Use my Search Websuite to scan PubMed, PMCentral, Journal Hosts and Journal Archives, FullText. Kick-your-searchterm to multiple Engines kick-your-query now !>

A dictionary by aggregated review articles of nephrology, medicine and the life sciences Your one-stop-run pathway from word to the immediate pdf of peer-reviewed on-topic knowledge.

10.1038/nrd.2016.211 http://scihub22266oqcxt.onion/10.1038/nrd.2016.211 C5684876!5684876 !27885283     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=27885283 &cmd=llinks): Failed to open stream: HTTP request failed! HTTP/1.1 429 Too Many Requests in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 215 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Warning: imagejpeg(C:\Inetpub\vhosts\kidney.de\httpdocs\phplern\27885283 .jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117       Nat+Rev+Drug+Discov 2017 ; 16 (2 ): 101-114 Nephropedia Template TP {{tp|p=27885283 |t=2017. Induced protein degradation: an emerging drug discovery paradigm |pdf=|usr=}}{{27885283 }} gab.com Text Induced protein degradation: an emerging drug discovery paradigm JO: Nat Rev Drug Discov http://www.kidney.de/pget.php?&tw=1&pmid=27885283 #FOAvip Small-molecule drug discovery has traditionally focused on occupancy of a binding site that directly affects protein function, and this approach typically precludes targeting proteins that lack such amenable sites. Furthermore, high systemic drug exposures may be needed to maintain sufficient target inhibition in vivo, increasing the risk of undesirable off-target effects. Induced protein degradation is an alternative approach that is event-driven: upon drug binding, the target protein is tagged for elimination. Emerging technologies based on proteolysis-targeting chimaeras (PROTACs) that exploit cellular quality control machinery to selectively degrade target proteins are attracting considerable attention in the pharmaceutical industry owing to the advantages they could offer over traditional small-molecule strategies. These advantages include the potential to reduce systemic drug exposure, the ability to counteract increased target protein expression that often accompanies inhibition of protein function and the potential ability to target proteins that are not currently therapeutically tractable, such as transcription factors, scaffolding and regulatory proteins. Twit Text FOAVip Induced protein degradation: an emerging drug discovery paradigm ????Nat Rev Drug Discov http://www.kidney.de/pget.php?&tw=1&pmid=27885283 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=27885283 #FOAvip English Wikipedia <ref>{{Cite pmid|27885283 }}</ref> Induced protein degradation: an emerging drug discovery paradigm #MMPMID27885283 Lai AC ; Crews CM Nat Rev Drug Discov 2017[Feb]; 16 (2 ): 101-114 PMID27885283 show ga Small-molecule drug discovery has traditionally focused on occupancy of a binding site that directly affects protein function, and this approach typically precludes targeting proteins that lack such amenable sites. Furthermore, high systemic drug exposures may be needed to maintain sufficient target inhibition in vivo, increasing the risk of undesirable off-target effects. Induced protein degradation is an alternative approach that is event-driven: upon drug binding, the target protein is tagged for elimination. Emerging technologies based on proteolysis-targeting chimaeras (PROTACs) that exploit cellular quality control machinery to selectively degrade target proteins are attracting considerable attention in the pharmaceutical industry owing to the advantages they could offer over traditional small-molecule strategies. These advantages include the potential to reduce systemic drug exposure, the ability to counteract increased target protein expression that often accompanies inhibition of protein function and the potential ability to target proteins that are not currently therapeutically tractable, such as transcription factors, scaffolding and regulatory proteins. |Animals [MESH] |Drug Discovery/*methods [MESH] |High-Throughput Screening Assays [MESH] |Humans [MESH] |Mutant Chimeric Proteins [MESH] |Protein Binding/drug effects [MESH] |Proteins/*chemistry/drug effects [MESH] |Proteomics [MESH]Induced protein degradation: an emerging drug discovery paradigm (epmc).pdf DeepDyve Pubget Overpricing