In summary, WDR binders from a previous hit-discovery campaign for EED27 have been screened and optimized using NMR, computer-aided drug design, biophysics and structure–activity relationship approaches. This resulted in the discovery of a scaffold that occupies the DCAF1 WDR donut-hole pocket. ...
Using high throughput, high-content imaging, a proprietary library was screened against intracellular Trypanosoma cruzi amastigotes to identify compounds with novel activity against the parasite. Five inhibitors were discovered, which did not clear all o
Taken together, our results offer new insights into structure-activity relationships of antiplasmodial HDAC inhibitors and highlight the potential of 6i as a promising starting point for the development of novel antimalarial drug leads. 4. Methods 4.1. Chemistry Chemicals were obtained from abcr ...
Owing to its function in controlling the cellular homeostasis of cancer-related proteins such as B-Raf (protein kinase encoded by the BRAF gene), CDK4, and v-src (tyrosine kinase encoded by the v-Src gene), Hsp90 has emerged as a promising target for anti-cancer drug development (Garg ...
Formulation approaches to improving the delivery of an antiviral drug with activity against seasonal fluBioavailabilityco-solventscyclodextrinssolubilityUssing chambersThe main objective of the present study was to develop formulations of noscapine hydrochloride hydra...
Highlighting this risk scenario is theindictmentof two Iranian nationals who were charged for conducting a cyber-enabled campaign to disrupt the 2020 U.S. Presidential election. This operation involved intimidating American voters, undermining voter confidence, and spreading discord. ...
Drug Carrier Design, Drug Delivery Platform Technology, Drug Discovery Chemistry, drug repurposing, Endocrine Diseases, Endoplasmic reticulum, Enzyme Induction, Enzymes and isoenzymes, Epigenetics and Cardiovascular Risks, Epigenetics and Environmental Factors, Evolution of Biology Through Culture, Fatty acids...
Therefore, the inhibition of LPS activated macrophages to release cytokines and mediators is always used to develop and evaluate new anti-inflammatory agents. In recent years, drug development has often relied on the use of natural and synthetic drugs for the prevention or treatment of many ...
Whether feeblin itself will represent the starting point of a future therapeutic or not, it provides a mechanistic proof-of-principle for the development of a potential anti-inflammatory drug for SLE and related diseases. Methods Ethical statement Human primary PBMCs were isolated from the blood of...
The content is solely the responsibility of the authors and does not necessarily represent the official views of the NIH or the Food and Drug Administration (FDA). D.S.B. also acknowledges support from the John D. and Catherine T. MacArthur Foundation and from the Alfred P. Sloan Foundation...