Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors

Cancer statistics, 2019

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Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

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AR-V7 and Resistance to Enzalutamide and Abiraterone in Prostate Cancer

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An improved ATAC-seq protocol reduces background and enables interrogation of frozen tissues

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Development of a second-generation antiandrogen for treatment of advanced prostate cancer.

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Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

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Cyclin-dependent kinases

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The cellular thermal shift assay for evaluating drug target interactions in cells

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Cdks, cyclins and CKIs: roles beyond cell cycle regulation

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Mediator and RNA polymerase II clusters associate in transcription-dependent condensates

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c-Myc Regulates Transcriptional Pause Release

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Transcriptional Addiction in Cancer

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YY1 Is a Structural Regulator of Enhancer-Promoter Loops

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Getting up to speed with transcription elongation by RNA polymerase II

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Prostate cancer progression after androgen deprivation therapy: mechanisms of castrate resistance and novel therapeutic approaches

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Targeting transcription regulation in cancer with a covalent CDK7 inhibitor

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Pol II phosphorylation regulates a switch between transcriptional and splicing condensates

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Thiol-linked alkylation of RNA to assess expression dynamics

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Thiol-linked alkylation for the metabolic sequencing of RNA

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Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation

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Mechanisms of resistance in castration-resistant prostate cancer (CRPC).

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ChIPmentation: fast, robust, low-input ChIP-seq for histones and transcription factors

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Expression of Androgen Receptor Splice Variants in Prostate Cancer Bone Metastases is Associated with Castration-Resistance and Short Survival

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BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment

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Androgen receptor splice variant-7 expression emerges with castration resistance in prostate cancer

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Strategies toward the Design of Novel and Selective Protein Tyrosine Kinase Inhibitors

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

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SLAM-seq defines direct gene-regulatory functions of the BRD4-MYC axis

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The structure of P‐TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation

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Small molecules of different origins have distinct distributions of structural complexity that correlate with protein-binding profiles

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Transcription control by the ENL YEATS domain in acute leukaemia

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A small molecule that binds Hedgehog and blocks its signaling in human cells

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AZD4573 Is a Highly Selective CDK9 Inhibitor That Suppresses MCL-1 and Induces Apoptosis in Hematologic Cancer Cells

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Distinct structural classes of activating FOXA1 alterations in advanced prostate cancer

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FOXA1 mutations alter pioneering activity, differentiation and prostate cancer phenotypes

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Targeting CDK9 Reactivates Epigenetically Silenced Genes in Cancer

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Methyltrienolone, a specific ligand for cellular androgen receptors

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Use of a Pharmacophore Model for the Design of EGF-R Tyrosine Kinase Inhibitors: 4-(Phenylamino)pyrazolo[3,4-d]pyrimidines

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CDK9-mediated transcription elongation is required for MYC addiction in hepatocellular carcinomaPreprint

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Overview of CDK9 as a target in cancer research

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Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer

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Genome-Wide Promoter Analysis of the SOX4 Transcriptional Network in Prostate Cancer Cells

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Kinase Inhibitor Selectivity Profiling Using Differential Scanning Fluorimetry

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ARv7 Represses Tumor-Suppressor Genes in Castration-Resistant Prostate Cancer

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Phosphorylation of the C-terminal Domain of RNA Polymerase II Plays Central Roles in the Integrated Events of Eucaryotic Gene Expression

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Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype

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Small-molecule targeting of brachyury transcription factor addiction in chordoma

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CDK9 inhibitors in acute myeloid leukemia

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Quantification of experimentally induced nucleotide conversions in high-throughput sequencing datasets

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Androgen receptor phosphorylation: biological context and functional consequences

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TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties

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CDK9: A key player in cancer and other diseases

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Selective Mediator dependence of cell-type-specifying transcription

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Halogen Bonds Form the Basis for Selective P-TEFb Inhibition by DRB

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Stabilization of the Max Homodimer with a Small Molecule Attenuates Myc-Driven Transcription

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A Robust Small-Molecule Microarray Platform for Screening Cell Lysates

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Small Molecule Microarrays Enable the Identification of a Selective, Quadruplex-Binding Inhibitor of MYC Expression

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Small-molecule microarrays as tools in ligand discovery

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Enzalutamide: A Novel Antiandrogen for Patients with Castrate-Resistant Prostate Cancer

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Intrinsic disorder in the androgen receptor: identification, characterisation and drugability

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Persistent androgen receptor addiction in castration-resistant prostate cancer

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Application of a MYC degradation screen identifies sensitivity to CDK9 inhibitors in KRAS-mutant pancreatic cancer

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A Small Molecule That Binds and Inhibits the ETV1 Transcription Factor Oncoprotein

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Preclinical development of G1T38: A novel, potent and selective inhibitor of cyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors

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Cyclin-dependent kinase (CDK) 9 and 4/6 inhibitors in acute myeloid leukemia (AML): a promising therapeutic approach

