ABT-888 inhibitor The discoveries from this work could be foundational for the creation of novel anticancer agents, focusing on VEGFR-2 inhibitors that are capable of targeting multiple molecules.The mycotoxin gliotoxin, produced by Aspergillus fumigatus, manifests a variety of pharmacological effects,...
The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders. The compounds have general formula (Ia), (Ib), (Ic) or (Id). Examples of compounds of the invention are 1-[5-(3’-Chloro-2-fluoro-...
PDE10A inhibitors increase cyclic nucleotides in striatal neurons, thereby mimicking the effects of dopamine receptor D2 antagonists and D1 agonists. We evaluated the PDE10A inhibitor MK-8189 for treating schizophrenia.METHODSRandomized, double-blind, placebo and active-controlled, phase 2a, multicenter...
Inhibitors of phosphodiesterase as cancer therapeutics TingPeng, ...JianyouShi, inEuropean Journal of Medicinal Chemistry, 2018 2.6PDE6 PDE6, also known as thephotoreceptorphosphodiesterases, contains three genes, PDE6A (chromosomes 5q31.2–34),PDE6B(chromosomes 4p16.3), and PDE6C (chromosomes 10q...
A1R, A2AR ligands and PDE10A inhibitors with Ki and IC50 values less than or equal to 1 µM revealed that the most frequently occurring common heterocycles among the actives against the three target classes were pyridine, pyrimidine, piperazine, and 1H-pyrazole (Additional file 1: Figure S1)...
As inhibitors, recombinant FAT10 ((+) = 1.67 µg, (++) = 5 µg) or FAT10-AV ((+) = 1.5 µg, (++) = 4.5 µg) were added. FAT10 storage buffer served as a control. Shown is the mean ± S.E. (error bars) of five experiments (n = 5). Significance was calculated...
Using SQL (script provided in Additional file1), human A1R (2860), A2AR (3566) ligands and PDE10A inhibitors (843) were extracted from the ChEMBL 20 database with Kiand IC50values less than or equal to 1 μM respectively, and confidence scores of 8 or 9 [30]. Following extraction, ...
Additional data is provided in the following Examples. Such a result is indicative of the intrinsic activity of the compounds in use as inhibitors of the PDE10 enzyme. In general, one of ordinary skill in the art would appreciate that a substance is considered to effectively inhibit PDE10 ...
The present invention provides compounds according to formula (I) below that are PDE1 enzyme inhibitors and their use as medicaments, in particular for the treatment of neurodegenerative disorders and psychiatric disorders. The present invention also provides pharmaceutical compositions comprising compounds ...
PDE10A has limited but high expression in the brain and testes. The high expression in the brain and, in particular, the neurons of the striatum, unique to PDE10, suggests that inhibitors thereto may be well suited from treating neurological and psychiatric disorders and conditions....