Literature DB >> 30595531

Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML.

Matthias Brand1, Baishan Jiang2, Sophie Bauer1, Katherine A Donovan2, Yanke Liang2, Eric S Wang2, Radosław P Nowak2, Jingting C Yuan3, Tinghu Zhang2, Nicholas Kwiatkowski2, André C Müller1, Eric S Fischer2, Nathanael S Gray4, Georg E Winter5.   

Abstract

The design of selective small molecules is often stymied by similar ligand binding pockets. Here, we report BSJ-03-123, a phthalimide-based degrader that exploits protein-interface determinants to achieve proteome-wide selectivity for the degradation of cyclin-dependent kinase 6 (CDK6). Pharmacologic CDK6 degradation targets a selective dependency of acute myeloid leukemia cells, and transcriptomics and phosphoproteomics profiling of acute degradation of CDK6 enabled dynamic mapping of its immediate role in coordinating signaling and transcription.
Copyright © 2018 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  AML; CDK6; PROTAC; acute myeloid leukemia; molecular pharmacology; phosphoproteomics; selectivity; systems biology; targeted protein degradation; transcriptomics

Mesh：

Substances：

Year:  2018        PMID： 30595531      PMCID： PMC6444916          DOI： 10.1016/j.chembiol.2018.11.006

Source DB:  PubMed          Journal:  Cell Chem Biol        ISSN： 2451-9448            Impact factor:   9.039


  24 in total

Review 1.  CDK6-a review of the past and a glimpse into the future: from cell-cycle control to transcriptional regulation.

Authors:  A-S Tigan; F Bellutti; K Kollmann; G Tebb; V Sexl
Journal:  Oncogene       Date:  2015-10-26       Impact factor: 9.867

2.  DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation.

Authors:  Georg E Winter; Dennis L Buckley; Joshiawa Paulk; Justin M Roberts; Amanda Souza; Sirano Dhe-Paganon; James E Bradner
Journal:  Science       Date:  2015-05-21       Impact factor: 47.728

3.  A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader.

Authors:  Hai-Tsang Huang; Dennis Dobrovolsky; Joshiawa Paulk; Guang Yang; Ellen L Weisberg; Zainab M Doctor; Dennis L Buckley; Joong-Heui Cho; Eunhwa Ko; Jaebong Jang; Kun Shi; Hwan Geun Choi; James D Griffin; Ying Li; Steven P Treon; Eric S Fischer; James E Bradner; Li Tan; Nathanael S Gray
Journal:  Cell Chem Biol       Date:  2017-11-09       Impact factor: 8.116

4.  Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead.

Authors:  Daniel P Bondeson; Blake E Smith; George M Burslem; Alexandru D Buhimschi; John Hines; Saul Jaime-Figueroa; Jing Wang; Brian D Hamman; Alexey Ishchenko; Craig M Crews
Journal:  Cell Chem Biol       Date:  2017-11-09       Impact factor: 8.116

5.  A systematic screen for CDK4/6 substrates links FOXM1 phosphorylation to senescence suppression in cancer cells.

Authors:  Lars Anders; Nan Ke; Per Hydbring; Yoon J Choi; Hans R Widlund; Joel M Chick; Huili Zhai; Marc Vidal; Stephen P Gygi; Pascal Braun; Piotr Sicinski
Journal:  Cancer Cell       Date:  2011-11-15       Impact factor: 31.743

6.  HIPPIE v2.0: enhancing meaningfulness and reliability of protein-protein interaction networks.

Authors:  Gregorio Alanis-Lobato; Miguel A Andrade-Navarro; Martin H Schaefer
Journal:  Nucleic Acids Res       Date:  2016-10-24       Impact factor: 16.971

7.  Computational correction of copy number effect improves specificity of CRISPR-Cas9 essentiality screens in cancer cells.

Authors:  Robin M Meyers; Jordan G Bryan; James M McFarland; Barbara A Weir; Ann E Sizemore; Han Xu; Neekesh V Dharia; Phillip G Montgomery; Glenn S Cowley; Sasha Pantel; Amy Goodale; Yenarae Lee; Levi D Ali; Guozhi Jiang; Rakela Lubonja; William F Harrington; Matthew Strickland; Ting Wu; Derek C Hawes; Victor A Zhivich; Meghan R Wyatt; Zohra Kalani; Jaime J Chang; Michael Okamoto; Kimberly Stegmaier; Todd R Golub; Jesse S Boehm; Francisca Vazquez; David E Root; William C Hahn; Aviad Tsherniak
Journal:  Nat Genet       Date:  2017-10-30       Impact factor: 38.330

8.  Kinase-substrate enrichment analysis provides insights into the heterogeneity of signaling pathway activation in leukemia cells.

