K
Ko Eunhwa
Researcher at Yale University
Publications - 16
Citations - 1737
Ko Eunhwa is an academic researcher from Yale University. The author has contributed to research in topics: Proteolysis targeting chimera & Active ingredient. The author has an hindex of 6, co-authored 16 publications receiving 1277 citations. Previous affiliations of Ko Eunhwa include Korea Research Institute of Bioscience and Biotechnology.
Papers
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Journal ArticleDOI
Catalytic in vivo protein knockdown by small-molecule PROTACs
Daniel P. Bondeson,Alina Mares,Ian Edward David Smith,Ko Eunhwa,Sebastien Andre Campos,Afjal Hussain Miah,Katie E Mulholland,Natasha Routly,Dennis L. Buckley,Jeffrey L. Gustafson,Nico Zinn,Paola Grandi,Satoko Shimamura,Giovanna Bergamini,Maria Faelth-Savitski,Marcus Bantscheff,Carly S. Cox,Deborah A. Gordon,Ryan R. Willard,John J. Flanagan,Linda N. Casillas,Bartholomew J. Votta,Willem den Besten,Kristoffer Famm,Laurens Kruidenier,Paul S. Carter,John D. Harling,Ian Churcher,Craig M. Crews +28 more
TL;DR: Major improvements to the proteolysis targeting chimeras (PROTACs) method are described, a chemical knockdown strategy in which a heterobifunctional molecule recruits a specific protein target to an E3 ubiquitin ligase, resulting in the target's ubiquitination and degradation.
Journal ArticleDOI
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL
Ashton C. Lai,Momar Toure,Doris Hellerschmied,Jemilat Salami,Saul Jaime-Figueroa,Ko Eunhwa,John Hines,Craig M. Crews +7 more
TL;DR: During the course of their development, it was discovered that the capacity of a PROTAC to induce degradation involves more than just target binding: the identity of the inhibitor warhead and the recruited E3 ligase largely determine the degradation profiles of the compounds.
Journal ArticleDOI
A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader
Hai-Tsang Huang,Dennis Dobrovolsky,Joshiawa Paulk,Guang Yang,Ellen Weisberg,Zainab M. Doctor,Dennis L. Buckley,Cho Joong-Heui,Ko Eunhwa,Jaebong Jang,Kun Shi,Hwan Geun Choi,James D. Griffin,Ying Li,Steven P. Treon,Eric S. Fischer,James E. Bradner,Li Tan,Li Tan,Nathanael S. Gray +19 more
TL;DR: This study designed a multi-kinase degrader by conjugating a highly promiscuous kinase inhibitor with a cereblon-binding ligand, and used quantitative proteomics to discover 28 kinases, including BTK,PTK2, PTK2B, FLT3, AurKA, AURKB, TEC, ULK1, ITK, and nine members of the CDK family, as degradable.
Journal ArticleDOI
Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation.
TL;DR: Evaluating different E3 ubiquitin ligases, engineered in their substrate binding domains to accept a recruiting ligand, found five out of six E3 ligases were found to be amenable to recruitment for target degradation.
Patent
Proteolysis targeting chimera compounds and methods of preparing and using same
TL;DR: In this paper, the authors present novel compounds and methods for preventing or treating diseases associated with and/or caused by overexpression and uncontrolled activation of a tyrosine kinase in a subject in need thereof.