Literature DB >> 33632038

Small molecule inhibitors of cyclin-dependent kinase 9 for cancer therapy.

Aisha Alsfouk1.   

Abstract

Cyclin-dependent kinase 9 (CDK9) plays a vital role in transcription through regulation of short-lived anti-apoptotic genes required for cancer cell survival. Therefore, targeting CDK9 with small molecule inhibitors has emerged as a potential cancer therapy. This article reviews the most recent CDK9 patent literature (2012-2020) related to small molecule inhibitors in cancer along with their selectivity profile and biological results in preclinical studies.

Entities:  

Keywords:  CDK9; kinases; proliferative disorders

Mesh:

Substances:

Year:  2021        PMID: 33632038      PMCID: PMC7919902          DOI: 10.1080/14756366.2021.1890726

Source DB:  PubMed          Journal:  J Enzyme Inhib Med Chem        ISSN: 1475-6366            Impact factor:   5.051


  48 in total

1.  Flavopiridol inactivates P-TEFb and blocks most RNA polymerase II transcription in vivo.

Authors:  S H Chao; D H Price
Journal:  J Biol Chem       Date:  2001-06-28       Impact factor: 5.157

2.  CDKI-73: an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia.

Authors:  Muhammed H Rahaman; Yingyi Yu; Longjin Zhong; Julian Adams; Frankie Lam; Peng Li; Ben Noll; Robert Milne; Jun Peng; Shudong Wang
Journal:  Invest New Drugs       Date:  2018-09-08       Impact factor: 3.850

3.  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.

Authors:  Judith E Karp; Elizabeth Garrett-Mayer; Elihu H Estey; Michelle A Rudek; B Douglas Smith; Jacqueline M Greer; D Michelle Drye; Karen Mackey; Kathleen Shannon Dorcy; Steven D Gore; Mark J Levis; Michael A McDevitt; Hetty E Carraway; Keith W Pratz; Douglas E Gladstone; Margaret M Showel; Megan Othus; L Austin Doyle; John J Wright; John M Pagel
Journal:  Haematologica       Date:  2012-06-24       Impact factor: 9.941

4.  MicroRNA-874 inhibits cell proliferation and induces apoptosis in human breast cancer by targeting CDK9.

Authors:  Ling Wang; Wen Gao; Fan Hu; Zhiyang Xu; Fuqiang Wang
Journal:  FEBS Lett       Date:  2014-10-02       Impact factor: 4.124

Review 5.  Targeting CDK9: a promising therapeutic opportunity in prostate cancer.

Authors:  Muhammed H Rahaman; Malika Kumarasiri; Laychiluh B Mekonnen; Mingfeng Yu; Sarah Diab; Hugo Albrecht; Robert W Milne; Shudong Wang
Journal:  Endocr Relat Cancer       Date:  2016-08-31       Impact factor: 5.678

Review 6.  Flavopiridol: the first cyclin-dependent kinase inhibitor in human clinical trials.

Authors:  A M Senderowicz
Journal:  Invest New Drugs       Date:  1999       Impact factor: 3.850

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

Authors:  E Walsby; M Lazenby; C Pepper; A K Burnett
Journal:  Leukemia       Date:  2011-01-07       Impact factor: 11.528

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

Authors:  Sonja Baumli; Graziano Lolli; Edward D Lowe; Sonia Troiani; Luisa Rusconi; Alex N Bullock; Judit E Debreczeni; Stefan Knapp; Louise N Johnson
Journal:  EMBO J       Date:  2008-06-19       Impact factor: 11.598

9.  Phase II study of flavopiridol in relapsed chronic lymphocytic leukemia demonstrating high response rates in genetically high-risk disease.

Authors:  Thomas S Lin; Amy S Ruppert; Amy J Johnson; Beth Fischer; Nyla A Heerema; Leslie A Andritsos; Kristie A Blum; Joseph M Flynn; Jeffrey A Jones; Weihong Hu; Mollie E Moran; Sarah M Mitchell; Lisa L Smith; Amy J Wagner; Chelsey A Raymond; Larry J Schaaf; Mitch A Phelps; Miguel A Villalona-Calero; Michael R Grever; John C Byrd
Journal:  J Clin Oncol       Date:  2009-10-13       Impact factor: 44.544

10.  The novel cyclin-dependent kinase inhibitor dinaciclib (SCH727965) promotes apoptosis and abrogates microenvironmental cytokine protection in chronic lymphocytic leukemia cells.

Authors:  A J Johnson; Y-Y Yeh; L L Smith; A J Wagner; J Hessler; S Gupta; J Flynn; J Jones; X Zhang; R Bannerji; M R Grever; J C Byrd
Journal:  Leukemia       Date:  2012-05-30       Impact factor: 11.528

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  4 in total

1.  Synthesis of Novel 2-Thiouracil-5-Sulfonamide Derivatives as Potent Inducers of Cell Cycle Arrest and CDK2A Inhibition Supported by Molecular Docking.

Authors:  Samar S Fatahala; Amira I Sayed; Shahenda Mahgoub; Heba Taha; Mohamed-I Kotb El-Sayed; Mohamed F El-Shehry; Samir M Awad; Rania H Abd El-Hameed
Journal:  Int J Mol Sci       Date:  2021-11-04       Impact factor: 5.923

2.  Phosphorylated MED1 links transcription recycling and cancer growth.

Authors:  Zhong Chen; Zhenqing Ye; Raymond E Soccio; Tomoyoshi Nakadai; William Hankey; Yue Zhao; Furong Huang; Fuwen Yuan; Hongyan Wang; Zhifen Cui; Benjamin Sunkel; Dayong Wu; Richard K Dzeng; Jennifer M Thomas-Ahner; Tim H M Huang; Steven K Clinton; Jiaoti Huang; Mitchell A Lazar; Victor X Jin; Robert G Roeder; Qianben Wang
Journal:  Nucleic Acids Res       Date:  2022-05-06       Impact factor: 19.160

3.  Synthesis and Biological Evaluation of Imadazo[1,2-a]pyrazines as Anticancer and Antiviral Agents through Inhibition of CDK9 and Human Coronavirus.

Authors:  Aisha A Alsfouk; Hanan M Alshibl; Bshra A Alsfouk; Najla A Altwaijry; Ebtehal S Al-Abdullah
Journal:  Pharmaceuticals (Basel)       Date:  2022-07-13

4.  Corosolic acid inhibits cancer progression by decreasing the level of CDK19-mediated O-GlcNAcylation in liver cancer cells.

Authors:  Congcong Zhang; Yongjie Niu; Zhixian Wang; Xin Xu; Yan Li; Lifang Ma; Jiayi Wang; Yongchun Yu
Journal:  Cell Death Dis       Date:  2021-09-29       Impact factor: 8.469

  4 in total

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