K
Ka Hing Che
Researcher at Structural Genomics Consortium
Publications - 7
Citations - 791
Ka Hing Che is an academic researcher from Structural Genomics Consortium. The author has contributed to research in topics: Histone Demethylases & Bromodomain. The author has an hindex of 7, co-authored 7 publications receiving 686 citations. Previous affiliations of Ka Hing Che include University of Cambridge & Wellcome Trust/Cancer Research UK Gurdon Institute.
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Journal ArticleDOI
Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.
Sarah Picaud,Sarah Picaud,Oleg Fedorov,Oleg Fedorov,Angeliki Thanasopoulou,Katharina Leonards,Katherine Louise Jones,Julia Meier,Julia Meier,Heidi Olzscha,Octovia P. Monteiro,Octovia P. Monteiro,Sarah Martin,Sarah Martin,Martin Philpott,Martin Philpott,Anthony Tumber,Anthony Tumber,Panagis Filippakopoulos,Panagis Filippakopoulos,Clarence Yapp,Christopher Wells,Christopher Wells,Ka Hing Che,Andrew J. Bannister,Samuel Robson,Umesh Kumar,Nigel J. Parr,Kevin Lee,Dave Lugo,Philip D. Jeffrey,Simon Taylor,Matteo Vecellio,C. Bountra,Paul Brennan,Paul Brennan,Alison O'Mahony,Sharlene Velichko,Susanne Müller,Susanne Müller,Duncan Hay,Danette L. Daniels,Marjeta Urh,Nicholas B. La Thangue,Tony Kouzarides,Rab K. Prinjha,Jürg Schwaller,Stefan Knapp,Stefan Knapp +48 more
TL;DR: A novel, potent inhibitor targeting CBP/p300 bromodomains that impairs aberrant self-renewal of leukemic cells is reported that provides new opportunities for combinatorial treatment of leukemia and potentially other cancers.
Journal ArticleDOI
Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition
Natalie Hope Theodoulou,Paul Bamborough,Andrew J. Bannister,Isabelle Becher,Rino A. Bit,Ka Hing Che,Chun-wa Chung,Antje Dittmann,Gerard Drewes,David H. Drewry,Laurie J. Gordon,Paola Grandi,Melanie Leveridge,Matthew J Lindon,Anne-Marie Michon,Judit Molnar,Samuel Robson,Nicholas C. O. Tomkinson,Tony Kouzarides,Rab K. Prinjha,Philip G. Humphreys +20 more
TL;DR: I-BRD9 represents the first selective tool compound available to elucidate the cellular phenotype of BRD9 bromodomain inhibition, leading to greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromidomain-containing protein 7 (BRD7).
Journal ArticleDOI
A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases.
Xuelai Luo,Yongxiang Liu,Stefan Kubicek,Stefan Kubicek,Stefan Kubicek,Johanna Myllyharju,Anthony Tumber,S.S. Ng,Ka Hing Che,Jessica D. Podoll,Tom D. Heightman,Udo Oppermann,Stuart L. Schreiber,Stuart L. Schreiber,Xiang Wang +14 more
TL;DR: The characterization of a small-molecule inhibitor of Jumonji C domain-containing histone demethylases is reported, which derives from a structure-based design and preferentially inhibits the subfamily of trimethyl lysine dem methylases.
Journal ArticleDOI
5-Carboxy-8-hydroxyquinoline is a broad spectrum 2-oxoglutarate oxygenase inhibitor which causes iron translocation
Richard J. Hopkinson,Anthony Tumber,Clarence Yapp,Rasheduzzaman Chowdhury,Wei Shen Aik,Ka Hing Che,Xuan Shirley Li,Jan B. L. Kristensen,Oliver N. King,Mun Chiang Chan,Kar Kheng Yeoh,Hwanho Choi,Louise J. Walport,Cyrille C. Thinnes,Jacob T. Bush,Clarisse Lejeune,Anna M. Rydzik,Nathan R. Rose,Eleanor A.L. Bagg,Michael A. McDonough,T. Krojer,Wyatt W. Yue,S.S. Ng,Lars Folke Olsen,Paul Brennan,Udo Oppermann,Susanne Muller-Knapp,Robert J. Klose,Peter J. Ratcliffe,Christopher J. Schofield,Akane Kawamura +30 more
TL;DR: Crystallographic studies on these oxygenases demonstrate that IOX1, but not 4C8HQ, can cause translocation of the active site metal, revealing a rare example of protein ligand-induced metal movement.
Journal ArticleDOI
Linking of 2-oxoglutarate and substrate binding sites enables potent and highly selective inhibition of JmjC histone demethylases.
Esther C. Y. Woon,Anthony Tumber,Akane Kawamura,Lars Hillringhaus,Wei Ge,Nathan R. Rose,Jerome Ma,Mun Chiang Chan,Louise J. Walport,Ka Hing Che,S.S. Ng,Brian D. Marsden,Udo Oppermann,Michael A. McDonough,Christopher J. Schofield +14 more
TL;DR: It is reported that a strategy involving binding to both the 2OG and substrate binding sites leads to selective and potent inhibitors of the JMJD2 subfamily, the largest family of demethylases in the world.