Matches in SemOpenAlex for { <https://semopenalex.org/work/W1837009307> ?p ?o ?g. }
Showing items 1 to 94 of
94
with 100 items per page.
- W1837009307 abstract "Proceedings: AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CAThe canonical Wnt pathway regulates the ability of β-catenin to activate specific target genes. Aberrant activation of the Wnt pathway is believed to drive the development and growth of many cancers; for example, APC mutations were observed in >80% of the sporadic colorectal cancers. The casein kinase 1 (CK1) family of serine/threonine protein kinases is highly conserved. Multiple members of the CK1 family are shown to regulate the Wnt pathway through interactions with various proteins. The central role of CK1γ in Wnt signal transduction makes it an attractive target for the treatment of Wnt-pathway dependent cancers. We employed a structure-based approach and identified a series of pyridyl pyrrolopyridinones as potent and selective CK1γ inhibitors. These compounds exhibited good enzyme and cell potency, as well as selectivity against other CK1 isoforms, and favorable rodent PK profiles. Oral dosing of optimized lead compounds resulted in significant inhibition of LRP6 phosphorylation in a mouse tumor PD model.Citation Format: Hongbing Huang, Lisa Acquaviva, Howard Bregman, John Buchanan, Nagasree Chakka, Erin F. DiMauro, Jennifer Dovey, Hakan Gunaydin, Zihao Hua, Xin Huang, Liyue Huang, Vinod F. Patel, Matthew W. Martin, Randy Serafino, Cindy Wilson. Discovery of pyridyl pyrrolopyridinones as potent and selective CK1γ inhibitors. [abstract]. In: Proceedings of the 105th Annual Meeting of the American Association for Cancer Research; 2014 Apr 5-9; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2014;74(19 Suppl):Abstract nr 1621. doi:10.1158/1538-7445.AM2014-1621" @default.
- W1837009307 created "2016-06-24" @default.
- W1837009307 creator A5007100513 @default.
- W1837009307 creator A5008598686 @default.
- W1837009307 creator A5018799253 @default.
- W1837009307 creator A5028265641 @default.
- W1837009307 creator A5032342352 @default.
- W1837009307 creator A5037666395 @default.
- W1837009307 creator A5051089170 @default.
- W1837009307 creator A5051160676 @default.
- W1837009307 creator A5051379817 @default.
- W1837009307 creator A5065381552 @default.
- W1837009307 creator A5070673203 @default.
- W1837009307 creator A5071841589 @default.
- W1837009307 creator A5077823599 @default.
- W1837009307 creator A5078718914 @default.
- W1837009307 creator A5091908601 @default.
- W1837009307 date "2014-09-30" @default.
- W1837009307 modified "2023-09-27" @default.
- W1837009307 title "Abstract 1621: Discovery of pyridyl pyrrolopyridinones as potent and selective CK1γ inhibitors" @default.
- W1837009307 doi "https://doi.org/10.1158/1538-7445.am2014-1621" @default.
- W1837009307 hasPublicationYear "2014" @default.
- W1837009307 type Work @default.
- W1837009307 sameAs 1837009307 @default.
- W1837009307 citedByCount "0" @default.
- W1837009307 crossrefType "proceedings-article" @default.
- W1837009307 hasAuthorship W1837009307A5007100513 @default.
- W1837009307 hasAuthorship W1837009307A5008598686 @default.
- W1837009307 hasAuthorship W1837009307A5018799253 @default.
- W1837009307 hasAuthorship W1837009307A5028265641 @default.
- W1837009307 hasAuthorship W1837009307A5032342352 @default.
- W1837009307 hasAuthorship W1837009307A5037666395 @default.
- W1837009307 hasAuthorship W1837009307A5051089170 @default.
- W1837009307 hasAuthorship W1837009307A5051160676 @default.
- W1837009307 hasAuthorship W1837009307A5051379817 @default.
- W1837009307 hasAuthorship W1837009307A5065381552 @default.
- W1837009307 hasAuthorship W1837009307A5070673203 @default.
- W1837009307 hasAuthorship W1837009307A5071841589 @default.
- W1837009307 hasAuthorship W1837009307A5077823599 @default.
- W1837009307 hasAuthorship W1837009307A5078718914 @default.
- W1837009307 hasAuthorship W1837009307A5091908601 @default.
- W1837009307 hasConcept C11960822 @default.
- W1837009307 hasConcept C121608353 @default.
- W1837009307 hasConcept C126322002 @default.
- W1837009307 hasConcept C137620995 @default.
- W1837009307 hasConcept C160110348 @default.
- W1837009307 hasConcept C184235292 @default.
- W1837009307 hasConcept C2776414213 @default.
- W1837009307 hasConcept C502942594 @default.
- W1837009307 hasConcept C55493867 @default.
- W1837009307 hasConcept C62478195 @default.
- W1837009307 hasConcept C71924100 @default.
- W1837009307 hasConcept C86803240 @default.
- W1837009307 hasConcept C97029542 @default.
- W1837009307 hasConceptScore W1837009307C11960822 @default.
- W1837009307 hasConceptScore W1837009307C121608353 @default.
- W1837009307 hasConceptScore W1837009307C126322002 @default.
- W1837009307 hasConceptScore W1837009307C137620995 @default.
- W1837009307 hasConceptScore W1837009307C160110348 @default.
- W1837009307 hasConceptScore W1837009307C184235292 @default.
- W1837009307 hasConceptScore W1837009307C2776414213 @default.
- W1837009307 hasConceptScore W1837009307C502942594 @default.
- W1837009307 hasConceptScore W1837009307C55493867 @default.
- W1837009307 hasConceptScore W1837009307C62478195 @default.
- W1837009307 hasConceptScore W1837009307C71924100 @default.
- W1837009307 hasConceptScore W1837009307C86803240 @default.
- W1837009307 hasConceptScore W1837009307C97029542 @default.
- W1837009307 hasLocation W18370093071 @default.
- W1837009307 hasOpenAccess W1837009307 @default.
- W1837009307 hasPrimaryLocation W18370093071 @default.
- W1837009307 hasRelatedWork W1968832908 @default.
- W1837009307 hasRelatedWork W1970209296 @default.
- W1837009307 hasRelatedWork W1971947883 @default.
- W1837009307 hasRelatedWork W1991500129 @default.
- W1837009307 hasRelatedWork W2068728061 @default.
- W1837009307 hasRelatedWork W2072589624 @default.
- W1837009307 hasRelatedWork W2078358665 @default.
- W1837009307 hasRelatedWork W2085039090 @default.
- W1837009307 hasRelatedWork W2091013891 @default.
- W1837009307 hasRelatedWork W2097690387 @default.
- W1837009307 hasRelatedWork W2234429706 @default.
- W1837009307 hasRelatedWork W2407580700 @default.
- W1837009307 hasRelatedWork W2431421260 @default.
- W1837009307 hasRelatedWork W2499212547 @default.
- W1837009307 hasRelatedWork W2517249684 @default.
- W1837009307 hasRelatedWork W2922140265 @default.
- W1837009307 hasRelatedWork W2954467453 @default.
- W1837009307 hasRelatedWork W2992271344 @default.
- W1837009307 hasRelatedWork W601853544 @default.
- W1837009307 hasRelatedWork W653456025 @default.
- W1837009307 isParatext "false" @default.
- W1837009307 isRetracted "false" @default.
- W1837009307 magId "1837009307" @default.
- W1837009307 workType "article" @default.