Matches in SemOpenAlex for { <https://semopenalex.org/work/W2159838315> ?p ?o ?g. }
Showing items 1 to 68 of
68
with 100 items per page.
- W2159838315 endingPage "212" @default.
- W2159838315 startingPage "200" @default.
- W2159838315 abstract "The pivotal role of proteases in many diseases has generated considerable interest in their basic biology, and in the potential to target them for chemotherapy. Although fundamental to the initiation and progression of diseases such as cancer, diabetes, arthritis and malaria, in many cases their precise role remains unknown. Activity-based chemical proteomics-an emerging field involving a combination of organic synthesis, biochemistry, cell biology, biophysics and bioinformatics-allows the detection, visualisation and activity quantification of whole families or selected sub-sets of proteases based upon their substrate specificity. This approach can be applied for drug target/lead identification and validation, the fundamentals of drug discovery. The activity-based probes discussed in this review contain three key features; a ‘warhead’ (binds irreversibly but selectively to the active site), a ‘tag’ (allowing enzyme ‘handling’, with a combination of fluorescent, affinity and/or radio labels), and a linker region between warhead and tag. From the design and synthesis of the linker arise some of the latest developments discussed here; not only can the physical properties (e.g., solubility, localisation) of the probe be tuned, but the inclusion of a cleavable moiety allows selective removal of tagged enzyme from affinity beads etc. The design and synthesis of recently reported probes is discussed, including modular assembly of highly versatile probes via solid phase synthesis. Recent applications of activity-based protein profiling to specific proteases (serine, threonine, cysteine and metalloproteases) are reviewed as are demonstrations of their use in the study of disease function in cancer and malaria. Keywords: Protease, proteomics, activity based probes, drug targets, click chemistry, solid phase synthesis, target validation, cleavable linker" @default.
- W2159838315 created "2016-06-24" @default.
- W2159838315 creator A5001533319 @default.
- W2159838315 creator A5018429085 @default.
- W2159838315 creator A5080941265 @default.
- W2159838315 date "2008-09-01" @default.
- W2159838315 modified "2023-09-23" @default.
- W2159838315 title "Activity Based Chemical Proteomics: Profiling Proteases as Drug Targets" @default.
- W2159838315 doi "https://doi.org/10.2174/157016308785739866" @default.
- W2159838315 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/18690889" @default.
- W2159838315 hasPublicationYear "2008" @default.
- W2159838315 type Work @default.
- W2159838315 sameAs 2159838315 @default.
- W2159838315 citedByCount "22" @default.
- W2159838315 countsByYear W21598383152012 @default.
- W2159838315 countsByYear W21598383152013 @default.
- W2159838315 countsByYear W21598383152014 @default.
- W2159838315 countsByYear W21598383152015 @default.
- W2159838315 countsByYear W21598383152017 @default.
- W2159838315 countsByYear W21598383152019 @default.
- W2159838315 crossrefType "journal-article" @default.
- W2159838315 hasAuthorship W2159838315A5001533319 @default.
- W2159838315 hasAuthorship W2159838315A5018429085 @default.
- W2159838315 hasAuthorship W2159838315A5080941265 @default.
- W2159838315 hasConcept C104317684 @default.
- W2159838315 hasConcept C171852809 @default.
- W2159838315 hasConcept C181199279 @default.
- W2159838315 hasConcept C182220744 @default.
- W2159838315 hasConcept C185592680 @default.
- W2159838315 hasConcept C2776714187 @default.
- W2159838315 hasConcept C46111723 @default.
- W2159838315 hasConcept C55493867 @default.
- W2159838315 hasConcept C70721500 @default.
- W2159838315 hasConcept C74187038 @default.
- W2159838315 hasConcept C86803240 @default.
- W2159838315 hasConceptScore W2159838315C104317684 @default.
- W2159838315 hasConceptScore W2159838315C171852809 @default.
- W2159838315 hasConceptScore W2159838315C181199279 @default.
- W2159838315 hasConceptScore W2159838315C182220744 @default.
- W2159838315 hasConceptScore W2159838315C185592680 @default.
- W2159838315 hasConceptScore W2159838315C2776714187 @default.
- W2159838315 hasConceptScore W2159838315C46111723 @default.
- W2159838315 hasConceptScore W2159838315C55493867 @default.
- W2159838315 hasConceptScore W2159838315C70721500 @default.
- W2159838315 hasConceptScore W2159838315C74187038 @default.
- W2159838315 hasConceptScore W2159838315C86803240 @default.
- W2159838315 hasIssue "3" @default.
- W2159838315 hasLocation W21598383151 @default.
- W2159838315 hasLocation W21598383152 @default.
- W2159838315 hasOpenAccess W2159838315 @default.
- W2159838315 hasPrimaryLocation W21598383151 @default.
- W2159838315 hasRelatedWork W1004757146 @default.
- W2159838315 hasRelatedWork W1965819162 @default.
- W2159838315 hasRelatedWork W2007208290 @default.
- W2159838315 hasRelatedWork W2069508712 @default.
- W2159838315 hasRelatedWork W2072272548 @default.
- W2159838315 hasRelatedWork W2122711913 @default.
- W2159838315 hasRelatedWork W2127406568 @default.
- W2159838315 hasRelatedWork W2329621995 @default.
- W2159838315 hasRelatedWork W2380868738 @default.
- W2159838315 hasRelatedWork W2491451478 @default.
- W2159838315 hasVolume "5" @default.
- W2159838315 isParatext "false" @default.
- W2159838315 isRetracted "false" @default.
- W2159838315 magId "2159838315" @default.
- W2159838315 workType "article" @default.