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Cyclin-Dependent Kinase-9 Is a Therapeutic Target in MYC-Expressing Diffuse Large B-Cell Lymphoma

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Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer

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CDK9 inhibitors selectively target estrogen receptor-positive breast cancer cells through combined inhibition of MYB and MCL-1 expression

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Transcriptional Silencing of MCL-1 Through Cyclin-Dependent Kinase Inhibition in Acute Myeloid Leukemia

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MAFG is a potential therapeutic target to restore chemosensitivity in cisplatin-resistant cancer cells by increasing reactive oxygen species

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Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile

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Antineoplastic effects of selective CDK9 inhibition with atuveciclib on cancer stem-like cells in triple-negative breast cancer

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KLF6 Loss of Function in Human Prostate Cancer Progression Is Implicated in Resistance to Androgen Deprivation

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Real-Time RT-PCR for the Measurement of Prostate-Specific Antigen mRNA Expression in Benign Hyperplasia and Adenocarcinoma of Prostate

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Abstract 5133: TP-1287, an oral prodrug of the cyclin-dependent kinase-9 inhibitor alvocidib

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CT7001, a Novel Orally Bio-Available CDK7 Inhibitor, Is Highly Active in in-Vitro and in-Vivo Models of AML

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Abstract 4421: SY-5609, an orally available selective CDK7 inhibitor demonstrates broad anti-tumor activity in vivo

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Probing Small‐Molecule Microarrays with Tagged Proteins in Cell Lysates

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From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy

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Targeting CDK9 for the Treatment of Glioblastoma

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Addressing Transcriptional Dysregulation in Cancer through CDK9 Inhibition

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Design, synthesis, and biological evaluation of novel 4,4′-bipyridine derivatives acting as CDK9-Cyclin T1 protein-protein interaction inhibitors against triple-negative breast cancer

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Targeting Transcriptional Regulation with a CDK9 Inhibitor Suppresses Growth of Endocrine- and Palbociclib-Resistant ER+ Breast Cancers

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Acute BRCAness induction and AR pathway blockage through CDK12/7/9 degradation enhances PARP inhibitor sensitivity in prostate cancer

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Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B

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CDK9 inhibitors for the treatment of solid tumors

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Targeting MYC-driven lymphoma: lessons learned and future directions

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A patent review of selective CDK9 inhibitors in treating cancer

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Targeting the Heterogeneous Genomic Landscape in Triple-Negative Breast Cancer through Inhibitors of the Transcriptional Machinery

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Targeting cyclin-dependent kinases: From pocket specificity to drug selectivity

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Small-Molecule Approaches to Target Transcription Factors

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Emerging Developments in ETS-Positive Prostate Cancer Therapy

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Discovery of HyT‐Based Degraders of CDK9‐Cyclin T1 Complex

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Functional implications and therapeutic targeting of androgen response elements in prostate cancer

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Choosing Kinase Inhibitors for Androgen Deprivation Therapy-Resistant Prostate Cancer

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Discovery of a highly potent, selective, and stable d-amino acid-containing peptide inhibitor of CDK9/cyclin T1 interaction for the treatment of prostate cancer

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Unravelling the Role of Kinases That Underpin Androgen Signalling in Prostate Cancer

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Emerging target discovery and drug repurposing opportunities in chordoma

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A preclinical platform for assessing antitumor effects and systemic toxicities of cancer drug targets

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Biomimetic black phosphorus nanosheets codeliver CDK9 and BRD4 inhibitors for gastric cancer targeted therapy

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Design and synthesis of CDK9/EZH2 dual-target inhibitors to achieve synergistic antitumor effects

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Targeting the Hippo pathway in Schwann cells ameliorates peripheral nerve degeneration via a polypharmacological mechanism

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Improving the study of RNA dynamics through advances in RNA-seq with metabolic labeling and nucleotide-recoding chemistryPreprint

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A Gene Expression Signature to Predict Nucleotide Excision Repair Defects and Novel Therapeutic Approaches

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Dynamic O-GlcNAcylation and phosphorylation attract and expel proteins from RNA polymerase II to regulate mRNA maturation

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Chemical Probe Discovery for DEAD-Box RNA-Binding Protein DDX21 Using Small-Molecule Microarrays

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Chromatin Regulatory Targets for Anticancer Therapeutics

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Structure–activity insights and molecular modeling approaches of anti-TNBC agents: a comprehensive systematic review

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Small molecule modulators of TOX protein re-invigorate T cell activityPreprint

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Phenotypic screening converges on CDK9 inhibition as a therapeutic strategy in translocation renal cell carcinomaPreprint

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A functional map of CDK-drug interactions at single amino acid resolutionPreprint

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Blocking the Enablers: Selective Inhibition of CDK9 Reins in an Unchecked Master Regulator

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Synthetic Small Molecules in Prostate Cancer Therapeutics

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Synthetic Small Molecules in Prostate Cancer Therapeutics

