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 ...
The success of fragment-based drug design (FBDD) hinges upon the optimization of low molecular weight compounds (MW<300) with weak binding affinities to lead compounds with high affinity and selectivity. Usually, structural information from fragment-protein complexes is used to develop ideas about ...
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 rise of antibiotic-resistant bacteria represents a silent pandemic and is eroding the safety of these basic medical interventions and is an increasing cause of mortality globally1,3. Antibiotic resistance has disproportionately accumulated among specific Gram-negative pathogens. To better align global...
Understanding the mechanistic effects of novel immunotherapy agents is critical to improving their successful clinical translation. These effects need to be studied in preclinical models that maintain the heterogenous tumor microenvironment (TME) and dys
Although most cells do not remain viable after undergoing such a dramatic alteration, those that do could, in theory, express oncogenic fusion proteins or give rise to dysregulated expression of particular genes that could cause problems Click here to read more...
Independent of the administrative route, AIT usually results in a rapid but transient initial rise of specific IgE levels in serum. Long-term AIT, however, will result in a decline in serum allergen-specific IgE levels, which promotes long-term clinical tolerance (Scadding et al., 2017). In...
3,6 By adopting cutting-edge technologies such as fragment-based drug discovery (FBDD), a method leveraging stochastic screening and structure-based design; computer-aided drug design (CADD), simulating and computationally predicting drug-target interactions to screen, design and optimize lead ...
The resulting complex then undergoes specific bond formation, which gives rise to the inhibited complex. In cases in which bond formation iasreefdfeicsttiinvecltyfirrormevemrseicbhlea,nki–s2mw-ibllaessesdenintiaaclltyivbaetozresroin. TtChaIst the latter use the catalytic machinery of an enzyme...