This study uses APEX2 proteomics to map the spatiotemporal interactome of the luteinizing hormone receptor (LHR) and identifies novel interactors like RAP2B that modulate receptor signaling and trafficking.

Cell chemical biology · May 1, 2025Peer-reviewedBiochemistry

Structure-guided design and optimization of covalent VHL-targeted sulfonyl fluoride PROTACs

Rishi R. Shah, Elena De Vita, Preethi Soundarya Sathyamurthi, Daniel Conole, Xinyue Zhang, Elliot Fellows, Eleanor R. Dickinson, Carlos Martinez-Fleites, Markus A. Queisser, John D. Harling, Edward W. Tate

This study designs and optimizes covalent VHL-targeted sulfonyl fluoride PROTACs that degrade BRD4 and androgen receptor without linker optimization.

Journal of Medicinal Chemistry · Mar 13, 2024Peer-reviewedMolecular Biology

Chemical Tools for Profiling the Intracellular ADP-ribosylated Proteome

Simeon D. Draganov, Michael Gruet, Daniel Conole, Cristina Domingo Balcells, Alexandros Siskos, Hector C. Keun, Dorian O. Haskard, Edward W. Tate

The paper introduces a chemical tool, 6Yn-Pro, for identifying intracellular ADP-ribosylated proteins through metabolic labeling and chemical proteomics in HEK293T cells.

RSC Chemical Biology · Jan 1, 2024Peer-reviewedSystems Biology

Electrophile scanning by chemical proteomics reveals a potent pan-active DUB probe for investigation of deubiquitinase activity in live cells

Daniel Conole, Fangyuan Cao, Christopher W. am Ende, Liang Xue, Sheila Kantesaria, Dahye Kang, Jun Hong Jin, Dafydd R. Owen, Linda Lohr, Monica Schenone, Jaimeen D. Majmudar, Edward W. Tate

The paper identifies a small molecule DUB probe, IMP-2373, that quantitatively engages multiple DUBs in live cells and demonstrates its use in studying DUB activity changes during MYC deregulation.

bioRxiv · Sep 28, 2022 · PreprintSystems Biology