Metoclopramide : A Template for Drug Discovery 来自 Semantic Scholar 喜欢 0 阅读量: 16 作者: G Sanger 摘要: Metoclopramide was described in 1964 as an anti-emetic drug and stimulant of gastrointestinal motility. Dopamine D2 receptor antagonism explained the anti-emetic activity and was suggested ...
However, established methods for fragment detection do not address the central question in fragment-based ligand discovery: how can a primary ligand be optimally extended by a secondary fragment? Dynamic screening methods solve this issue by using a protein target as a template for ligand assembly,...
Here, we review strategies for the use of advanced biochemistry and NMR techniques with GPCRs, survey projects in which crystal or cryo-EM structures have been complemented with NMR investigations and discuss the impact of this integrative approach on GPCR biology and drug discovery. This is a ...
Structure-based virtual screening is a key tool in early drug discovery, with growing interest in the screening of multi-billion chemical compound libraries. However, the success of virtual screening crucially depends on the accuracy of the binding pose and binding affinity predicted by computational ...
For example, the assay could be useful to uncover tumor-specific activity in the context of genome engineering as well as for the discovery of cell-type-specific oncogenes.Abbreviations BSA: bovine serum albumin DHFR: dihydrofolate reductase DMEM: Dulbecco's modified Eagle's medium gDNA: ...
1. Introduction New drugs with better efficacy and reduced toxicity are always in high demand, however the process of drug discovery and development is costly and time consuming and presents a number of challenges. The pitfalls of target validation and hit identification aside, a high failure rate...
Introduction Drug discovery is a complex process that is focused on the optimization of the molecular interactions between a drug molecule and a biomolecular target. The contacted drugs or, more generally, ligands (in Latin 'ligare' means 'tie') and macromolecules initiate the signals that control...
Currently, infectious diseases are emerging at a global level and a rate never seen before, representing a challenge for the 21st century regarding to the discovery and development of new formulations (31,33). The WHO brings cholera, Ebola virus, influenza, meningitis, COVID-19, poliomyelitis, ...
ChemInform Abstract: Fumonisin, a Template for Methodology Development and Drug Discoveryorganic chemistry, reviewother bioactive productspharmacology, medicinal chemistry, vaccines, serumsReview: 60 refs.doi:10.1002/chin.201144233FrankDep.E.Dep.McDonald...
drug discoverynatural products synthesisstereoselective synthesisstereospecific rearrangementThe chemistry and biology of the fumonisin family of natural products has inspired an integrated research program featuring methods development for stereoselective synthesis of homoallylic alcohols, accompanied by applications ...