Literature DB >> 31955850

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery.

George M Burslem1, Craig M Crews2.   

Abstract

New biological tools provide new techniques to probe fundamental biological processes. Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which are capable of modulating protein concentrations at a post-translational level by co-opting the ubiquitin-proteasome system. We describe the PROTAC technology and its application to drug discovery and provide examples where PROTACs have enabled novel biological insights. Furthermore, we provide a workflow for PROTAC development and use and discuss the benefits and issues associated with PROTACs. Finally, we compare PROTAC-mediated protein-level modulation with other technologies, such as RNAi and genome editing.
Copyright © 2019 Elsevier Inc. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2020        PMID： 31955850      PMCID： PMC7319047          DOI： 10.1016/j.cell.2019.11.031

Source DB:  PubMed          Journal:  Cell        ISSN： 0092-8674            Impact factor:   41.582


  129 in total

1.  Bortezomib.

Authors:  Andrew Paramore; Simon Frantz
Journal:  Nat Rev Drug Discov       Date:  2003-08       Impact factor: 84.694

Review 2.  Unraveling the crucial roles of Meis1 in leukemogenesis and normal hematopoiesis.

Authors:  Bob Argiropoulos; Eric Yung; R Keith Humphries
Journal:  Genes Dev       Date:  2007-11-15       Impact factor: 11.361

3.  Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation.

Authors:  Philipp Ottis; Momar Toure; Philipp M Cromm; Eunhwa Ko; Jeffrey L Gustafson; Craig M Crews
Journal:  ACS Chem Biol       Date:  2017-09-05       Impact factor: 5.100

4.  Transcription Factors Activate Genes through the Phase-Separation Capacity of Their Activation Domains.

Authors:  Ann Boija; Isaac A Klein; Benjamin R Sabari; Alessandra Dall'Agnese; Eliot L Coffey; Alicia V Zamudio; Charles H Li; Krishna Shrinivas; John C Manteiga; Nancy M Hannett; Brian J Abraham; Lena K Afeyan; Yang E Guo; Jenna K Rimel; Charli B Fant; Jurian Schuijers; Tong Ihn Lee; Dylan J Taatjes; Richard A Young
Journal:  Cell       Date:  2018-11-15       Impact factor: 41.582

5.  Technological innovation leads to fundamental understanding in cell biology.

Authors:  David Botstein
Journal:  Mol Biol Cell       Date:  2010-11-15       Impact factor: 4.138

6.  Delineating the role of cooperativity in the design of potent PROTACs for BTK.

Authors:  Adelajda Zorba; Chuong Nguyen; Yingrong Xu; Jeremy Starr; Kris Borzilleri; James Smith; Hongyao Zhu; Kathleen A Farley; WeiDong Ding; James Schiemer; Xidong Feng; Jeanne S Chang; Daniel P Uccello; Jennifer A Young; Carmen N Garcia-Irrizary; Lara Czabaniuk; Brandon Schuff; Robert Oliver; Justin Montgomery; Matthew M Hayward; Jotham Coe; Jinshan Chen; Mark Niosi; Suman Luthra; Jaymin C Shah; Ayman El-Kattan; Xiayang Qiu; Graham M West; Mark C Noe; Veerabahu Shanmugasundaram; Adam M Gilbert; Matthew F Brown; Matthew F Calabrese
Journal:  Proc Natl Acad Sci U S A       Date:  2018-07-16       Impact factor: 11.205

7.  A pharmacodynamic study of the FLT3 inhibitor KW-2449 yields insight into the basis for clinical response.

Authors:  Keith W Pratz; Jorge Cortes; Gail J Roboz; Niranjan Rao; Omotayo Arowojolu; Adam Stine; Yukimasa Shiotsu; Aiko Shudo; Shiro Akinaga; Donald Small; Judith E Karp; Mark Levis
Journal:  Blood       Date:  2008-11-24       Impact factor: 22.113

8.  Mutant NPM1 Maintains the Leukemic State through HOX Expression.

Authors:  Lorenzo Brunetti; Michael C Gundry; Daniele Sorcini; Anna G Guzman; Yung-Hsin Huang; Raghav Ramabadran; Ilaria Gionfriddo; Federica Mezzasoma; Francesca Milano; Behnam Nabet; Dennis L Buckley; Steven M Kornblau; Charles Y Lin; Paolo Sportoletti; Maria Paola Martelli; Brunangelo Falini; Margaret A Goodell
Journal:  Cancer Cell       Date:  2018-09-10       Impact factor: 31.743

