Structural basis of PROTAC cooperative recognition for selective protein degradation MS Gadd, A Testa, X Lucas, KH Chan, W Chen, DJ Lamont, M Zengerle, ... Nature chemical biology 13 (5), 514-521, 2017 | 1059 | 2017 |
Selective small molecule induced degradation of the BET bromodomain protein BRD4 M Zengerle, KH Chan, A Ciulli ACS chemical biology 10 (8), 1770-1777, 2015 | 1031 | 2015 |
Impact of target warhead and linkage vector on inducing protein degradation: comparison of bromodomain and extra-terminal (BET) degraders derived from triazolodiazepine (JQ1 … KH Chan, M Zengerle, A Testa, A Ciulli Journal of medicinal chemistry 61 (2), 504-513, 2018 | 230 | 2018 |
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity S Imaide, KM Riching, N Makukhin, V Vetma, C Whitworth, SJ Hughes, ... Nature chemical biology 17 (11), 1157-1167, 2021 | 168 | 2021 |
A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes MGJ Baud, E Lin-Shiao, T Cardote, C Tallant, A Pschibul, KH Chan, ... Science 346 (6209), 638-641, 2014 | 162 | 2014 |
3-Fluoro-4-hydroxyprolines: synthesis, conformational analysis, and stereoselective recognition by the VHL E3 ubiquitin ligase for targeted protein degradation A Testa, X Lucas, GV Castro, KH Chan, JE Wright, AC Runcie, MS Gadd, ... Journal of the American Chemical Society 140 (29), 9299-9313, 2018 | 137 | 2018 |
Understanding and improving the membrane permeability of VH032-based PROTACs VG Klein, CE Townsend, A Testa, M Zengerle, C Maniaci, SJ Hughes, ... ACS medicinal chemistry letters 11 (9), 1732-1738, 2020 | 113 | 2020 |
Development of BromoTag: a “Bump-and-Hole”–PROTAC system to induce potent, rapid, and selective degradation of tagged target proteins AG Bond, C Craigon, KH Chan, A Testa, A Karapetsas, R Fasimoye, ... Journal of Medicinal Chemistry 64 (20), 15477-15502, 2021 | 70 | 2021 |
Targeting endogenous K-RAS for degradation through the affinity-directed protein missile system S Röth, TJ Macartney, A Konopacka, KH Chan, H Zhou, MA Queisser, ... Cell Chemical Biology 27 (9), 1151-1163. e6, 2020 | 59 | 2020 |
Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition AC Runcie, M Zengerle, KH Chan, A Testa, L Van Beurden, MGJ Baud, ... Chemical Science 9 (9), 2452-2468, 2018 | 45 | 2018 |
Chemical genetics approaches for selective intervention in epigenetics AC Runcie, KH Chan, M Zengerle, A Ciulli Current Opinion in Chemical Biology 33, 186-194, 2016 | 28 | 2016 |
Identification of KLHDC2 as an efficient proximity-induced degrader of K-RAS, STK33, β-catenin, and FoxP3 S Röth, NM Kocaturk, PS Sathyamurthi, B Carton, M Watt, TJ Macartney, ... Cell Chemical Biology 30 (10), 1261-1276. e7, 2023 | 12 | 2023 |
Derivatives of 1-[(cyclopentyl or 2-pyrrolidinyl) carbonylaminomethyl]-4-(l, 3-thiazol-5-yl) benzene which are useful for the treatment of proliferative, autoimmune or … A Ciulli, M Zengerle, KH Chan US Patent 11,179,373, 2021 | 3 | 2021 |
Correction to “3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation” A Testa, X Lucas, GV Castro, KH Chan, JE Wright, AC Runcie, MS Gadd, ... Journal of the American Chemical Society 141 (18), 7644-7644, 2019 | 2 | 2019 |
Screening of E3 ligases uncovers KLHDC2 as an efficient proximity-induced degrader of K-RAS, STK33, β-catenin and FoxP3 S Röth, B Carton, PS Sathyamurthi, M Watt, TJ Macartney, KH Chan, ... STK33, β-catenin and FoxP3, 2022 | 1 | 2022 |
Enzymes Functional Probes EL Shiao, MGJ Baud, A Ciulli, KH Chan, M Zengerle US Patent App. 15/039,350, 2017 | | 2017 |