Matches in SemOpenAlex for { <https://semopenalex.org/work/W4309492242> ?p ?o ?g. }
- W4309492242 endingPage "270" @default.
- W4309492242 startingPage "247" @default.
- W4309492242 abstract "PROteolysis-TArgeting Chimera (PROTACs) represent a new-age therapeutic approach for unmet medical needs. These molecules possess a great potential as protein degraders, which target the overexpressed proteins with a major role in the disease pathophysiology, progression, and maintenance. Rather than inhibiting the macromolecular targets by small-molecule drugs, PROTACs recruit them to ubiquitin-proteasomal system (UPS) due to their unique ability to bind to E3 ligases on one end and the protein-of-interest (POI) on the other. The subsequent polyubiquitination of the POI leads to its degradation by 26S proteasome. The PROTAC then binds to the new POI molecule and the process continues. The catalytic role played by these entities necessitates a smaller dose for the therapeutic effect. Majority of the reported agents are targeted for cancer treatment, including the most advanced clinical agents – ARV-110 and ARV-471, both in Phase 2, while many small-molecule candidates are already in Phase 1. Other therapeutic indications include inflammatory diseases, neurodegenerative diseases, immunological diseases, and viral infections. Despite the interest by the pharmaceutical industry, challenges in PROTACs development remain. These include synthetic, cell permeation, metabolic stability, and in vivo bioavailability issues. The development of resistance to these agents has been observed lately. The new-age candidates are being targeted for G-protein-coupled receptors ( GPCRs ), RNA-binding proteins, and many other POIs. The promises and hope offered by the PROTACs are real and they are going to revolutionize the therapeutic targeting of undruggable genomes and drug-resistant proteins." @default.
- W4309492242 created "2022-11-28" @default.
- W4309492242 creator A5069312240 @default.
- W4309492242 creator A5089418881 @default.
- W4309492242 date "2022-11-18" @default.
- W4309492242 modified "2023-10-14" @default.
- W4309492242 title "Application of <scp>PROTAC</scp> Technology in Drug Development" @default.
- W4309492242 cites W2052268618 @default.
- W4309492242 cites W2090983338 @default.
- W4309492242 cites W2176682109 @default.
- W4309492242 cites W2340678549 @default.
- W4309492242 cites W2735605417 @default.
- W4309492242 cites W2791709201 @default.
- W4309492242 cites W2792069216 @default.
- W4309492242 cites W2805296794 @default.
- W4309492242 cites W2883077013 @default.
- W4309492242 cites W2891213440 @default.
- W4309492242 cites W2902166673 @default.
- W4309492242 cites W2908747386 @default.
- W4309492242 cites W2913322889 @default.
- W4309492242 cites W2914719317 @default.
- W4309492242 cites W2917115789 @default.
- W4309492242 cites W2921294745 @default.
- W4309492242 cites W2944640816 @default.
- W4309492242 cites W2946370603 @default.
- W4309492242 cites W2949458744 @default.
- W4309492242 cites W2960105328 @default.
- W4309492242 cites W2966441858 @default.
- W4309492242 cites W2968014120 @default.
- W4309492242 cites W2970837975 @default.
- W4309492242 cites W2973216672 @default.
- W4309492242 cites W2977584853 @default.
- W4309492242 cites W2981722541 @default.
- W4309492242 cites W2982299031 @default.
- W4309492242 cites W2982416093 @default.
- W4309492242 cites W2983017086 @default.
- W4309492242 cites W2996380129 @default.
- W4309492242 cites W2997874238 @default.
- W4309492242 cites W3002542796 @default.
- W4309492242 cites W3011413773 @default.
- W4309492242 cites W3011548650 @default.
- W4309492242 cites W3016041115 @default.
- W4309492242 cites W3020980264 @default.
- W4309492242 cites W3027679488 @default.
- W4309492242 cites W3034911617 @default.
- W4309492242 cites W3042697772 @default.
- W4309492242 cites W3046562742 @default.
- W4309492242 cites W3082051822 @default.
- W4309492242 cites W3084944257 @default.
- W4309492242 cites W3093071830 @default.
- W4309492242 cites W3095840616 @default.
- W4309492242 cites W3096947063 @default.
- W4309492242 cites W3103592087 @default.
- W4309492242 cites W3107131835 @default.
- W4309492242 cites W3112568052 @default.
- W4309492242 cites W3117557114 @default.
- W4309492242 cites W3123765654 @default.
- W4309492242 cites W3156593072 @default.
- W4309492242 cites W3160556876 @default.
- W4309492242 cites W3160714053 @default.
- W4309492242 cites W3163006786 @default.
- W4309492242 cites W3167295725 @default.
- W4309492242 cites W3182488106 @default.
- W4309492242 cites W3185882124 @default.
- W4309492242 doi "https://doi.org/10.1002/9783527827855.ch10" @default.
- W4309492242 hasPublicationYear "2022" @default.
- W4309492242 type Work @default.
- W4309492242 citedByCount "0" @default.
- W4309492242 crossrefType "other" @default.
- W4309492242 hasAuthorship W4309492242A5069312240 @default.
- W4309492242 hasAuthorship W4309492242A5089418881 @default.
- W4309492242 hasConcept C104317684 @default.
- W4309492242 hasConcept C25602115 @default.
- W4309492242 hasConcept C27740335 @default.
- W4309492242 hasConcept C2780035454 @default.
- W4309492242 hasConcept C2992195973 @default.
- W4309492242 hasConcept C55493867 @default.
- W4309492242 hasConcept C60644358 @default.
- W4309492242 hasConcept C64903051 @default.
- W4309492242 hasConcept C70721500 @default.
- W4309492242 hasConcept C71924100 @default.
- W4309492242 hasConcept C74187038 @default.
- W4309492242 hasConcept C86803240 @default.
- W4309492242 hasConcept C95444343 @default.
- W4309492242 hasConcept C98274493 @default.
- W4309492242 hasConceptScore W4309492242C104317684 @default.
- W4309492242 hasConceptScore W4309492242C25602115 @default.
- W4309492242 hasConceptScore W4309492242C27740335 @default.
- W4309492242 hasConceptScore W4309492242C2780035454 @default.
- W4309492242 hasConceptScore W4309492242C2992195973 @default.
- W4309492242 hasConceptScore W4309492242C55493867 @default.
- W4309492242 hasConceptScore W4309492242C60644358 @default.
- W4309492242 hasConceptScore W4309492242C64903051 @default.
- W4309492242 hasConceptScore W4309492242C70721500 @default.
- W4309492242 hasConceptScore W4309492242C71924100 @default.
- W4309492242 hasConceptScore W4309492242C74187038 @default.
- W4309492242 hasConceptScore W4309492242C86803240 @default.
- W4309492242 hasConceptScore W4309492242C95444343 @default.