Следене
Kwok-Ho Chan
Kwok-Ho Chan
Investigator, GSK
Потвърден имейл адрес: gsk.com
Заглавие
Позовавания
Позовавания
Година
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
11062017
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
10522015
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
2302018
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
1762021
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
1662014
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
1382018
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
1172020
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
742021
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
622020
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
472018
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
292016
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
142023
Derivatives of 1-[(cyclopentyl or 2-pyrrolidinyl) carbonylaminomethyl]-4-(1, 3-thiazol-5-yl) benzene which are useful for the treatment of proliferative, autoimmune or …
A Ciulli, M Zengerle, KH Chan
WO Patent WO/2016/146,985, 2016
7*2016
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
22019
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, ...
SSRN Electron J, 2022
12022
Enzymes Functional Probes
EL Shiao, MGJ Baud, A Ciulli, KH Chan, M Zengerle
US Patent App. 15/039,350, 2017
2017
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