Overview of CDK9 as a target in cancer research

Reduced occurrence of tumor flare with flavopiridol followed by combined flavopiridol and lenalidomide in patients with relapsed chronic lymphocytic leukemia (CLL)

(2015) Kami Maddocks et al.   AMERICAN JOURNAL OF HEMATOLOGY

Discovery of novel indirubin-3′-monoxime derivatives as potent inhibitors against CDK2 and CDK9

(2015) Lei Yan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Final results of EFC6663: A multicenter, international, phase 2 study of alvocidib for patients with fludarabine-refractory chronic lymphocytic leukemia

(2015) Mark C. Lanasa et al.   LEUKEMIA RESEARCH

Discovery of novel 5-fluoro-N2,N4-diphenylpyrimidine-2,4-diamines as potent inhibitors against CDK2 and CDK9

(2015) Jiadi Gao et al.   MedChemComm

P-TEFb, the Super Elongation Complex and Mediator Regulate a Subset of Non-paused Genes during Early Drosophila Embryo Development

(2015) Olle Dahlberg et al.   PLoS Genetics

A novel Cdk9 inhibitor preferentially targets tumor cells and synergizes with fludarabine

(2015) Elisabeth Walsby et al.   Oncotarget

Dinaciclib, a novel CDK inhibitor, demonstrates encouraging single-agent activity in patients with relapsed multiple myeloma

(2014) S. K. Kumar et al.   BLOOD

Clinical study of the novel cyclin-dependent kinase inhibitor dinaciclib in combination with rituximab in relapsed/refractory chronic lymphocytic leukemia patients

(2014) Claire Fabre et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Phase I Study of RGB-286638, A Novel, Multitargeted Cyclin-Dependent Kinase Inhibitor in Patients with Solid Tumors

(2014) D. A. J. van der Biessen et al.   CLINICAL CANCER RESEARCH

Phase I Trial of Bortezomib (PS-341; NSC 681239) and "Nonhybrid" (Bolus) Infusion Schedule of Alvocidib (Flavopiridol; NSC 649890) in Patients with Recurrent or Refractory Indolent B-cell Neoplasms

(2014) B. Holkova et al.   CLINICAL CANCER RESEARCH

In silico design of small molecule inhibitors of CDK9/cyclin T1 interaction

(2014) Jelena Randjelovic et al.   JOURNAL OF MOLECULAR GRAPHICS & MODELLING

The Clinical Trials Transformation Initiative: innovation through collaboration

(2014) Pamela Tenaerts et al.   NATURE REVIEWS DRUG DISCOVERY

Genome-wide dynamics of Pol II elongation and its interplay with promoter proximal pausing, chromatin, and exons

(2014) Iris Jonkers et al.   eLife

Flavopiridol can be safely administered using a pharmacologically derived schedule and demonstrates activity in relapsed and refractory non-Hodgkin's lymphoma

(2013) Jeffrey A. Jones et al.   AMERICAN JOURNAL OF HEMATOLOGY

Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor

(2013) T K Albert et al.   BRITISH JOURNAL OF PHARMACOLOGY

A phase I trial of flavopiridol in relapsed multiple myeloma

(2013) Craig C. Hofmeister et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Clinical and laboratory studies of the novel cyclin-dependent kinase inhibitor dinaciclib (SCH 727965) in acute leukemias

(2013) Ivana Gojo et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Randomized Phase II Trial of the Cyclin-Dependent Kinase Inhibitor Dinaciclib (MK-7965) Versus Capecitabine in Patients With Advanced Breast Cancer

(2013) Monica M. Mita et al.   Clinical Breast Cancer

Potent Antimyeloma Activity of a Novel ERK5/CDK Inhibitor

(2013) S. Alvarez-Fernandez et al.   CLINICAL CANCER RESEARCH

Synthesis, structure–activity relationship and biological evaluation of 2,4,5-trisubstituted pyrimidine CDK inhibitors as potential anti-tumour agents

(2013) Hao Shao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Substituted 4-(Thiazol-5-yl)-2-(phenylamino)pyrimidines Are Highly Active CDK9 Inhibitors: Synthesis, X-ray Crystal Structures, Structure–Activity Relationship, and Anticancer Activities

(2013) Hao Shao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Computational study and peptide inhibitors design for the CDK9 – cyclin T1 complex

(2013) Jelena Randjelović et al.   JOURNAL OF MOLECULAR MODELING

A first-in-human, phase 1, dose-escalation study of dinaciclib, a novel cyclin-dependent kinase inhibitor, administered weekly in subjects with advanced malignancies

(2013) John J Nemunaitis et al.   Journal of Translational Medicine

Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs

(2013) D Cirstea et al.   LEUKEMIA

Cyclophosphamide, alvocidib (flavopiridol), and rituximab, a novel feasible chemoimmunotherapy regimen for patients with high-risk chronic lymphocytic leukemia

(2013) Deborah M. Stephens et al.   LEUKEMIA RESEARCH

Randomized phase 2 study of the cyclin-dependent kinase inhibitor dinaciclib (MK-7965) versus erlotinib in patients with non-small cell lung cancer

(2013) Joe J. Stephenson et al.   LUNG CANCER

Dinaciclib (SCH727965) Inhibits the Unfolded Protein Response through a CDK1- and 5-Dependent Mechanism

(2013) T. K. Nguyen et al.   MOLECULAR CANCER THERAPEUTICS

Phase I trial of the combination of flavopiridol and imatinib mesylate in patients with Bcr-Abl+ hematological malignancies

