A patent review of cyclin-dependent kinase 7 (CDK7) inhibitors (2018-2022)

Synergistic Anti-Tumor Effect of Combining Selective CDK7 and BRD4 Inhibition in Neuroblastoma

(2022) Yang Gao et al.   Frontiers in Oncology

A phase 1 dose-escalation and expansion-cohort study of the oral CDK7 inhibitor XL102 as a single-agent and in combination therapy in patients (pts) with advanced solid tumors.

(2022) Geoffrey Shapiro et al.   JOURNAL OF CLINICAL ONCOLOGY

Antileukemic activity of YPN-005, a CDK7 inhibitor, inducing apoptosis through c-MYC and FLT3 suppression in acute myeloid leukemia

(2022) Bon-Kwan Koo et al.   Heliyon

Discovery of Potent Inhibitors of Cyclin‐Dependent Kinases 7 and 9: Design, Synthesis, Structure‐Activity Relationship Analysis and Biological Evaluation

(2022) Renjie Chen et al.   ChemMedChem

Discovery of Novel N-(5-(Pyridin-3-yl)-1H-indazol-3-yl)benzamide Derivatives as Potent Cyclin-Dependent Kinase 7 Inhibitors for the Treatment of Autosomal Dominant Polycystic Kidney Disease

(2022) Bowen Yang et al.   Journal of Medicinal Chemistry

Targeting CDK7 in oncology: The avenue forward

(2022) Zhi-Mei Li et al.   PHARMACOLOGY & THERAPEUTICS

2.5Å-resolution structure of the human CDK-activating kinase bound to the clinical inhibitor ICEC0942

(2021) Basil J. Greber et al.   BIOPHYSICAL JOURNAL

265P Study of samuraciclib (CT7001), a first-in-class, oral, selective inhibitor of CDK7, in combination with fulvestrant in patients with advanced hormone receptor positive HER2 negative breast cancer (HR+BC)

(2021) S.J. Howell et al.   ANNALS OF ONCOLOGY

230MO First in human, modular study of samuraciclib (CT7001), a first-in-class, oral, selective inhibitor of CDK7, in patients with advanced solid malignancies

(2021) M.G. Krebs et al.   ANNALS OF ONCOLOGY

Discovery of a novel CDK7 inhibitor YPN-005 in small cell lung cancer

(2021) Yun Jung Choi et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

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

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

CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?

(2020) Sarah Diab et al.   JOURNAL OF MEDICINAL CHEMISTRY

CDK7 inhibitor THZ1 enhances antiPD-1 therapy efficacy via the p38α/MYC/PD-L1 signaling in non-small cell lung cancer

(2020) Jian Wang et al.   Journal of Hematology & Oncology

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

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

The cryoelectron microscopy structure of the human CDK-activating kinase

(2020) Basil J. Greber et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Angel or Devil ? - CDK8 as the new drug target

(2020) Dan Wu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Aberrant super‐enhancer landscape in human hepatocellular carcinoma

(2019) Felice Ho‐Ching Tsang et al.   HEPATOLOGY

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

(2019) Shanhu Hu et al.   CANCER RESEARCH

The covalent CDK7 inhibitor THZ1 potently induces apoptosis in multiple myeloma cells in vitro and in vivo

(2019) Yu Zhang et al.   CLINICAL CANCER RESEARCH

Efficacy of the novel CDK7 inhibitor QS1189 in mantle cell lymphoma

(2019) Yun Jung Choi et al.   Scientific Reports

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

(2019) Hua Zhang et al.   CANCER CELL

Recent advances in the development of cyclin-dependent kinase 7 inhibitors

(2019) Yuou Teng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Abstract P1-09-08:BCL2L1(BCL-XL) expression and MYC super-enhancer positivity predict sensitivity to the covalent CDK7 inhibitor SY-1365 in triple negative breast cancer (TNBC) cell lines

(2018) N Rajagopal et al.   CANCER RESEARCH

High MITF Expression Is Associated with Super-Enhancers and Suppressed by CDK7 Inhibition in Melanoma