Authors:  Pedro Casado; Juan-Carlos Rodriguez-Prados; Sabina C Cosulich; Sylvie Guichard; Bart Vanhaesebroeck; Simon Joel; Pedro R Cutillas
Journal:  Sci Signal       Date:  2013-03-26       Impact factor: 8.192

9.  A kinase-independent function of CDK6 links the cell cycle to tumor angiogenesis.

Authors:  Karoline Kollmann; Gerwin Heller; Christine Schneckenleithner; Wolfgang Warsch; Ruth Scheicher; Rene G Ott; Markus Schäfer; Sabine Fajmann; Michaela Schlederer; Ana-Iris Schiefer; Ursula Reichart; Matthias Mayerhofer; Christoph Hoeller; Sabine Zöchbauer-Müller; Dontscho Kerjaschki; Christoph Bock; Lukas Kenner; Gerald Hoefler; Michael Freissmuth; Anthony R Green; Richard Moriggl; Meinrad Busslinger; Marcos Malumbres; Veronika Sexl
Journal:  Cancer Cell       Date:  2013-08-12       Impact factor: 31.743

Review 10.  Treating cancer with selective CDK4/6 inhibitors.

Authors:  Ben O'Leary; Richard S Finn; Nicholas C Turner
Journal:  Nat Rev Clin Oncol       Date:  2016-03-31       Impact factor: 66.675
View more
  71 in total

Review 1.  Preclinical and Clinical Advances of Targeted Protein Degradation as a Novel Cancer Therapeutic Strategy: An Oncologist Perspective.

Authors:  Xinrui Yang; He Yin; Richard D Kim; Jason B Fleming; Hao Xie
Journal:  Target Oncol       Date:  2020-12-28       Impact factor: 4.493

2.  Selective degradation of CDK6 by a palbociclib based PROTAC.

Authors:  Sandeep Rana; Mourad Bendjennat; Smit Kour; Hannah M King; Smitha Kizhake; Muhammad Zahid; Amarnath Natarajan
Journal:  Bioorg Med Chem Lett       Date:  2019-03-26       Impact factor: 2.823

Review 3.  PROTACs: great opportunities for academia and industry.

Authors:  Xiuyun Sun; Hongying Gao; Yiqing Yang; Ming He; Yue Wu; Yugang Song; Yan Tong; Yu Rao
Journal:  Signal Transduct Target Ther       Date:  2019-12-24

Review 4.  Advances in targeting 'undruggable' transcription factors with small molecules.

Authors:  Matthew J Henley; Angela N Koehler
Journal:  Nat Rev Drug Discov       Date:  2021-05-18       Impact factor: 84.694

5.  Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling.

Authors:  Inchul You; Emily C Erickson; Katherine A Donovan; Nicholas A Eleuteri; Eric S Fischer; Nathanael S Gray; Alex Toker
Journal:  Cell Chem Biol       Date:  2019-12-16       Impact factor: 8.116

6.  Exploiting Ubiquitin Ligases for Induced Target Degradation as an Antiviral Strategy.

Authors:  Rati Verma
Journal:  Adv Exp Med Biol       Date:  2021       Impact factor: 2.622

Review 7.  Proteolysis-targeting chimeras in drug development: A safety perspective.

Authors:  Kevin Moreau; Muireann Coen; Andrew X Zhang; Fiona Pachl; M Paola Castaldi; Goran Dahl; Helen Boyd; Clay Scott; Pete Newham
Journal:  Br J Pharmacol       Date:  2020-02-25       Impact factor: 8.739

Review 8.  Emerging modes-of-action in drug discovery.

Authors:  Eric Valeur; Frank Narjes; Christian Ottmann; Alleyn T Plowright
Journal:  Medchemcomm       Date:  2019-06-25       Impact factor: 3.597

9.  A Nimbolide-Based Kinase Degrader Preferentially Degrades Oncogenic BCR-ABL.

Authors:  Bingqi Tong; Jessica N Spradlin; Luiz F T Novaes; Erika Zhang; Xirui Hu; Malte Moeller; Scott M Brittain; Lynn M McGregor; Jeffrey M McKenna; John A Tallarico; Markus Schirle; Thomas J Maimone; Daniel K Nomura
Journal:  ACS Chem Biol       Date:  2020-06-25       Impact factor: 5.100

10.  Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library.

Authors:  Chelsea E Powell; Guangyan Du; Jianwei Che; Zhixiang He; Katherine A Donovan; Hong Yue; Eric S Wang; Radosław P Nowak; Tinghu Zhang; Eric S Fischer; Nathanael S Gray
Journal:  ACS Chem Biol       Date:  2020-09-28       Impact factor: 5.100
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.