Transcription associated cyclin-dependent kinases as therapeutic targets for prostate cancer

Targeting CDK7 suppresses super enhancer-linked inflammatory genes and alleviates CAR T cell-induced cytokine release syndrome

(2021) Ye Wei et al.   Molecular Cancer

Structure and noncanonical Cdk8 activation mechanism within an Argonaute-containing Mediator kinase module

(2021) Yi-Chuan Li et al.   Science Advances

Discovery and resistance mechanism of a selective CDK12 degrader

(2021) Baishan Jiang et al.   Nature Chemical Biology

13P SY-5609, a highly potent and selective oral CDK7 inhibitor, exhibits robust antitumor activity in preclinical models of KRAS mutant cancers as a single agent and in combination with chemotherapy

(2021) S.H. Henry et al.   ANNALS OF ONCOLOGY

Safety and efficacy of VIP152, a CDK9 inhibitor, in patients with double-hit lymphoma (DHL).

(2021) Victor Moreno et al.   JOURNAL OF CLINICAL ONCOLOGY

CRISPR screening identifies CDK12 as a conservative vulnerability of prostate cancer

(2021) Hanqi Lei et al.   Cell Death & Disease

Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma

(2021) Baishan Jiang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7

(2021) Jason J. Marineau et al.   JOURNAL OF MEDICINAL CHEMISTRY

CDK7 Inhibition is Effective in all the Subtypes of Breast Cancer: Determinants of Response and Synergy with EGFR Inhibition

(2020) Martina S.J. McDermott et al.   Cells

Selective Mediator dependence of cell-type-specifying transcription

(2020) Martin G. Jaeger et al.   NATURE GENETICS

CDK11 is required for transcription of replication-dependent histone genes

(2020) Pavla Gajdušková et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Potent anti-tumor activity of AUR102, a selective covalent inhibitor of CDK7

(2020) L.K. Satyam et al.   EUROPEAN JOURNAL OF CANCER

Selective inhibition of CDK7 reveals high-confidence targets and new models for TFIIH function in transcription

(2020) Jenna K. Rimel et al.   GENES & DEVELOPMENT

Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies

(2020) Bernard Barlaam et al.   JOURNAL OF MEDICINAL CHEMISTRY

Super-enhancer in prostate cancer: transcriptional disorders and therapeutic targets

(2020) Xuanrong Chen et al.   npj Precision Oncology

Discovery and characterization of SY-1365, a selective, covalent inhibitor of CDK7

(2019) Shanhu Hu et al.   CANCER RESEARCH

The complete structure of the human TFIIH core complex

(2019) Basil J Greber et al.   eLife

Structural basis of TFIIH activation for nucleotide excision repair

(2019) Goran Kokic et al.   Nature Communications

CDK12 loss in cancer cells affects DNA damage response genes through premature cleavage and polyadenylation

(2019) Malgorzata Krajewska et al.   Nature Communications

Inhibition of the transcriptional kinase CDK7 overcomes therapeutic resistance in HER2-positive breast cancers

(2019) Bowen Sun et al.   ONCOGENE

CDK7 inhibition suppresses Castration-Resistant Prostate Cancer through MED1 inactivation

(2019) Reyaz Ur Rasool et al.   Cancer Discovery

Therapeutic Targeting of CDK12/CDK13 in Triple-Negative Breast Cancer

(2019) Victor Quereda et al.   CANCER CELL

AZD4573 is a highly selective CDK9 inhibitor that suppresses Mcl-1 and induces apoptosis in hematological cancer cells.

(2019) Justin Cidado et al.   CLINICAL CANCER RESEARCH

Systemic Toxicity Reported for CDK8/19 Inhibitors CCT251921 and MSC2530818 Is Not Due to Target Inhibition

(2019) Mengqian Chen et al.   Cells

CDK7 Inhibition Potentiates Genome Instability Triggering Anti-tumor Immunity in Small Cell Lung Cancer

(2019) Hua Zhang et al.   CANCER CELL

A novel CDK9 inhibitor increases the efficacy of venetoclax (ABT-199) in multiple models of hematologic malignancies

(2019) Darren C. Phillips et al.   LEUKEMIA

Cyclin-dependent kinase 7 (CDK7)-mediated phosphorylation of the CDK9 activation loop promotes P-TEFb assembly with Tat and proviral HIV reactivation

(2018) Uri Mbonye et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment

(2018) Hetal Patel et al.   MOLECULAR CANCER THERAPEUTICS

CDK8/19 inhibition induces premature G1/S transition and ATR-dependent cell death in prostate cancer cells

(2018) Akito Nakamura et al.   Oncotarget

Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models

(2018) Waleed Minzel et al.   CELL

Phase I dose escalation study of the first-in-class selective PTEFb inhibitor BAY 1251152 in patients with advanced cancer: Novel target validation and early evidence of clinical activity.

(2018) Jennifer Robinson Diamond et al.   JOURNAL OF CLINICAL ONCOLOGY

Structure of paused transcription complex Pol II–DSIF–NELF

(2018) Seychelle M. Vos et al.   NATURE

Selective gene dependencies in MYCN-amplified neuroblastoma include the core transcriptional regulatory circuitry

(2018) Adam D. Durbin et al.   NATURE GENETICS

Targeting CDK9 Reactivates Epigenetically Silenced Genes in Cancer

(2018) Hanghang Zhang et al.   CELL

CDK12 regulates DNA repair genes by suppressing intronic polyadenylation

(2018) Sara J. Dubbury et al.   NATURE

Preclinical Efficacy and Molecular Mechanism of Targeting CDK7-Dependent Transcriptional Addiction in Ovarian Cancer