9.  MELK is not necessary for the proliferation of basal-like breast cancer cells.

Authors:  Hai-Tsang Huang; Hyuk-Soo Seo; Tinghu Zhang; Yubao Wang; Baishan Jiang; Qing Li; Dennis L Buckley; Behnam Nabet; Justin M Roberts; Joshiawa Paulk; Shiva Dastjerdi; Georg E Winter; Hilary McLauchlan; Jennifer Moran; James E Bradner; Michael J Eck; Sirano Dhe-Paganon; Jean J Zhao; Nathanael S Gray
Journal:  Elife       Date:  2017-09-19       Impact factor: 8.140

10.  Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma.

Authors:  Gerard L Brien; David Remillard; Junwei Shi; Matthew L Hemming; Jonathon Chabon; Kieran Wynne; Eugène T Dillon; Gerard Cagney; Guido Van Mierlo; Marijke P Baltissen; Michiel Vermeulen; Jun Qi; Stefan Fröhling; Nathanael S Gray; James E Bradner; Christopher R Vakoc; Scott A Armstrong
Journal:  Elife       Date:  2018-11-15       Impact factor: 8.713
View more
  140 in total

1.  A kinetic proofreading model for bispecific protein degraders.

Authors:  Derek W Bartlett; Adam M Gilbert
Journal:  J Pharmacokinet Pharmacodyn       Date:  2020-10-22       Impact factor: 2.745

Review 2.  Emerging New Concepts of Degrader Technologies.

Authors:  Yu Ding; Yiyan Fei; Boxun Lu
Journal:  Trends Pharmacol Sci       Date:  2020-04-23       Impact factor: 14.819

3.  Ligand Design for Cereblon Based Immunomodulatory Therapy.

Authors:  Robert B Kargbo
Journal:  ACS Med Chem Lett       Date:  2020-05-08       Impact factor: 4.345

4.  Discovery of IAP-recruiting BCL-XL PROTACs as potent degraders across multiple cancer cell lines.

Authors:  Xuan Zhang; Yonghan He; Peiyi Zhang; Vivekananda Budamagunta; Dongwen Lv; Dinesh Thummuri; Yang Yang; Jing Pei; Yaxia Yuan; Daohong Zhou; Guangrong Zheng
Journal:  Eur J Med Chem       Date:  2020-05-04       Impact factor: 6.514

Review 5.  Tau: Enabler of diverse brain disorders and target of rapidly evolving therapeutic strategies.

Authors:  Che-Wei Chang; Eric Shao; Lennart Mucke
Journal:  Science       Date:  2021-02-26       Impact factor: 47.728

Review 6.  Chemical strategies to overcome resistance against targeted anticancer therapeutics.

Authors:  Rudolf Pisa; Tarun M Kapoor
Journal:  Nat Chem Biol       Date:  2020-07-21       Impact factor: 15.040

7.  Cereblon Promotes the Ubiquitination and Proteasomal Degradation of Interleukin Enhancer-Binding Factor 2.

Authors:  Qihui Lian; Yuan Gao; Qian Li; Xian He; Xiaogang Jiang; Zhongjian Pu; Guoqiang Xu
Journal:  Protein J       Date:  2020-10-03       Impact factor: 2.371

8.  Scaffold hopping enables direct access to more potent PROTACs with in vivo activity.

Authors:  George M Burslem; Daniel P Bondeson; Craig M Crews
Journal:  Chem Commun (Camb)       Date:  2020-06-23       Impact factor: 6.222

9.  Development of CDK2 and CDK5 Dual Degrader TMX-2172.

Authors:  Mingxing Teng; Jie Jiang; Zhixiang He; Nicholas P Kwiatkowski; Katherine A Donovan; Caitlin E Mills; Chiara Victor; John M Hatcher; Eric S Fischer; Peter K Sorger; Tinghu Zhang; Nathanael S Gray
Journal:  Angew Chem Int Ed Engl       Date:  2020-06-03       Impact factor: 15.336

10.  PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes.

Authors:  Joshua P Smalley; Grace E Adams; Christopher J Millard; Yun Song; James K S Norris; John W R Schwabe; Shaun Michael Cowley; James T Hodgkinson
Journal:  Chem Commun (Camb)       Date:  2020-04-21       Impact factor: 6.222
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.