Literature DB >> 23033251

Kinetic template-guided tethering of fragments.

Rebecca H Nonoo1, Alan Armstrong, David J Mann.   

Abstract

Birds of a tether: A tethering strategy for the site-directed discovery of low-molecular-weight fragments that bind weakly to defined protein surfaces is described. A solvent-exposed protein thiol captures acrylamide-modified fragments in a conjugate addition reaction that requires a template to produce a measureable quantity of protein-fragment adduct, which can be rapidly identified by mass spectrometry.
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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Year:  2012        PMID: 23033251     DOI: 10.1002/cmdc.201200404

Source DB:  PubMed          Journal:  ChemMedChem        ISSN: 1860-7179            Impact factor:   3.466


  16 in total

1.  Covalent Tethering of Fragments For Covalent Probe Discovery.

Authors:  Stefan G Kathman; Alexander V Statsyuk
Journal:  Medchemcomm       Date:  2016-01-28       Impact factor: 3.597

2.  Electrophilic fragment-based design of reversible covalent kinase inhibitors.

Authors:  Rand M Miller; Ville O Paavilainen; Shyam Krishnan; Iana M Serafimova; Jack Taunton
Journal:  J Am Chem Soc       Date:  2013-03-29       Impact factor: 15.419

3.  FP Tethering: a screening technique to rapidly identify compounds that disrupt protein-protein interactions.

Authors:  Jean M Lodge; T Justin Rettenmaier; James A Wells; William C Pomerantz; Anna K Mapp
Journal:  Medchemcomm       Date:  2014-03-01       Impact factor: 3.597

4.  Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.

Authors:  Paul A Jackson; John C Widen; Daniel A Harki; Kay M Brummond
Journal:  J Med Chem       Date:  2016-12-20       Impact factor: 7.446

5.  A binding hotspot in Trypanosoma cruzi histidyl-tRNA synthetase revealed by fragment-based crystallographic cocktail screens.

Authors:  Cho Yeow Koh; Latha Kallur Siddaramaiah; Ranae M Ranade; Jasmine Nguyen; Tengyue Jian; Zhongsheng Zhang; J Robert Gillespie; Frederick S Buckner; Christophe L M J Verlinde; Erkang Fan; Wim G J Hol
Journal:  Acta Crystallogr D Biol Crystallogr       Date:  2015-07-31

6.  Quantitative Irreversible Tethering (qIT) for Target-directed Covalent Fragment Screening.

Authors:  Gregory B Craven; Alan Armstrong; David J Mann
Journal:  Bio Protoc       Date:  2020-12-20

7.  Covalent Fragment Screening Identifies Rgl2 RalGEF Cysteine for Targeted Covalent Inhibition of Ral GTPase Activation.

Authors:  Khuchtumur Bum-Erdene; Mona K Ghozayel; David Xu; Samy O Meroueh
Journal:  ChemMedChem       Date:  2022-02-09       Impact factor: 3.540

8.  Mechanism of action of thalassospiramides, a new class of calpain inhibitors.

Authors:  Liang Lu; Michael J Meehan; Shuo Gu; Zhilong Chen; Weipeng Zhang; Gen Zhang; Lingli Liu; Xuhui Huang; Pieter C Dorrestein; Ying Xu; Bradley S Moore; Pei-Yuan Qian
Journal:  Sci Rep       Date:  2015-03-05       Impact factor: 4.379

9.  Proteome-wide covalent ligand discovery in native biological systems.

Authors:  Keriann M Backus; Bruno E Correia; Kenneth M Lum; Stefano Forli; Benjamin D Horning; Gonzalo E González-Páez; Sandip Chatterjee; Bryan R Lanning; John R Teijaro; Arthur J Olson; Dennis W Wolan; Benjamin F Cravatt
Journal:  Nature       Date:  2016-06-15       Impact factor: 49.962

10.  A fragment-based method to discover irreversible covalent inhibitors of cysteine proteases.

Authors:  Stefan G Kathman; Ziyang Xu; Alexander V Statsyuk
Journal:  J Med Chem       Date:  2014-05-28       Impact factor: 7.446

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