Matches in SemOpenAlex for { <https://semopenalex.org/work/W4366453105> ?p ?o ?g. }
- W4366453105 endingPage "2337" @default.
- W4366453105 startingPage "2326" @default.
- W4366453105 abstract "Current strategies to inhibit androgen receptor (AR) are circumvented in castration-resistant prostate cancer (CRPC). Cyclin-dependent kinase 7 (CDK7) promotes AR signalling, in addition to established roles in cell cycle and global transcription, providing a rationale for its therapeutic targeting in CRPC.The antitumour activity of CT7001, an orally bioavailable CDK7 inhibitor, was investigated across CRPC models in vitro and in xenograft models in vivo. Cell-based assays and transcriptomic analyses of treated xenografts were employed to investigate the mechanisms driving CT7001 activity, alone and in combination with the antiandrogen enzalutamide.CT7001 selectively engages with CDK7 in prostate cancer cells, causing inhibition of proliferation and cell cycle arrest. Activation of p53, induction of apoptosis, and suppression of transcription mediated by full-length and constitutively active AR splice variants contribute to antitumour efficacy in vitro. Oral administration of CT7001 represses growth of CRPC xenografts and significantly augments growth inhibition achieved by enzalutamide. Transcriptome analyses of treated xenografts indicate cell cycle and AR inhibition as the mode of action of CT7001 in vivo.This study supports CDK7 inhibition as a strategy to target deregulated cell proliferation and demonstrates CT7001 is a promising CRPC therapeutic, alone or in combination with AR-targeting compounds." @default.
- W4366453105 created "2023-04-22" @default.
- W4366453105 creator A5010189211 @default.
- W4366453105 creator A5024566237 @default.
- W4366453105 creator A5027653806 @default.
- W4366453105 creator A5033616141 @default.
- W4366453105 creator A5034697409 @default.
- W4366453105 creator A5042273532 @default.
- W4366453105 creator A5044381904 @default.
- W4366453105 creator A5046383495 @default.
- W4366453105 creator A5048574269 @default.
- W4366453105 creator A5052152507 @default.
- W4366453105 creator A5053097935 @default.
- W4366453105 creator A5055145006 @default.
- W4366453105 creator A5068935163 @default.
- W4366453105 creator A5070453729 @default.
- W4366453105 creator A5072402301 @default.
- W4366453105 creator A5088128749 @default.
- W4366453105 date "2023-04-19" @default.
- W4366453105 modified "2023-10-16" @default.
- W4366453105 title "The CDK7 inhibitor CT7001 (Samuraciclib) targets proliferation pathways to inhibit advanced prostate cancer" @default.
- W4366453105 cites W1578291413 @default.
- W4366453105 cites W1827081793 @default.
- W4366453105 cites W1875122842 @default.
- W4366453105 cites W1919512980 @default.
- W4366453105 cites W1963547267 @default.
- W4366453105 cites W1964471916 @default.
- W4366453105 cites W1977702358 @default.
- W4366453105 cites W1982003542 @default.
- W4366453105 cites W1984143603 @default.
- W4366453105 cites W1993251792 @default.
- W4366453105 cites W1999608828 @default.
- W4366453105 cites W2004278446 @default.
- W4366453105 cites W2013094945 @default.
- W4366453105 cites W2036274810 @default.
- W4366453105 cites W2045673429 @default.
- W4366453105 cites W2060334131 @default.
- W4366453105 cites W2080176881 @default.
- W4366453105 cites W2092021778 @default.
- W4366453105 cites W2109537367 @default.
- W4366453105 cites W2109689528 @default.
- W4366453105 cites W2129214044 @default.
- W4366453105 cites W2153206714 @default.
- W4366453105 cites W2156923287 @default.
- W4366453105 cites W2167742248 @default.
- W4366453105 cites W2171613528 @default.
- W4366453105 cites W2179438025 @default.
- W4366453105 cites W2214074259 @default.
- W4366453105 cites W2344714812 @default.
- W4366453105 cites W2554439427 @default.
- W4366453105 cites W2611637096 @default.
- W4366453105 cites W2762804773 @default.
- W4366453105 cites W2792462338 @default.
- W4366453105 cites W2792645148 @default.
- W4366453105 cites W2897146989 @default.
- W4366453105 cites W2900251974 @default.
- W4366453105 cites W2901306165 @default.
- W4366453105 cites W2905512551 @default.
- W4366453105 cites W2924545529 @default.
- W4366453105 cites W2942460312 @default.
- W4366453105 cites W2942605529 @default.
- W4366453105 cites W2944403040 @default.
- W4366453105 cites W2970215199 @default.
- W4366453105 cites W2997732097 @default.
- W4366453105 cites W3007726005 @default.
- W4366453105 cites W3009540553 @default.
- W4366453105 cites W3014482292 @default.
- W4366453105 cites W3015921770 @default.
- W4366453105 cites W3023627784 @default.
- W4366453105 cites W3029225363 @default.
- W4366453105 cites W3118886469 @default.
- W4366453105 cites W3128646645 @default.
- W4366453105 cites W3201791394 @default.
- W4366453105 cites W3202886367 @default.
- W4366453105 cites W4226018889 @default.
- W4366453105 doi "https://doi.org/10.1038/s41416-023-02252-8" @default.
- W4366453105 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/37076563" @default.
- W4366453105 hasPublicationYear "2023" @default.
- W4366453105 type Work @default.
- W4366453105 citedByCount "1" @default.
- W4366453105 countsByYear W43664531052023 @default.
- W4366453105 crossrefType "journal-article" @default.
- W4366453105 hasAuthorship W4366453105A5010189211 @default.
- W4366453105 hasAuthorship W4366453105A5024566237 @default.
- W4366453105 hasAuthorship W4366453105A5027653806 @default.
- W4366453105 hasAuthorship W4366453105A5033616141 @default.
- W4366453105 hasAuthorship W4366453105A5034697409 @default.
- W4366453105 hasAuthorship W4366453105A5042273532 @default.
- W4366453105 hasAuthorship W4366453105A5044381904 @default.
- W4366453105 hasAuthorship W4366453105A5046383495 @default.
- W4366453105 hasAuthorship W4366453105A5048574269 @default.
- W4366453105 hasAuthorship W4366453105A5052152507 @default.
- W4366453105 hasAuthorship W4366453105A5053097935 @default.
- W4366453105 hasAuthorship W4366453105A5055145006 @default.
- W4366453105 hasAuthorship W4366453105A5068935163 @default.
- W4366453105 hasAuthorship W4366453105A5070453729 @default.
- W4366453105 hasAuthorship W4366453105A5072402301 @default.
- W4366453105 hasAuthorship W4366453105A5088128749 @default.