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Additional file 1 of MC180295 is a highly potent and selective CDK9 inhibitor with preclinical in vitro and in vivo efficacy in cancer

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CDK9 inhibition triggers MT2A-dependent apoptosis in HCC cells

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Structure-Based Drug Design to Identify Potent, Selective, and Orally Available Cyclin-Dependent Kinase 9 Inhibitors for the Treatment of Castration-Resistant Prostate Cancer

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Generalizable Strategies for the Synthesis of Cereblon‐Recruiting PROTAC Prodrugs

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Generalizable Strategies for the Synthesis of Cereblon‐Recruiting PROTAC Prodrugs

Wang, A., Liu, B., Ackerman, E. M., Xiang, Y., Nguyen, H. V. ‐., Jiang, Y., Koehler, A. N., & Johnson, J. A. (2026) · Angewandte Chemie International Edition · doi:10.1002/anie.3238473

A guide to transcriptional cyclin‐dependent kinases in cancer

Devlin, J. R., Kyheröinen, S., & Johnstone, R. W. (2026) · FEBS Journal · doi:10.1111/febs.70731

BindingDB Entry 50023643: Discovery of a highly potent, selective, and stable d-amino acid-containing peptide inhibitor of CDK9/cyclin T1 interaction for the treatment of prostate cancer.

BindingDB (2026) · UC San Diego · doi:10.7270/q25m6bpr

BindingDB Entry 50021951: Targeting cyclin-dependent kinases: From pocket specificity to drug selectivity.

BindingDB (2025) · UC San Diego · doi:10.7270/q2vh5th3

BindingDB Entry 50015017: Changing for the Better: Discovery of the Highly Potent and Selective CDK9 Inhibitor VIP152 Suitable for Once Weekly Intravenous Dosing for the Treatment of Cancer.

BindingDB (2023) · UC San Diego · doi:10.7270/q2k0784n

BindingDB Entry 50017151: Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.

BindingDB (2023) · UC San Diego · doi:10.7270/q2bv7mpd

BindingDB Entry 50022443: Design, synthesis, and biological evaluation of novel 4,4'-bipyridine derivatives acting as CDK9-Cyclin T1 protein-protein interaction inhibitors against triple-negative breast cancer.

BindingDB (2025) · UC San Diego · doi:10.7270/q2d50spj

BindingDB Entry 50016345: Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B.

BindingDB (2023) · UC San Diego · doi:10.7270/q2cz3c5m

BindingDB Entry 50018115: CDK9 inhibitors in cancer research.

BindingDB (2024) · UC San Diego · doi:10.7270/q24b35h7

BindingDB Entry 50020536: Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers.

BindingDB (2024) · UC San Diego · doi:10.7270/q2kp86mc

BindingDB Entry 50021712: Recent Discovery and Development of Inhibitors that Target CDK9 and Their Therapeutic Indications.

BindingDB (2025) · UC San Diego · doi:10.7270/q2tm7gs1

BindingDB Entry 50016285: From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.

BindingDB (2023) · UC San Diego · doi:10.7270/q2sb49qv

Abstract 1771: Targeting oncogenic transcription in prostate cancer with a novel, oral bioavailable, and ultra-selective CDK9 inhibitor

Richters, A., Freeman, D. B., Lee, C. L. L., Kabinger, F., Doyle, S. K., Leifer, B. S., Mikochik, P. J., Jagannathan, S., Koren, J. V., Karlin, K. L., et al. (2020) · Cancer Research · doi:10.1158/1538-7445.am2020-1771

Abstract 616: Transcription-regulating kinases CDK8 and CDK19 as novel therapeutic targets for advanced prostate cancer

Chen, M., Kaza, V., Liang, J., McDermott, M. S. J., & Roninson, I. B. (2014) · Cancer Research · doi:10.1158/1538-7445.am2014-616

Abstract B016: CDK7 inhibition suppresses AR addicted Castration-Resistant Prostate Cancer through MED1 inactivation

Rasool, R. U., Natesan, R., Deng, Q., Aras, S., Lal, P., Posimo, J. M., Palanisamy, N., Narla, G., Den, R. B., Freedman, M. L., et al. (2019) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.targ-19-b016

Targeting CDK9: a promising therapeutic opportunity in prostate cancer

Rahaman, M. H., Kumarasiri, M., Mekonnen, L. B., Yu, M., Diab, S., Albrecht, H., Milne, R. W., & Wang, S. (2016) · Endocrine Related Cancer · doi:10.1530/erc-16-0299 · Cited by 74 · see citing works

CDK7 Inhibition Suppresses Castration-Resistant Prostate Cancer through MED1 Inactivation

Rasool, R. U., Natesan, R., Deng, Q., Aras, S., Lal, P., Effron, S. S., Mitchell-Velasquez, E., Posimo, J. M., Carskadon, S. L., Baca, S. C., et al. (2019) · Cancer Discovery · doi:10.1158/2159-8290.cd-19-0189 · Cited by 116 · see citing works