(2012) Prithviraj Bose et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Effect of aprepitant on the pharmacokinetics of the cyclin-dependent kinase inhibitor dinaciclib in patients with advanced malignancies

(2012) Da Zhang et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Flavopiridol induces phosphorylation of AKT in a human glioblastoma cell line, in contrast to siRNA-mediated silencing of Cdk9: Implications for drug design and development

(2012) Valentina Caracciolo et al.   CELL CYCLE

The Cyclin-Dependent Kinase Inhibitor Flavopiridol Potentiates Doxorubicin Efficacy in Advanced Sarcomas: Preclinical Investigations and Results of a Phase I Dose-Escalation Clinical Trial

(2012) J. J. Luke et al.   CLINICAL CANCER RESEARCH

Perspective of Cyclin-dependent kinase 9 (CDK9) as a Drug Target

(2012) Vladimir Krystof et al.   CURRENT PHARMACEUTICAL DESIGN

A Phase 2 Trial of Flavopiridol (Alvocidib) and Cisplatin in Platin-Resistant Ovarian and Primary Peritoneal Carcinoma: MC0261

(2012) Keith C. Bible et al.   GYNECOLOGIC ONCOLOGY

Randomized phase II study of two schedules of flavopiridol given as timed sequential therapy with cytosine arabinoside and mitoxantrone for adults with newly diagnosed, poor-risk acute myelogenous leukemia

(2012) J. E. Karp et al.   HAEMATOLOGICA

Comparative Structural and Functional Studies of 4-(Thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 Inhibitors Suggest the Basis for Isotype Selectivity

(2012) Alison J. Hole et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effect of Mimetic CDK9 Inhibitors on HIV-1-Activated Transcription

(2012) Rachel Van Duyne et al.   JOURNAL OF MOLECULAR BIOLOGY

Structure-based design of nitrogen-linked macrocyclic kinase inhibitors leading to the clinical candidate SB1317/TG02, a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3)

(2012) Anders Poulsen et al.   JOURNAL OF MOLECULAR MODELING

Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors

(2011) Stuart C. Wilson et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Phase 1 and pharmacokinetic study of bolus-infusion flavopiridol followed by cytosine arabinoside and mitoxantrone for acute leukemias

(2011) J. E. Karp et al.   BLOOD

NPMc+ AML cell line shows differential protein expression and lower sensitivity to DNA-damaging and p53-inducing anticancer compounds

(2011) Qiao Jing Lew et al.   CELL CYCLE

The selective P-TEFb inhibitor CAN508 targets angiogenesis

(2011) Vladimír Kryštof et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

(2011) K C Goh et al.   LEUKEMIA

The cyclin-dependent kinase inhibitor SNS-032 has single agent activity in AML cells and is highly synergistic with cytarabine

(2011) E Walsby et al.   LEUKEMIA

Wogonin and related natural flavones are inhibitors of CDK9 that induce apoptosis in cancer cells by transcriptional suppression of Mcl-1

(2011) G Polier et al.   Cell Death & Disease

A Phase I Study of Flavopiridol in Combination With Gemcitabine and Irinotecan in Patients With Metastatic Cancer

(2010) Houman M. Fekrazad et al.   AMERICAN JOURNAL OF CLINICAL ONCOLOGY-CANCER CLINICAL TRIALS

55K isoform of CDK9 associates with Ku70 and is involved in DNA repair

(2010) Hongbing Liu et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

A phase I clinical trial of FOLFIRI in combination with the pan-cyclin-dependent kinase (CDK) inhibitor flavopiridol

(2010) Mark A. Dickson et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Role of the cyclin-dependent kinase 9-related pathway in mammalian gene expression and human diseases

(2010) Gaetano Romano et al.   CELL CYCLE

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

(2010) Sonja Baumli et al.   CHEMISTRY & BIOLOGY

Phase I evaluation of seliciclib (R-roscovitine), a novel oral cyclin-dependent kinase inhibitor, in patients with advanced malignancies

(2010) Christophe Le Tourneau et al.   EUROPEAN JOURNAL OF CANCER

A dose-finding, pharmacokinetic and pharmacodynamic study of a novel schedule of flavopiridol in patients with advanced solid tumors

(2010) Bhuvaneswari Ramaswamy et al.   INVESTIGATIONAL NEW DRUGS

A phase I pharmacokinetic study of pulse-dose vorinostat with flavopiridol in solid tumors

(2010) Mark Andrew Dickson et al.   INVESTIGATIONAL NEW DRUGS

Phase I and Pharmacologic Study of SNS-032, a Potent and Selective Cdk2, 7, and 9 Inhibitor, in Patients With Advanced Chronic Lymphocytic Leukemia and Multiple Myeloma

(2010) Wei-Gang Tong et al.   JOURNAL OF CLINICAL ONCOLOGY

Dinaciclib (SCH 727965), a Novel and Potent Cyclin-Dependent Kinase Inhibitor

(2010) David Parry et al.   MOLECULAR CANCER THERAPEUTICS

Binding to DNA of the RNA-polymerase II C-terminal domain allows discrimination between Cdk7 and Cdk9 phosphorylation

(2009) G. Lolli   NUCLEIC ACIDS RESEARCH

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

(2008) Sonja Baumli et al.   EMBO JOURNAL

CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases

(2008) K Bettayeb et al.   ONCOGENE

Flavopiridol displays preclinical activity in acute lymphoblastic leukemia

(2007) Kelly M. Jackman et al.   PEDIATRIC BLOOD & CANCER