Literature DB >> 30454768

Activating p53 and Inhibiting Superenhancers to Cure Leukemia.

Brian Ball1, Omar Abdel-Wahab2.   

Abstract

In a recent study, Minzel and colleagues identified a novel series of molecules that inhibit casein kinase 1α (CK1α), CDK7, and CDK9, resulting in p53 activation and preferential inhibition of superenhancer (SE)-driven transcription. This study demonstrates a highly effective therapeutic strategy combining p53 activation with suppression of SEs to promote the cooperative killing of leukemic cells.
Copyright © 2018 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Acute myeloid leukemia; CDK7; CDK9; Casein Kinase 1a; Myelodysplastic Syndromes; P53

Mesh：

Substances：

Year:  2018        PMID： 30454768      PMCID： PMC6614867          DOI： 10.1016/j.tips.2018.10.009

Source DB:  PubMed          Journal:  Trends Pharmacol Sci        ISSN： 0165-6147            Impact factor:   14.819


  9 in total

1.  Phase-separation mechanism for C-terminal hyperphosphorylation of RNA polymerase II.

Authors:  Huasong Lu; Dan Yu; Anders S Hansen; Sourav Ganguly; Rongdiao Liu; Alec Heckert; Xavier Darzacq; Qiang Zhou
Journal:  Nature       Date:  2018-05-30       Impact factor: 49.962

2.  Casein kinase 1α regulates an MDMX intramolecular interaction to stimulate p53 binding.

Authors:  Shaofang Wu; Lihong Chen; Andreas Becker; Ernst Schonbrunn; Jiandong Chen
Journal:  Mol Cell Biol       Date:  2012-10-01       Impact factor: 4.272

3.  Super-enhancers in the control of cell identity and disease.

Authors:  Denes Hnisz; Brian J Abraham; Tong Ihn Lee; Ashley Lau; Violaine Saint-André; Alla A Sigova; Heather A Hoke; Richard A Young
Journal:  Cell       Date:  2013-10-10       Impact factor: 41.582

Review 4.  Kinase inhibitors: the road ahead.

Authors:  Fleur M Ferguson; Nathanael S Gray
Journal:  Nat Rev Drug Discov       Date:  2018-03-16       Impact factor: 84.694

5.  CKIα ablation highlights a critical role for p53 in invasiveness control.

Authors:  Ela Elyada; Ariel Pribluda; Robert E Goldstein; Yael Morgenstern; Guy Brachya; Gady Cojocaru; Irit Snir-Alkalay; Ido Burstain; Rebecca Haffner-Krausz; Steffen Jung; Zoltan Wiener; Kari Alitalo; Moshe Oren; Eli Pikarsky; Yinon Ben-Neriah
Journal:  Nature       Date:  2011-02-17       Impact factor: 49.962

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

Authors:  Waleed Minzel; Avanthika Venkatachalam; Avner Fink; Eric Hung; Guy Brachya; Ido Burstain; Maya Shaham; Amitai Rivlin; Itay Omer; Adar Zinger; Shlomo Elias; Eitan Winter; Paul E Erdman; Robert W Sullivan; Leah Fung; Frank Mercurio; Dansu Li; Joseph Vacca; Nathali Kaushansky; Liran Shlush; Moshe Oren; Ross Levine; Eli Pikarsky; Irit Snir-Alkalay; Yinon Ben-Neriah
Journal:  Cell       Date:  2018-08-23       Impact factor: 41.582

7.  Role of casein kinase 1A1 in the biology and targeted therapy of del(5q) MDS.

Authors:  Rebekka K Schneider; Vera Ademà; Dirk Heckl; Marcus Järås; Mar Mallo; Allegra M Lord; Lisa P Chu; Marie E McConkey; Rafael Kramann; Ann Mullally; Rafael Bejar; Francesc Solé; Benjamin L Ebert
Journal:  Cancer Cell       Date:  2014-09-18       Impact factor: 31.743

8.  Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS.

Authors:  Jan Krönke; Emma C Fink; Paul W Hollenbach; Kyle J MacBeth; Slater N Hurst; Namrata D Udeshi; Philip P Chamberlain; D R Mani; Hon Wah Man; Anita K Gandhi; Tanya Svinkina; Rebekka K Schneider; Marie McConkey; Marcus Järås; Elizabeth Griffiths; Meir Wetzler; Lars Bullinger; Brian E Cathers; Steven A Carr; Rajesh Chopra; Benjamin L Ebert
Journal:  Nature       Date:  2015-07-01       Impact factor: 49.962

Review 9.  Biological functions of casein kinase 1 isoforms and putative roles in tumorigenesis.

Authors:  Birgit Schittek; Tobias Sinnberg
Journal:  Mol Cancer       Date:  2014-10-11       Impact factor: 27.401
  9 in total
  1 in total

Review 1.  PROTACs: great opportunities for academia and industry (an update from 2020 to 2021).

Authors:  Ming He; Chaoguo Cao; Zhihao Ni; Yongbo Liu; Peilu Song; Shuang Hao; Yuna He; Xiuyun Sun; Yu Rao
Journal:  Signal Transduct Target Ther       Date:  2022-06-09
  1 in total

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