FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2154493372> ?p ?o ?g. }

• W2154493372 endingPage "334" @default.
• W2154493372 startingPage "326" @default.
• W2154493372 abstract "Medullary and papillary thyroid carcinomas are often associated with oncogenic activation of the RET tyrosine kinase. We evaluated whether the biaryl urea BAY 43-9006, which is known to inhibit several other tyrosine kinases, blocks RET kinase function and oncogenic activity.We examined BAY 43-9006 activity against oncogenic RET in vitro and in cellular RET signaling in oncogenic RET-transfected NIH3T3 fibroblasts by using immunocomplex kinase assays and immunoblotting with phospho-specific antibodies. The effects of BAY 43-9006 on proliferation of human TPC1 and TT thyroid carcinoma cells, which harbor spontaneous oncogenic RET alleles, and on RAT1 fibroblasts transformed with oncogenic RET mutants, including mutants that are resistant to other chemotherapeutic agents, were determined using growth curves and flow cytometry. Growth of TT cell-derived xenograft tumors in athymic mice treated orally with BAY 43-9006 or with vehicle was measured. All statistical tests were two-sided.BAY 43-9006 inhibited oncogenic RET kinase activity at half-maximal inhibitory concentrations (IC50s) of 50 nM or less in NIH3T3 cells. It also arrested the growth of NIH3T3 and RAT1 fibroblasts transformed by oncogenic RET and of thyroid carcinoma cells that harbor spontaneous oncogenic RET alleles. Moreover, BAY 43-9006 inhibited the growth of cells carrying RET V804L (IC50 = 110 nM, 95% confidence interval [CI] = 88 to 133 nM) or RET V804M (IC50 = 147 nM, 95% CI = 123 nM to 170 nM), both mutants that are resistant to anilinoquinazolines and pyrazolopyrimidines. After 3 weeks of oral treatment with BAY 43-9006 (60 mg/kg/day), the volume of TT cell xenografts (n = 7) was reduced from 72.5 to 44 mm3 (difference = 28.5 mm3, 95% CI = 7 mm3 to 50 mm3), whereas in vehicle-treated mice (n = 7), mean tumor volume increased to 408 mm3 (difference = 320 mm3, 95% CI = 180 mm3 to 460 mm3; untreated versus treated, P =.02). This inhibition paralleled a decrease in RET phosphorylation.BAY 43-9006 is a powerful inhibitor of the RET kinase. Its potential as a therapeutic tool for RET-positive thyroid tumors, including those expressing V804 mutations merits study." @default.
• W2154493372 created "2016-06-24" @default.
• W2154493372 creator A5015782345 @default.
• W2154493372 creator A5020376130 @default.
• W2154493372 creator A5032330087 @default.
• W2154493372 creator A5048243012 @default.
• W2154493372 creator A5048413494 @default.
• W2154493372 creator A5067056980 @default.
• W2154493372 creator A5087264016 @default.
• W2154493372 date "2006-03-01" @default.
• W2154493372 modified "2023-10-14" @default.
• W2154493372 title "BAY 43-9006 Inhibition of Oncogenic RET Mutants" @default.
• W2154493372 cites W1963579412 @default.
• W2154493372 cites W1969482148 @default.
• W2154493372 cites W1980886652 @default.
• W2154493372 cites W1985219947 @default.
• W2154493372 cites W1988242880 @default.
• W2154493372 cites W1988897856 @default.
• W2154493372 cites W1991920146 @default.
• W2154493372 cites W1997087712 @default.
• W2154493372 cites W2002937040 @default.
• W2154493372 cites W2003984225 @default.
• W2154493372 cites W2005556522 @default.
• W2154493372 cites W2012952884 @default.
• W2154493372 cites W2043768887 @default.
• W2154493372 cites W2057936106 @default.
• W2154493372 cites W2058743530 @default.
• W2154493372 cites W2069398477 @default.
• W2154493372 cites W2082170965 @default.
• W2154493372 cites W2092436145 @default.
• W2154493372 cites W2114578972 @default.
• W2154493372 cites W2124196948 @default.
• W2154493372 cites W2125695627 @default.
• W2154493372 cites W2126497869 @default.
• W2154493372 cites W2128805986 @default.
• W2154493372 cites W2138621695 @default.
• W2154493372 cites W2140765540 @default.
• W2154493372 cites W2141398233 @default.
• W2154493372 cites W2142586136 @default.
• W2154493372 cites W2144785546 @default.
• W2154493372 cites W2148763134 @default.
• W2154493372 cites W2157367076 @default.
• W2154493372 cites W2317053903 @default.
• W2154493372 cites W2988080293 @default.
• W2154493372 cites W4211107646 @default.
• W2154493372 cites W4248988283 @default.
• W2154493372 cites W4293247451 @default.
• W2154493372 doi "https://doi.org/10.1093/jnci/djj069" @default.
• W2154493372 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/16507829" @default.
• W2154493372 hasPublicationYear "2006" @default.
• W2154493372 type Work @default.
• W2154493372 sameAs 2154493372 @default.
• W2154493372 citedByCount "432" @default.
• W2154493372 countsByYear W21544933722012 @default.
• W2154493372 countsByYear W21544933722013 @default.
• W2154493372 countsByYear W21544933722014 @default.
• W2154493372 countsByYear W21544933722015 @default.
• W2154493372 countsByYear W21544933722016 @default.
• W2154493372 countsByYear W21544933722017 @default.
• W2154493372 countsByYear W21544933722018 @default.
• W2154493372 countsByYear W21544933722019 @default.
• W2154493372 countsByYear W21544933722020 @default.
• W2154493372 countsByYear W21544933722021 @default.
• W2154493372 countsByYear W21544933722022 @default.
• W2154493372 countsByYear W21544933722023 @default.
• W2154493372 crossrefType "journal-article" @default.
• W2154493372 hasAuthorship W2154493372A5015782345 @default.
• W2154493372 hasAuthorship W2154493372A5020376130 @default.
• W2154493372 hasAuthorship W2154493372A5032330087 @default.
• W2154493372 hasAuthorship W2154493372A5048243012 @default.
• W2154493372 hasAuthorship W2154493372A5048413494 @default.
• W2154493372 hasAuthorship W2154493372A5067056980 @default.
• W2154493372 hasAuthorship W2154493372A5087264016 @default.
• W2154493372 hasBestOaLocation W21544933721 @default.
• W2154493372 hasConcept C101544691 @default.
• W2154493372 hasConcept C104317684 @default.
• W2154493372 hasConcept C115880899 @default.
• W2154493372 hasConcept C11960822 @default.
• W2154493372 hasConcept C127413603 @default.
• W2154493372 hasConcept C134018914 @default.
• W2154493372 hasConcept C143065580 @default.
• W2154493372 hasConcept C147176958 @default.
• W2154493372 hasConcept C153911025 @default.
• W2154493372 hasConcept C160539049 @default.
• W2154493372 hasConcept C170493617 @default.
• W2154493372 hasConcept C184235292 @default.
• W2154493372 hasConcept C185592680 @default.
• W2154493372 hasConcept C185856081 @default.
• W2154493372 hasConcept C2908751931 @default.
• W2154493372 hasConcept C2993294228 @default.
• W2154493372 hasConcept C42362537 @default.
• W2154493372 hasConcept C502942594 @default.
• W2154493372 hasConcept C526584372 @default.
• W2154493372 hasConcept C54355233 @default.
• W2154493372 hasConcept C55493867 @default.
• W2154493372 hasConcept C62112901 @default.
• W2154493372 hasConcept C62478195 @default.
• W2154493372 hasConcept C81885089 @default.

• next