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- W4377019861 endingPage "117334" @default.
- W4377019861 startingPage "117334" @default.
- W4377019861 abstract "Over the last two decades, proteolysis targeting chimeras (PROTACs) have been revolutionary in drug development rendering targeted protein degradation (TPD) as an emerging therapeutic modality. These heterobifunctional molecules are comprised of three units: a ligand for the protein of interest (POI), a ligand for an E3 ubiquitin ligase, and a linker that tethers the two motifs together. Von Hippel-Lindau (VHL) is one of the most widely employed E3 ligases in PROTACs development due to its prevalent expression across tissue types and well-characterised ligands. Linker composition and length has proven to play an important role in determining the physicochemical properties and spatial orientation of the POI-PROTAC-E3 ternary complex, thus influencing the bioactivity of degraders. Numerous articles and reports have been published showcasing the medicinal chemistry aspects of the linker design, but few have focused on the chemistry around tethering linkers to E3 ligase ligands. In this review, we focus on the current synthetic linker strategies employed in the assembly of VHL-recruiting PROTACs. We aim to cover a range of fundamental chemistries used to incorporate linkers of varying length, composition and functionality." @default.
- W4377019861 created "2023-05-19" @default.
- W4377019861 creator A5061501904 @default.
- W4377019861 creator A5091972320 @default.
- W4377019861 creator A5091972321 @default.
- W4377019861 creator A5091972322 @default.
- W4377019861 date "2023-06-01" @default.
- W4377019861 modified "2023-10-09" @default.
- W4377019861 title "A beginner’s guide to current synthetic linker strategies towards VHL-recruiting PROTACs" @default.
- W4377019861 cites W1603251764 @default.
- W4377019861 cites W1968222033 @default.
- W4377019861 cites W2002111767 @default.
- W4377019861 cites W2026560403 @default.
- W4377019861 cites W2108366666 @default.
- W4377019861 cites W2151683271 @default.
- W4377019861 cites W2156492800 @default.
- W4377019861 cites W2178689284 @default.
- W4377019861 cites W2292464399 @default.
- W4377019861 cites W2310322011 @default.
- W4377019861 cites W2407533823 @default.
- W4377019861 cites W2546637348 @default.
- W4377019861 cites W2559947248 @default.
- W4377019861 cites W2597078857 @default.
- W4377019861 cites W2604744033 @default.
- W4377019861 cites W2604930678 @default.
- W4377019861 cites W2751709490 @default.
- W4377019861 cites W2761240402 @default.
- W4377019861 cites W2769590617 @default.
- W4377019861 cites W2900888512 @default.
- W4377019861 cites W2903291787 @default.
- W4377019861 cites W2903964626 @default.
- W4377019861 cites W2904001172 @default.
- W4377019861 cites W2909034820 @default.
- W4377019861 cites W2914587883 @default.
- W4377019861 cites W2937372594 @default.
- W4377019861 cites W2948220248 @default.
- W4377019861 cites W2949458744 @default.
- W4377019861 cites W2968714973 @default.
- W4377019861 cites W2973306386 @default.
- W4377019861 cites W2974217727 @default.
- W4377019861 cites W2981857847 @default.
- W4377019861 cites W2987291349 @default.
- W4377019861 cites W2989702634 @default.
- W4377019861 cites W2991059836 @default.
- W4377019861 cites W2994376311 @default.
- W4377019861 cites W2999866448 @default.
- W4377019861 cites W3000673710 @default.
- W4377019861 cites W3006981712 @default.
- W4377019861 cites W3008159666 @default.
- W4377019861 cites W3009753365 @default.
- W4377019861 cites W3011548650 @default.
- W4377019861 cites W3011847211 @default.
- W4377019861 cites W3027174726 @default.
- W4377019861 cites W3043399847 @default.
- W4377019861 cites W3044388665 @default.
- W4377019861 cites W3080366164 @default.
- W4377019861 cites W3088870471 @default.
- W4377019861 cites W3092275826 @default.
- W4377019861 cites W3093395956 @default.
- W4377019861 cites W3093850074 @default.
- W4377019861 cites W3111051161 @default.
- W4377019861 cites W3112704307 @default.
- W4377019861 cites W3117557114 @default.
- W4377019861 cites W3127094302 @default.
- W4377019861 cites W3130443787 @default.
- W4377019861 cites W3136448722 @default.
- W4377019861 cites W3150595399 @default.
- W4377019861 cites W3166162063 @default.
- W4377019861 cites W3167897185 @default.
- W4377019861 cites W3167977328 @default.
- W4377019861 cites W3173540510 @default.
- W4377019861 cites W3177241069 @default.
- W4377019861 cites W3182488106 @default.
- W4377019861 cites W3199626449 @default.
- W4377019861 cites W3203780554 @default.
- W4377019861 cites W3215130076 @default.
- W4377019861 cites W3217439661 @default.
- W4377019861 cites W4205379795 @default.
- W4377019861 cites W4206666355 @default.
- W4377019861 cites W4206822530 @default.
- W4377019861 cites W4214695568 @default.
- W4377019861 cites W4220922043 @default.
- W4377019861 cites W4221082279 @default.
- W4377019861 cites W4226088918 @default.
- W4377019861 cites W4226101063 @default.
- W4377019861 cites W4226189761 @default.
- W4377019861 cites W4241319052 @default.
- W4377019861 cites W4256503849 @default.
- W4377019861 cites W4282926497 @default.
- W4377019861 cites W4283162868 @default.
- W4377019861 cites W4283388590 @default.
- W4377019861 cites W4284958712 @default.
- W4377019861 cites W4292295879 @default.
- W4377019861 cites W4293242763 @default.
- W4377019861 cites W4297517019 @default.
- W4377019861 cites W4304145060 @default.
- W4377019861 cites W4307362175 @default.
- W4377019861 cites W4307405016 @default.