(2017) Zhenfeng Zhang et al.   MOLECULAR CANCER THERAPEUTICS

Transcription regulation by the Mediator complex

(2017) Julie Soutourina   NATURE REVIEWS MOLECULAR CELL BIOLOGY

CDK12 regulates alternative last exon mRNA splicing and promotes breast cancer cell invasion

(2017) Jerry F. Tien et al.   NUCLEIC ACIDS RESEARCH

Suppression of Adaptive Responses to Targeted Cancer Therapy by Transcriptional Repression

(2017) Maria Rusan et al.   Cancer Discovery

SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains

(2017) Tomasz Rzymski et al.   Oncotarget

Human TFIIH Kinase CDK7 Regulates Transcription-Associated Chromatin Modifications

(2017) Christopher C. Ebmeier et al.   Cell Reports

Activation of the p53 Transcriptional Program Sensitizes Cancer Cells to Cdk7 Inhibitors

(2017) Sampada Kalan et al.   Cell Reports

P-TEFb regulation of transcription termination factor Xrn2 revealed by a chemical genetic screen for Cdk9 substrates

(2016) Miriam Sansó et al.   GENES & DEVELOPMENT

Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors

(2016) Tinghu Zhang et al.   Nature Chemical Biology

Identification of Mediator Kinase Substrates in Human Cells using Cortistatin A and Quantitative Phosphoproteomics

(2016) Zachary C. Poss et al.   Cell Reports

Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases

(2016) Paul A Clarke et al.   eLife

The Molecular Taxonomy of Primary Prostate Cancer

(2015) Adam Abeshouse et al.   CELL

Characterization of Human Cyclin-Dependent Kinase 12 (CDK12) and CDK13 Complexes in C-Terminal Domain Phosphorylation, Gene Transcription, and RNA Processing

(2015) Kaiwei Liang et al.   MOLECULAR AND CELLULAR BIOLOGY

THZ1 Reveals Roles for Cdk7 in Co-transcriptional Capping and Pausing

(2015) Kyle A. Nilson et al.   MOLECULAR CELL

Mediator kinase inhibition further activates super-enhancer-associated genes in AML

(2015) Henry E. Pelish et al.   NATURE

The androgen receptor cistrome is extensively reprogrammed in human prostate tumorigenesis

(2015) Mark M Pomerantz et al.   NATURE GENETICS

The history and future of targeting cyclin-dependent kinases in cancer therapy

(2015) Uzma Asghar et al.   NATURE REVIEWS DRUG DISCOVERY

CDK9 inhibitors define elongation checkpoints at both ends of RNA polymerase II–transcribed genes

(2015) Clélia Laitem et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

CDK9 inhibitors define elongation checkpoints at both ends of RNA polymerase II–transcribed genes

(2015) Clélia Laitem et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Estimating scenarios for survival time in men starting systemic therapies for castration-resistant prostate cancer: A systematic review of randomised trials

(2014) T.A. West et al.   EUROPEAN JOURNAL OF CANCER

TFIIH Phosphorylation of the Pol II CTD Stimulates Mediator Dissociation from the Preinitiation Complex and Promoter Escape

(2014) Koon Ho Wong et al.   MOLECULAR CELL

Targeting transcription regulation in cancer with a covalent CDK7 inhibitor

(2014) Nicholas Kwiatkowski et al.   NATURE

Cyclin-dependent kinases

(2014) Marcos Malumbres   GENOME BIOLOGY

The RNA Polymerase II Carboxy-Terminal Domain (CTD) Code

(2013) Dirk Eick et al.   CHEMICAL REVIEWS

Cyclin-dependent kinase inhibitor therapy for hematologic malignancies

(2013) Prithviraj Bose et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

CDK10/cyclin M is a protein kinase that controls ETS2 degradation and is deficient in STAR syndrome

(2013) V. J. Guen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Promoter clearance by RNA polymerase II

(2012) Donal S. Luse   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

The RNA polymerase II CTD coordinates transcription and RNA processing

(2012) J.-P. Hsin et al.   GENES & DEVELOPMENT

Cyclin-dependent kinase control of the initiation-to-elongation switch of RNA polymerase II

(2012) Stéphane Larochelle et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Role of Ser7 phosphorylation of the CTD during transcription of snRNA genes

(2012) Sylvain Egloff   RNA Biology

RNAP II CTD Phosphorylated on Threonine-4 Is Required for Histone mRNA 3' End Processing

(2011) J.-P. Hsin et al.   SCIENCE

The phosphorylation of the androgen receptor by TFIIH directs the ubiquitin/proteasome process

(2010) Pierre Chymkowitch et al.   EMBO JOURNAL

CDK9 Regulates AR Promoter Selectivity and Cell Growth through Serine 81 Phosphorylation

(2010) Vicki Gordon et al.   MOLECULAR ENDOCRINOLOGY

The Development of a Selective Cyclin-Dependent Kinase Inhibitor That Shows Antitumor Activity

(2009) S. Ali et al.   CANCER RESEARCH

CDK9 directs H2B monoubiquitination and controls replication-dependent histone mRNA 3′-end processing

(2009) Judith Pirngruber et al.   EMBO REPORTS

“Cotranscriptionality”: The Transcription Elongation Complex as a Nexus for Nuclear Transactions

(2009) Roberto Perales et al.   MOLECULAR CELL

Site-specific Androgen Receptor Serine Phosphorylation Linked to Epidermal Growth Factor-dependent Growth of Castration-recurrent Prostate Cancer

(2008) Liliana A. Ponguta et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Characterization of Cyclin L1 and L2 Interactions with CDK11 and Splicing Factors

(2008) Pascal Loyer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Nucleotide Excision Repair Driven by the Dissociation of CAK from TFIIH

(2008) Frédéric Coin et al.   MOLECULAR CELL