Literature DB >> 30672516

PROTAC-mediated crosstalk between E3 ligases.

Christian Steinebach1, Hannes Kehm, Stefanie Lindner, Lan Phuong Vu, Simon Köpff, Álvaro López Mármol, Corinna Weiler, Karl G Wagner, Michaela Reichenzeller, Jan Krönke, Michael Gütschow.   

Abstract

Small-molecule heterobifunctional degraders can effectively control protein levels and are useful research tools. We assembled proteolysis targeting chimeras (PROTACs) from a cereblon (CRBN) and a von-Hippel-Lindau (VHL) ligase ligand and demonstrated a PROTAC-induced heterodimerization of the two E3 ligases leading to unidirectional and efficient degradation of CRBN.

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Year:  2019        PMID： 30672516     DOI： 10.1039/c8cc09541h

Source DB:  PubMed          Journal:  Chem Commun (Camb)        ISSN： 1359-7345            Impact factor:   6.222


  23 in total

1.  A MedChem toolbox for cereblon-directed PROTACs.

Authors:  Christian Steinebach; Izidor Sosič; Stefanie Lindner; Aleša Bricelj; Franziska Kohl; Yuen Lam Dora Ng; Marius Monschke; Karl G Wagner; Jan Krönke; Michael Gütschow
Journal:  Medchemcomm       Date:  2019-05-28       Impact factor: 3.597

Review 2.  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

3.  On the correlation of cereblon binding, fluorination and antiangiogenic properties of immunomodulatory drugs.

Authors:  Christopher Heim; Samuel Maiwald; Christian Steinebach; Matthew K Collins; Jonathan Strope; Cindy H Chau; William D Figg; Michael Gütschow; Marcus D Hartmann
Journal:  Biochem Biophys Res Commun       Date:  2020-12-10       Impact factor: 3.575

Review 4.  Targeted protein degradation: elements of PROTAC design.

Authors:  Stacey-Lynn Paiva; Craig M Crews
Journal:  Curr Opin Chem Biol       Date:  2019-04-17       Impact factor: 8.822

5.  Encoding BRAF inhibitor functions in protein degraders.

Authors:  Daniel S J Miller; Sabine A Voell; Izidor Sosič; Matic Proj; Olivia W Rossanese; Gregor Schnakenburg; Michael Gütschow; Ian Collins; Christian Steinebach
Journal:  RSC Med Chem       Date:  2022-05-05

6.  Selective degradation-inducing probes for studying cereblon (CRBN) biology.

Authors:  Chelsea E Powell; Guangyan Du; Jonathan W Bushman; Zhixiang He; Tinghu Zhang; Eric S Fischer; Nathanael S Gray
Journal:  RSC Med Chem       Date:  2021-07-06

Review 7.  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

8.  Traceless Staudinger ligation enabled parallel synthesis of proteolysis targeting chimera linker variants.

Authors:  Troy A Bemis; James J La Clair; Michael D Burkart
Journal:  Chem Commun (Camb)       Date:  2021-01-06       Impact factor: 6.222

9.  AZD5438-PROTAC: A selective CDK2 degrader that protects against cisplatin- and noise-induced hearing loss.

Authors:  Santanu Hati; Marisa Zallocchi; Robert Hazlitt; Yuju Li; Sarath Vijayakumar; Jaeki Min; Zoran Rankovic; Sándor Lovas; Jian Zuo
Journal:  Eur J Med Chem       Date:  2021-09-20       Impact factor: 6.514

10.  Homo-PROTAC mediated suicide of MDM2 to treat non-small cell lung cancer.

Authors:  Shipeng He; Junhui Ma; Yuxin Fang; Ying Liu; Shanchao Wu; Guoqiang Dong; Wei Wang; Chunquan Sheng
Journal:  Acta Pharm Sin B       Date:  2020-12-02       Impact factor: 11.413
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