Murray CW, Rees DC. The rise of fragment-based drug discovery. Nat Chem 2009; 1(3): 187-92.Murray, C.W., Rees, D.C. The rise of fragment-based drug discovery. Nat. Chem. 2009, 1, 187-192.Murray, C. W.; Rees, D. C. The Rise of Fragment-Based Drug Discovery. Nat. Chem...
Fragment-Based Drug Discovery (FBDD) is here to stay. Validated as a technology with the delivery of Zelboraf (Vemurafenib) for the treatment of mutant B-Raf(V600E) melanoma, it has become embedded within the pharmaceutical and biotechnology industries. FBDD has delivered clinical development ...
Fragment-based lead discovery grows up: with multiple drug candidates in the clinic that originated from fragment-based lead discovery, the approach of starting small has become bigMonya Baker
The elucidation of disease mechanisms has been the key to innovative treatments. Thanks to the rise of genomics and proteomics, numerous clinically meaningful targets have been found in human disorders. However, as traditional medicinal chemistry concentrates on druggable targets, increasing disease-related...
Thus, for any given fragment of Cobra code, a Cobra programmer can easily distinguish the elements involved in the fragment or snippet. For example, in the following Cobra statement e = Element(alphabet[_random.next(alphabet.length)])
Rare subpopulations of dysfunctional CD8 T cells function as precursor or progenitor cells that give rise to terminally exhausted cells [2]. We examined a set of genes linked to precursors of exhausted T (TPEX) cells (TCF7, CCR7, SELL, IL7R, TNFRSF4, IL6R, IGFL2) [43, 52] (...
In the latter case, formation of neovessels is necessary to sustain newly formed granulation tissues, in such a way that the ECs divide with a turnover rate of about 5 days, giving rise to a new microvascular network. During the menstrual cycle, however, angiogenesis occurs in corpora lutea...
The rise of deep learning in drug discovery. Drug Discov. Today. 23, 1241–1250 (2018). Article PubMed Google Scholar Fleming, N. How artificial intelligence is changing drug discovery. Nature 557, S55–S57 (2018). Article CAS PubMed Google Scholar Macdonald, S. J., Fray, M. J. ...
Molecular docking is a computational technique that predicts the binding affinity of ligands to receptor proteins. Although it has potential uses in nutraceutical research, it has developed into a formidable tool for drug development. Bioactive substance
Chromogranin A (CHGA/CgA) is a major protein of the secretory granules of chromaffin cells. CHGA also gives rise to cardiovascular/metabolism regulatory peptides, such as catestatin (CST) [55]. It has been established that CST can be involve in a large range of processes, such as ...