Matches in SemOpenAlex for { <https://semopenalex.org/work/W2343257411> ?p ?o ?g. }
Showing items 1 to 91 of
91
with 100 items per page.
- W2343257411 endingPage "212" @default.
- W2343257411 startingPage "198" @default.
- W2343257411 abstract "SNX 5422 is a synthetic orally bioavailable inhibitor of Hsp90 discovered by the biotechnology company Serenex Inc. (Durham NC, USA) using the chemoproteomic platform proteome mining. The molecule is derived from an indoline scaffold and is therefore structurally distinct from all other known Hsp90 inhibitors reported in the literature. The molecule also inhibits with nM potency the related heat-shock proteins GRP94 and TRAP-1, although it has yet to be established to what extent these actions contribute to its biological effects in vivo. SNX5422 is a pro-drug with oral bioavailability and is hydrolyzed to the active parent compound SNX2112 upon uptake. In cell-based and initial animal studies, and subsequent full pre-clinical work-up, SNX5422 exhibited all the hallmarks of a bona fide Hsp90 inhibitor (i.e. degradation of the expected portfolio of Hsp90-dependent clients, induction of Hsp70, tumor growth arrest). In general, the compound was well tolerated in animals, and showed potent efficacy in a variety of xenograph models of human cancer, both alone and in combination with other existing anticancer agents. The compound was therefore advanced to Phase I safety studies. At the time of writing SNX5422 had completed two Phase I clinical trials conducted by the National Cancer Institutes (Bethesda, MD, USA) and Pfizer (who acquired Serenex in 2008). Chapter 7 covers the discovery and development of SNX5422 and summarizes its biological activities in vivo." @default.
- W2343257411 created "2016-06-24" @default.
- W2343257411 creator A5050348822 @default.
- W2343257411 creator A5090290061 @default.
- W2343257411 date "2013-10-30" @default.
- W2343257411 modified "2023-09-24" @default.
- W2343257411 title "Discovery of the Serenex Hsp90 Inhibitor, SNX5422" @default.
- W2343257411 cites W1507401672 @default.
- W2343257411 cites W1591880539 @default.
- W2343257411 cites W1953493409 @default.
- W2343257411 cites W1966229978 @default.
- W2343257411 cites W1980078464 @default.
- W2343257411 cites W1987040923 @default.
- W2343257411 cites W1994526004 @default.
- W2343257411 cites W2015743156 @default.
- W2343257411 cites W2030205108 @default.
- W2343257411 cites W2033706352 @default.
- W2343257411 cites W2042819247 @default.
- W2343257411 cites W2042985720 @default.
- W2343257411 cites W2053503219 @default.
- W2343257411 cites W2067405360 @default.
- W2343257411 cites W2079088085 @default.
- W2343257411 cites W2085961273 @default.
- W2343257411 cites W2090694532 @default.
- W2343257411 cites W2091688075 @default.
- W2343257411 cites W2096955693 @default.
- W2343257411 cites W2113007147 @default.
- W2343257411 cites W2127975859 @default.
- W2343257411 cites W2138778824 @default.
- W2343257411 cites W2139306838 @default.
- W2343257411 cites W2167117858 @default.
- W2343257411 cites W2327219846 @default.
- W2343257411 cites W2407600696 @default.
- W2343257411 cites W4210407906 @default.
- W2343257411 cites W4251383293 @default.
- W2343257411 cites W86567913 @default.
- W2343257411 doi "https://doi.org/10.1039/9781849739689-00198" @default.
- W2343257411 hasPublicationYear "2013" @default.
- W2343257411 type Work @default.
- W2343257411 sameAs 2343257411 @default.
- W2343257411 citedByCount "0" @default.
- W2343257411 crossrefType "book-chapter" @default.
- W2343257411 hasAuthorship W2343257411A5050348822 @default.
- W2343257411 hasAuthorship W2343257411A5090290061 @default.
- W2343257411 hasConcept C104317684 @default.
- W2343257411 hasConcept C150903083 @default.
- W2343257411 hasConcept C181389837 @default.
- W2343257411 hasConcept C185592680 @default.
- W2343257411 hasConcept C205260736 @default.
- W2343257411 hasConcept C207001950 @default.
- W2343257411 hasConcept C2775932338 @default.
- W2343257411 hasConcept C2777560012 @default.
- W2343257411 hasConcept C502942594 @default.
- W2343257411 hasConcept C55493867 @default.
- W2343257411 hasConcept C70721500 @default.
- W2343257411 hasConcept C74187038 @default.
- W2343257411 hasConcept C86803240 @default.
- W2343257411 hasConcept C98274493 @default.
- W2343257411 hasConceptScore W2343257411C104317684 @default.
- W2343257411 hasConceptScore W2343257411C150903083 @default.
- W2343257411 hasConceptScore W2343257411C181389837 @default.
- W2343257411 hasConceptScore W2343257411C185592680 @default.
- W2343257411 hasConceptScore W2343257411C205260736 @default.
- W2343257411 hasConceptScore W2343257411C207001950 @default.
- W2343257411 hasConceptScore W2343257411C2775932338 @default.
- W2343257411 hasConceptScore W2343257411C2777560012 @default.
- W2343257411 hasConceptScore W2343257411C502942594 @default.
- W2343257411 hasConceptScore W2343257411C55493867 @default.
- W2343257411 hasConceptScore W2343257411C70721500 @default.
- W2343257411 hasConceptScore W2343257411C74187038 @default.
- W2343257411 hasConceptScore W2343257411C86803240 @default.
- W2343257411 hasConceptScore W2343257411C98274493 @default.
- W2343257411 hasLocation W23432574111 @default.
- W2343257411 hasOpenAccess W2343257411 @default.
- W2343257411 hasPrimaryLocation W23432574111 @default.
- W2343257411 hasRelatedWork W2012172048 @default.
- W2343257411 hasRelatedWork W2020390659 @default.
- W2343257411 hasRelatedWork W2047334344 @default.
- W2343257411 hasRelatedWork W2049605560 @default.
- W2343257411 hasRelatedWork W2090231065 @default.
- W2343257411 hasRelatedWork W2153947444 @default.
- W2343257411 hasRelatedWork W2348318784 @default.
- W2343257411 hasRelatedWork W2900956587 @default.
- W2343257411 hasRelatedWork W3107154733 @default.
- W2343257411 hasRelatedWork W4225277224 @default.
- W2343257411 isParatext "false" @default.
- W2343257411 isRetracted "false" @default.
- W2343257411 magId "2343257411" @default.
- W2343257411 workType "book-chapter" @default.