Corrigendum: Inhibitor Selectivity for Cyclin‐Dependent Kinase 7: A Structural, Thermodynamic, and Modelling Study

Hazel, Pascale; Kroll, Sebastian H. B.; Bondke, Alexander; Barbazanges, Marion; Patel, Hetal; Fuchter, Matthew J.; Coombes, R. Charles; Ali, Simak; Barrett, Anthony G. M.; Freemont, Paul S.

doi:10.1002/cmdc.201700826

Cited by 4 publications

(2 citation statements)

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“…These CDK4/6 inhibitors are currently being studied in phase I/II trials (NCT03791112, NCT04488107, and NCT04539496). 364 A variety of reversible ATP-competitive inhibitors of other CDK isoforms have been evaluated in the clinic in combination with standard-of-care agents or as monotherapy, such as the CDK2 inhibitors inditinib (AGM-130) 377 and FN-1501, 378 the selective CDK7 inhibitor ICEC0942, 379 the CDK9 inhibitors BAY-1251152, 364 and CYC-065, a second-generation inhibitor of CDK2/5/9. Meanwhile, with the development of modern biotechnology, non-classical CDK inhibitors (allosteric inhibitors, covalent inhibitors, and PROTACS) have laid the foundation for the discovery of a novel generation of selective CDK inhibitors.…”

Section: Btk Inhibitorsmentioning

confidence: 99%

Small molecules in targeted cancer therapy: advances, challenges, and future perspectives

Zhong

Xiong

et al. 2021

Sig Transduct Target Ther

716

490

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Due to the advantages in efficacy and safety compared with traditional chemotherapy drugs, targeted therapeutic drugs have become mainstream cancer treatments. Since the first tyrosine kinase inhibitor imatinib was approved to enter the market by the US Food and Drug Administration (FDA) in 2001, an increasing number of small-molecule targeted drugs have been developed for the treatment of malignancies. By December 2020, 89 small-molecule targeted antitumor drugs have been approved by the US FDA and the National Medical Products Administration (NMPA) of China. Despite great progress, small-molecule targeted anti-cancer drugs still face many challenges, such as a low response rate and drug resistance. To better promote the development of targeted anti-cancer drugs, we conducted a comprehensive review of small-molecule targeted anti-cancer drugs according to the target classification. We present all the approved drugs as well as important drug candidates in clinical trials for each target, discuss the current challenges, and provide insights and perspectives for the research and development of anti-cancer drugs.

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Section: Btk Inhibitorsmentioning

confidence: 99%

Small molecules in targeted cancer therapy: advances, challenges, and future perspectives

Zhong

Xiong

et al. 2021

Sig Transduct Target Ther

716

490

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“…169 The pyrazolopyrimidine derivative samuraciclib (ICEC0942, 42) reversibly binds to the ATP-binding site of CDK7 (IC 50 = 40 nM) and exhibits antiproliferative activity in a range of cancer types, including AML, small cell lung cancer (SCLC), and TNBC (Figure 19). 170,171 The pyrazole [1,5-a] pyrimidine core forms two hydrogen bond interactions with the main chain of Leu83 in the hinge region. The third hydrogen bond forms between the nitrogen atom of the piperidine ring and Asn132; the previous fragment is also in electrostatic contact with Asp145.…”

Section: Launched and Clinical Cdk Inhibitorsmentioning

confidence: 99%

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

et al. 2022

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Herein, we discuss more than 50 cyclin-dependent kinase (CDK) inhibitors that have been approved or have undergone clinical trials and their therapeutic application in multiple cancers. This review discusses the design strategies, structure–activity relationships, and efficacy performances of these selective or nonselective CDK inhibitors. The theoretical basis of early broad-spectrum CDK inhibitors is similar to the scope of chemotherapy, but because their toxicity is greater than the benefit, there is no clinical therapeutic window. The notion that selective CDK inhibitors have a safer therapeutic potential than pan-CDK inhibitors has been widely recognized during the research process. Four CDK4/6 inhibitors have been approved for the treatment of breast cancer or for prophylactic administration during chemotherapy to protect bone marrow and immune system function. Furthermore, the emerging strategies in the field of CDK inhibitors are summarized briefly, and CDKs continue to be widely pursued as emerging anticancer drug targets for drug discovery.

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A review on kinases phosphorylating the carboxyl-terminal domain of RNA polymerase II—Biological functions and inhibitors

Zhang

Huang

et al. 2020

Bioorganic Chemistry

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Corrigendum: Inhibitor Selectivity for Cyclin‐Dependent Kinase 7: A Structural, Thermodynamic, and Modelling Study

Cited by 4 publications

References 0 publications

Small molecules in targeted cancer therapy: advances, challenges, and future perspectives

Small molecules in targeted cancer therapy: advances, challenges, and future perspectives

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

A review on kinases phosphorylating the carboxyl-terminal domain of RNA polymerase II—Biological functions and inhibitors

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