Therapeutic targeting of transcriptional cyclin-dependent kinases.
CDK
CTD
RNA polymerase II
elongation
transcription
Journal
Transcription
ISSN: 2154-1272
Titre abrégé: Transcription
Pays: United States
ID NLM: 101530967
Informations de publication
Date de publication:
04 2019
04 2019
Historique:
pubmed:
10
11
2018
medline:
2
5
2019
entrez:
10
11
2018
Statut:
ppublish
Résumé
The fact that many cancer types display transcriptional addiction driven by dysregulation of oncogenic enhancers and transcription factors has led to increased interest in a group of protein kinases, known as transcriptional cyclin dependent kinases (tCDKs), as potential therapeutic targets. Despite early reservations about targeting a process that is essential to healthy cell types, there is now evidence that targeting tCDKs could provide enough therapeutic window to be effective in the clinic. Here, we discuss recent developments in this field, with an emphasis on highly-selective inhibitors and the challenges to be addressed before these inhibitors could be used for therapeutic purposes. Abbreviations: CAK: CDK-activating kinase;CDK: cyclin-dependent kinase;CMGC group: CDK-, MAPK-, GSK3-, and CLK-like;CTD: C-terminal repeat domain of the RPB1 subunit of RNA polymerase II;DRB: 5,6-dichloro-1-β-D-ribofuranosylbenzimidazole;mCRPC: metastatic castration-resistant prostate cancer;NSCLC: non-small cell lung cancer;P-TEFb: positive elongation factor b;RNAPII: RNA polymerase II;S2: serine-2 of CTD repeats;S5: serine-5 of CTD repeats;S7: serine-7 of CTD repeats;SEC: super elongation complex;tCDK: transcriptional cyclin-dependent kinase;TNBC: triple-negative breast cancer.
Identifiants
pubmed: 30409083
doi: 10.1080/21541264.2018.1539615
pmc: PMC6602565
doi:
Substances chimiques
Antineoplastic Agents
0
Protein Kinase Inhibitors
0
Cyclin-Dependent Kinases
EC 2.7.11.22
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, U.S. Gov't, Non-P.H.S.
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
118-136Subventions
Organisme : NCI NIH HHS
ID : R01 CA117907
Pays : United States
Organisme : NIGMS NIH HHS
ID : R01 GM120109
Pays : United States
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