WS1358A1, a novel inhibitor of renal dehydropeptidase (DHP), augmented the urinary recovery of a carbapenem antibiotic imipenem and improved its protective effect in experimental infections when simultaneously administered to mice with the antibiotic. WS1358A1 was a competitive DHP inhibitor with a Ki value of 1.6 x 10(-7) M.

Adenylyl cyclase (AC) is a critical family of enzymes which modulates the dynamic cellular level of cAMP, cyclic adenosine monophosphate. The study of cAMP showed that it is indispensable for the signal transduction cascades during many physiological processes, such as immune responses and metabolism which highly relate to cancers. Previous studies of AC inhibitors have been limited due to a la...

Factor inhibiting hypoxia-inducible factor (FIH) is a JmjC domain 2-oxogluarate and Fe(II)-dependent oxygenase that catalyzes hydroxylation of specific asparagines in the C-terminal transcriptional activation alpha (HIF-?) isoforms. This modification suppresses activity HIF by reducing its interaction with coactivators p300/CBP. By contrast inhibition prolyl hydroxylases (PHDs), inhibitors FIH,...

1,3-dialkyl 3-phenylpyrrolidine-2, 5-diones were modified to produce potential steroid sulphatase inhibitors. these modifications were aimed at producing compounds, which could be expected to bind reasonably well to the active site of the steroid sulphatase enzyme but could not be hydrolyzed readily by the enzyme due to the covalent s-c bond present. in this regard the sulphinic acid derivative...

Worldwide, only two types of antiviral inhibitors (M2 ion channel protein inhibitor and Neuraminidase inhibitors) are approved to treat the influenza viral infection. But mutation amino acid sequence in membrane proteins creates resistance existing drugs or inhibitors. So corresponding have be reformulated match these antigenic variations. Fluorination on carbon–based molecule significantly enr...

combination therapy with clomiphene citrate plus gonadotropin (clomiphene citrate plus hmg) in induction ovulation reduce the gonadotropins dose but antiestrogenic effect of c.c. can decrease pregnancy rate. in a randomized clinical trial we compared 3 treatment protocol for induction ovulation and intra uterine insemination (i/o plus iui) in women with infertility history more than one year, n...