Literature DB >> 30601480

Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC).

S Krajcovicova1, R Jorda, D Hendrychova, V Krystof, M Soural.   

Abstract

A preloaded resin consisting of a thalidomide moiety and an ethylene-oxy linker allows the simple and fast formation of PROTACs. The feasibility of the procedure was illustrated by conjugating different protein kinase inhibitors. The biological functionality of an ibrutinib-like conjugate was then confirmed by a cellular experiment.

Entities:  

Year:  2019        PMID： 30601480     DOI： 10.1039/c8cc08716d

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


  9 in total

Review 1.  Major Advances in Emerging Degrader Technologies.

Authors:  Hang Luo; Li Wu; Yujian He; Chong Qin; Xinjing Tang
Journal:  Front Cell Dev Biol       Date:  2022-06-22

2.  Development of Rapid and Facile Solid-Phase Synthesis of PROTACs via a Variety of Binding Styles.

Authors:  Hanqiao Xu; Takashi Kurohara; Reina Takano; Hidetomo Yokoo; Norihito Shibata; Nobumichi Ohoka; Takao Inoue; Mikihiko Naito; Yosuke Demizu
Journal:  ChemistryOpen       Date:  2022-07       Impact factor: 2.630

3.  A platform for the rapid synthesis of proteolysis targeting chimeras (Rapid-TAC) under miniaturized conditions.

Authors:  Le Guo; Yaxian Zhou; Xueqing Nie; Zhongrui Zhang; Zhen Zhang; Chunrong Li; Taobo Wang; Weiping Tang
Journal:  Eur J Med Chem       Date:  2022-04-01       Impact factor: 7.088

4.  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

5.  Proteolysis Targeting Chimeras for BTK Efficiently Inhibit B-Cell Receptor Signaling and Can Overcome Ibrutinib Resistance in CLL Cells.

Authors:  Yamit Shorer Arbel; Ben-Zion Katz; Ronen Gabizon; Amit Shraga; Yotam Bronstein; Talia Kamdjou; Anat Globerson Levin; Chava Perry; Irit Avivi; Nir London; Yair Herishanu
Journal:  Front Oncol       Date:  2021-05-13       Impact factor: 6.244

6.  Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs.

Authors:  Ronen Gabizon; Amit Shraga; Paul Gehrtz; Ella Livnah; Yamit Shorer; Neta Gurwicz; Liat Avram; Tamar Unger; Hila Aharoni; Shira Albeck; Alexander Brandis; Ziv Shulman; Ben-Zion Katz; Yair Herishanu; Nir London
Journal:  J Am Chem Soc       Date:  2020-05-19       Impact factor: 15.419

7.  Site-Specific Labeling of Endogenous Proteins Using CoLDR Chemistry.

Authors:  Rambabu N Reddi; Adi Rogel; Efrat Resnick; Ronen Gabizon; Pragati Kishore Prasad; Neta Gurwicz; Haim Barr; Ziv Shulman; Nir London
Journal:  J Am Chem Soc       Date:  2021-11-24       Impact factor: 15.419

Review 8.  Degradation of proteins by PROTACs and other strategies.

Authors:  Yang Wang; Xueyang Jiang; Feng Feng; Wenyuan Liu; Haopeng Sun
Journal:  Acta Pharm Sin B       Date:  2019-08-13       Impact factor: 11.413

9.  PRosettaC: Rosetta Based Modeling of PROTAC Mediated Ternary Complexes.

Authors:  Daniel Zaidman; Jaime Prilusky; Nir London
Journal:  J Chem Inf Model       Date:  2020-10-06       Impact factor: 4.956
  9 in total

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