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Efthymios S. Gavriil on Muck Rack

Efthymios S. Gavriil

As seen in: Nature
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Articles

Electrophilic compound screening identifies GPX4-dependent ferroptosis as a senescence vulnerability

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By Mariantonietta D’Ambrosio, Matthew White, Efthymios S. Gavriil, Laura Bousset, Jodie Birch, Aleksandra Gruevska, Emiliano Pasquini, Manuel Colucci, Winnie Fong, Simone Mosole, Aurora Valdata, Dimitris Veroutis, Katie Tyson, Vikas Ranvir, Joaquim Pombo, Sanjay Khadayate, George Young, àlex Montoya, Georgia Roumelioti, Jack Houghton Verified, Jianan Lu, Pavel V. Shliaha, Elena De Vita, Santiago Vernia, Vassilis G. Gorgoulis, Suchira Gallage, Mathias Heikenwalder, Zoe Dare Hall, Andrea Alimonti, Iain A. McNeish, Edward Tate, Jesús Gil, Sandra Prokosch, Aoki Ardisson
| Nature Verified
Abstract Senescent cells drive ageing and age-related pathologies, including cancer. Consequently, senolytics, drugs that selectively kill senescent cells, have broad therapeutic appeal. Here we report a senolytic screen of a library of 10,480 electrophilic compounds. Among 38 identified hits, we found a subset of chloroacetamides with broad senolytic activity. Activity-based protein profiling, coupled with functional assays, identified the glutathione peroxidase GPX4 as a target.
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Identification of Actionable Targeted Protein Degradation Effector Sites through Site-Specific Ligand Incorporation-Induced Proximity (SLIP)

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By Zhangping Xiao, Fangyuan Cao, Xinyue Zhang, Efthymios S. Gavriil
| dx.doi.org
Introduction Click to copy section linkSection link copied! Chemically induced proximity (CIP) is a powerful concept in chemical biology and drug discovery whereby a bifunctional molecule or molecular glue brings two or more biomolecules into close spatial proximity. CIP between suitable effectors and target proteins may lead to diverse outcomes, including degradation, stabilization, inhibition, or activation of the targeted protein.
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