens and initiates nucleotide excision repair.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
Department of Animal Experimentation, Noguchi Memorial Institute for Medical Research, College of Health Sciences, University of Ghana, Accra P.O. Box LG581, Ghana.
Cisplatin is a common and highly effective chemotherapeutic agent whose nephrotoxic side effect is well-characterized. Sodium thiosulfate (STS), an FDA-approved hydrogen sulfide (HS) donor drug, is emerging as a chemoprotective agent against cisplatin-induced nephrotoxicity (CIN). In this study, we investigated the chemoprotective mechanism of STS in a rat model of CIN.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
School of Applied Sciences, College of Health, Science and Society, University of the West of England, Coldharbour Lane, Bristol BS16 1QY, UK.
The active metabolite of vitamin D3, calcitriol (1,25D), is widely recognised for its direct anti-proliferative and pro-differentiation effects. However, 1,25D is calcaemic, which restricts its clinical use for cancer treatment. Non-calcaemic agonists of the vitamin D receptor (VDR) could be better candidates for cancer treatment.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Metabolic Engineering Division, National Institute of Agricultural Sciences, Rural Development Administration, Wanju 55365, Republic of Korea.
The black soldier fly, , is a voracious scavenger of various organic materials; therefore, it could be exploited as a biological system for processing daily food waste. In order to survey novel hydrolytic enzymes, we constructed a fosmid metagenome library using unculturable intestinal microorganisms from . Through functional screening of the library on carboxymethyl cellulose plates, we identified a fosmid clone, the product of which displayed hydrolytic activity.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Institute of Biotechnology, Fujian Academy of Agricultural Sciences, Fuzhou 350003, China.
The lily is a globally popular cut flower, and managing dormancy in lily bulblets is essential for continuous, year-round production. While nitric oxide (NO) has been shown to influence seed dormancy and germination, its role in dormancy release in lilies was previously unconfirmed. In this study, we investigated the effects of NO on dormancy release in lily bulblets using SNP and c-PTIO.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!