(2018) Philip Eliades et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

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

(2018) Hetal Patel et al.   MOLECULAR CANCER THERAPEUTICS

Abstract 1525: SY-1365, a selective CDK7 inhibitor, exhibits potent antitumor activity against ovarian cancer models in vitro and in vivo

(2018) Panagiotis A. Konstantinopoulos et al.   CANCER RESEARCH

Abstract 4836: Targeting transcriptional regulation in multiple myeloma with a covalent CDK7 inhibitor THZ1

(2018) Liang Zhou et al.   CANCER RESEARCH

Abstract 4835: UD-017, a novel highly selective and orally active CDK7 inhibitor, shows a significant anticancer activity in patient-derived cancers

(2018) Takashi Matsushita et al.   CANCER RESEARCH

Abstract 4837: Evaluation of anticancer activities of UD-017, a novel selective and orally available CDK7 inhibitor, in blood cancers

(2018) Yasuhiro Aga et al.   CANCER RESEARCH

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

(2018) Waleed Minzel et al.   CELL

Trial design of a first-in-human phase 1 evaluation of SY-1365, a first-in-class selective CDK7 inhibitor, with initial expansions in ovarian and breast cancer.

(2018) Geoffrey Shapiro et al.   JOURNAL OF CLINICAL ONCOLOGY

Overexpression of CDK7 is associated with unfavourable prognosis in oral squamous cell carcinoma

(2018) Lei Jiang et al.   PATHOLOGY

CDK7 inhibition is a novel therapeutic strategy against GBM both in vitro and in vivo

(2018) Wei Meng et al.   Cancer Management and Research

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

(2017) Zhenfeng Zhang et al.   MOLECULAR CANCER THERAPEUTICS

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

(2017) Sampada Kalan et al.   Cell Reports

Upregulation of cyclin-dependent kinase 7 and matrix metalloproteinase-14 expression contribute to metastatic properties of gastric cancer

(2016) Ghodratolah Naseh et al.   IUBMB LIFE

Structural Basis for the Non-catalytic Functions of Protein Kinases

(2016) Jennifer E. Kung et al.   STRUCTURE

Selective CDK7 inhibition with BS-181 suppresses cell proliferation and induces cell cycle arrest and apoptosis in gastric cancer

(2016) Bo-Yong Wang et al.   Drug Design Development and Therapy

CDK7-Dependent Transcriptional Addiction in Triple-Negative Breast Cancer

(2015) Yubao Wang et al.   CELL

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

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

Targeting Transcriptional Addictions in Small Cell Lung Cancer with a Covalent CDK7 Inhibitor

(2014) Camilla L. Christensen et al.   CANCER CELL

CDK7 Inhibition Suppresses Super-Enhancer-Linked Oncogenic Transcription in MYCN-Driven Cancer

(2014) Edmond Chipumuro et al.   CELL

Inhibitors of p21-Activated Kinases (PAKs)

(2014) Joachim Rudolph et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cyclin-Dependent Kinase 7 Controls mRNA Synthesis by Affecting Stability of Preinitiation Complexes, Leading to Altered Gene Expression, Cell Cycle Progression, and Survival of Tumor Cells

(2014) T. W. R. Kelso et al.   MOLECULAR AND CELLULAR BIOLOGY

Targeting transcription regulation in cancer with a covalent CDK7 inhibitor

(2014) Nicholas Kwiatkowski et al.   NATURE

Genetic inactivation of Cdk7 leads to cell cycle arrest and induces premature aging due to adult stem cell exhaustion

(2012) Miguel Ganuza et al.   EMBO JOURNAL

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

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

Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth

(2010) B. W. Murray et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2009) S. Ali et al.   CANCER RESEARCH

TFIIH Kinase Places Bivalent Marks on the Carboxy-Terminal Domain of RNA Polymerase II

(2009) Md. Sohail Akhtar et al.   MOLECULAR CELL

Mammalian cell-cycle regulation: several Cdks, numerous cyclins and diverse compensatory mechanisms

(2009) A Satyanarayana et al.   ONCOGENE