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Literature DB >> 34778777

Estimating the cooperativity of PROTAC-induced ternary complexes using ¹⁹F NMR displacement assay.

Guilherme Vieira de Castro¹, Alessio Ciulli¹.

Abstract

Cooperativity is an important parameter to understand the ternary complexes formed by protein degraders. We developed fluorine NMR competition binding experiments to determine cooperativity of PROTACs. We show applicability to estimate both positive and negative cooperativity, also with homo-dimerizers, and highlight key features and considerations for optimal assay development. This journal is © The Royal Society of Chemistry.

Entities: Chemical

Year: 2021 PMID： 34778777 PMCID： PMC8528210 DOI： 10.1039/d1md00215e

Source DB: PubMed Journal: RSC Med Chem ISSN： 2632-8682

30 in total

1. Fluorine-NMR competition binding experiments for high-throughput screening of large compound mixtures.

Authors: Claudio Dalvit; Maria Flocco; Marina Veronesi; Brian J Stockman
Journal: Comb Chem High Throughput Screen Date: 2002-12 Impact factor: 1.339

2. A comprehensive mathematical model for three-body binding equilibria.

Authors: Eugene F Douglass; Chad J Miller; Gerson Sparer; Harold Shapiro; David A Spiegel
Journal: J Am Chem Soc Date: 2013-04-16 Impact factor: 15.419

3. Homo-PROTACs for the Chemical Knockdown of Cereblon.

Authors: Christian Steinebach; Stefanie Lindner; Namrata D Udeshi; Deepak C Mani; Hannes Kehm; Simon Köpff; Steven A Carr; Michael Gütschow; Jan Krönke
Journal: ACS Chem Biol Date: 2018-09-05 Impact factor: 5.100

4. Fluorine-NMR experiments for high-throughput screening: theoretical aspects, practical considerations, and range of applicability.

Authors: Claudio Dalvit; Paul E Fagerness; Daneen T A Hadden; Ronald W Sarver; Brian J Stockman
Journal: J Am Chem Soc Date: 2003-06-25 Impact factor: 15.419

5. Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex.

Authors: Dirksen E Bussiere; Lili Xie; Honnappa Srinivas; Wei Shu; Ashley Burke; Celine Be; Junping Zhao; Adarsh Godbole; Dan King; Rajeshri G Karki; Viktor Hornak; Fangmin Xu; Jennifer Cobb; Nathalie Carte; Andreas O Frank; Alexandra Frommlet; Patrick Graff; Mark Knapp; Aleem Fazal; Barun Okram; Songchun Jiang; Pierre-Yves Michellys; Rohan Beckwith; Hans Voshol; Christian Wiesmann; Jonathan M Solomon; Joshiawa Paulk
Journal: Nat Chem Biol Date: 2019-12-09 Impact factor: 15.040

6. Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide.

Authors: Eric S Fischer; Kerstin Böhm; John R Lydeard; Haidi Yang; Michael B Stadler; Simone Cavadini; Jane Nagel; Fabrizio Serluca; Vincent Acker; Gondichatnahalli M Lingaraju; Ritesh B Tichkule; Michael Schebesta; William C Forrester; Markus Schirle; Ulrich Hassiepen; Johannes Ottl; Marc Hild; Rohan E J Beckwith; J Wade Harper; Jeremy L Jenkins; Nicolas H Thomä
Journal: Nature Date: 2014-07-16 Impact factor: 49.962

7. Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds.

Authors: Kwok-Ho Chan; Michael Zengerle; Andrea Testa; Alessio Ciulli
Journal: J Med Chem Date: 2017-06-22 Impact factor: 7.446

Estimating the cooperativity of PROTAC-induced ternary complexes using ¹⁹F NMR displacement assay.

1. Fluorine-NMR competition binding experiments for high-throughput screening of large compound mixtures.

2. A comprehensive mathematical model for three-body binding equilibria.

3. Homo-PROTACs for the Chemical Knockdown of Cereblon.

4. Fluorine-NMR experiments for high-throughput screening: theoretical aspects, practical considerations, and range of applicability.

5. Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex.

6. Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide.

7. Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds.

8. Structural basis of PROTAC cooperative recognition for selective protein degradation.

9. Native Mass Spectrometry Can Effectively Predict PROTAC Efficacy.

10. Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation.

Review 1. Allostery: Allosteric Cancer Drivers and Innovative Allosteric Drugs.