Chan KH - Search Results

1

Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins.

Bond AG, Craigon C, Chan KH, Testa A, Karapetsas A, Fasimoye R, Macartney T, Blow JJ, Alessi DR, Ciulli A. Bond AG, et al. Among authors: chan kh. J Med Chem. 2021 Oct 28;64(20):15477-15502. doi: 10.1021/acs.jmedchem.1c01532. Epub 2021 Oct 15. J Med Chem. 2021. PMID: 34652918 Free PMC article.

2

Chemical biology. A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes.

Baud MGJ, Lin-Shiao E, Cardote T, Tallant C, Pschibul A, Chan KH, Zengerle M, Garcia JR, Kwan TT, Ferguson FM, Ciulli A. Baud MGJ, et al. Among authors: chan kh. Science. 2014 Oct 31;346(6209):638-641. doi: 10.1126/science.1249830. Epub 2014 Oct 16. Science. 2014. PMID: 25323695 Free PMC article.

3

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4.

Zengerle M, Chan KH, Ciulli A. Zengerle M, et al. Among authors: chan kh. ACS Chem Biol. 2015 Aug 21;10(8):1770-7. doi: 10.1021/acschembio.5b00216. Epub 2015 Jun 16. ACS Chem Biol. 2015. PMID: 26035625 Free PMC article.

4

Chemical genetics approaches for selective intervention in epigenetics.

Runcie AC, Chan KH, Zengerle M, Ciulli A. Runcie AC, et al. Among authors: chan kh. Curr Opin Chem Biol. 2016 Aug;33:186-94. doi: 10.1016/j.cbpa.2016.06.031. Epub 2016 Jul 14. Curr Opin Chem Biol. 2016. PMID: 27423045 Free PMC article. Review.

5

Structural basis of PROTAC cooperative recognition for selective protein degradation.

Gadd MS, Testa A, Lucas X, Chan KH, Chen W, Lamont DJ, Zengerle M, Ciulli A. Gadd MS, et al. Among authors: chan kh. Nat Chem Biol. 2017 May;13(5):514-521. doi: 10.1038/nchembio.2329. Epub 2017 Mar 13. Nat Chem Biol. 2017. PMID: 28288108 Free PMC article.

6

Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds.

Chan KH, Zengerle M, Testa A, Ciulli A. Chan KH, et al. J Med Chem. 2018 Jan 25;61(2):504-513. doi: 10.1021/acs.jmedchem.6b01912. Epub 2017 Jun 22. J Med Chem. 2018. PMID: 28595007 Free PMC article.

7

3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation.

Testa A, Lucas X, Castro GV, Chan KH, Wright JE, Runcie AC, Gadd MS, Harrison WTA, Ko EJ, Fletcher D, Ciulli A. Testa A, et al. Among authors: chan kh. J Am Chem Soc. 2018 Jul 25;140(29):9299-9313. doi: 10.1021/jacs.8b05807. Epub 2018 Jul 12. J Am Chem Soc. 2018. PMID: 29949369 Free PMC article.

8

Targeting Endogenous K-RAS for Degradation through the Affinity-Directed Protein Missile System.

Röth S, Macartney TJ, Konopacka A, Chan KH, Zhou H, Queisser MA, Sapkota GP. Röth S, et al. Among authors: chan kh. Cell Chem Biol. 2020 Sep 17;27(9):1151-1163.e6. doi: 10.1016/j.chembiol.2020.06.012. Epub 2020 Jul 14. Cell Chem Biol. 2020. PMID: 32668202 Free PMC article.

9

Understanding and Improving the Membrane Permeability of VH032-Based PROTACs.

Klein VG, Townsend CE, Testa A, Zengerle M, Maniaci C, Hughes SJ, Chan KH, Ciulli A, Lokey RS. Klein VG, et al. Among authors: chan kh. ACS Med Chem Lett. 2020 Jul 30;11(9):1732-1738. doi: 10.1021/acsmedchemlett.0c00265. eCollection 2020 Sep 10. ACS Med Chem Lett. 2020. PMID: 32939229 Free PMC article.

10

Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity.

Imaide S, Riching KM, Makukhin N, Vetma V, Whitworth C, Hughes SJ, Trainor N, Mahan SD, Murphy N, Cowan AD, Chan KH, Craigon C, Testa A, Maniaci C, Urh M, Daniels DL, Ciulli A. Imaide S, et al. Among authors: chan kh. Nat Chem Biol. 2021 Nov;17(11):1157-1167. doi: 10.1038/s41589-021-00878-4. Epub 2021 Oct 21. Nat Chem Biol. 2021. PMID: 34675414 Free PMC article.

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