F
Fengling Li
Researcher at Structural Genomics Consortium
Publications - 91
Citations - 3997
Fengling Li is an academic researcher from Structural Genomics Consortium. The author has contributed to research in topics: Methyltransferase & Methylation. The author has an hindex of 31, co-authored 79 publications receiving 2951 citations. Previous affiliations of Fengling Li include University of Toronto & University of Papua New Guinea.
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Journal ArticleDOI
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors
Wenyu Yu,Emma J. Chory,Emma J. Chory,Amy K. Wernimont,Wolfram Tempel,Alex Scopton,Alexander J. Federation,Jason J. Marineau,Jun Qi,Dalia Barsyte-Lovejoy,Joanna Yi,Richard Marcellus,Roxana E. Iacob,John R. Engen,Carly Griffin,Ahmed Aman,Erno Wienholds,Fengling Li,Javier Pineda,Javier Pineda,Guillermina Estiu,Tatiana Shatseva,Taraneh Hajian,Rima Al-awar,John E. Dick,Masoud Vedadi,Peter Brown,Cheryl H. Arrowsmith,James E. Bradner,Matthieu Schapira,Matthieu Schapira +30 more
TL;DR: The three-dimensional structure of the protein methyl transferase DOT1L bound to EPZ004777, the first S-adenosylmethionine-competitive inhibitor of a protein methyltransferase with in vivo efficacy, and those of four new analogues reveal remodelling of the catalytic site.
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Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia
Florian Grebien,Masoud Vedadi,Masoud Vedadi,Matthäus Getlik,Roberto Giambruno,Amit Grover,Roberto Avellino,Anna Skucha,Sarah Vittori,Ekaterina Kuznetsova,David Smil,Dalia Barsyte-Lovejoy,Fengling Li,Gennadiy Poda,Gennadiy Poda,Matthieu Schapira,Matthieu Schapira,Hong Wu,Aiping Dong,Guillermo Senisterra,Alexey Stukalov,Kilian Huber,Andreas Schönegger,Richard Marcellus,Martin Bilban,Christoph Bock,Peter Brown,Johannes Zuber,Keiryn L. Bennett,Rima Al-awar,Rima Al-awar,Ruud Delwel,Claus Nerlov,Cheryl H. Arrowsmith,Cheryl H. Arrowsmith,Cheryl H. Arrowsmith,Giulio Superti-Furga +36 more
TL;DR: It is shown that C/EBPα p30, but not the normal p42 isoform, preferentially interacts with Wdr5, a key component of SET/MLL histone-methyltransferase complexes, and OICR-9429 is a novel small-molecule antagonist of the Wdr 5-MLL interaction.
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Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia
Bowen Xu,Doan M. On,Anqi Ma,Trevor Parton,Kyle D. Konze,Samantha G. Pattenden,David F. Allison,Ling Cai,Shira Rockowitz,Shichong Liu,Ying Liu,Fengling Li,Masoud Vedadi,Stephen V. Frye,Benjamin A. Garcia,Deyou Zheng,Jian Jin,Gang Greg Wang +17 more
TL;DR: This study provides the detailed profiling for a set of chemicals to manipulate EZh2 and EZH1 and establishes specific enzymatic inhibition of polycomb repressive complex 2 (PRC2)-EZH2 and PRC2-EzH1 by small-molecule compounds as a novel therapeutics for MLL-rearranged leukemia.
Journal ArticleDOI
A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases
Mohammad S. Eram,Yudao Shen,Magdalena M. Szewczyk,Hong Wu,Guillermo Senisterra,Fengling Li,Kyle V. Butler,H. Uemit Kaniskan,Brandon A. Speed,Carlo C. dela Seña,Aiping Dong,Hong Zeng,Matthieu Schapira,Matthieu Schapira,Peter Brown,Cheryl H. Arrowsmith,Cheryl H. Arrowsmith,Dalia Barsyte-Lovejoy,Jing Liu,Masoud Vedadi,Masoud Vedadi,Jian Jin +21 more
TL;DR: The discovery of a potent, selective, and cell-active inhibitor of human type I PRMTs, MS023, and characterization of this inhibitor in a battery of biochemical, biophysical, and cellular assays are reported.
Journal ArticleDOI
The EED protein–protein interaction inhibitor A-395 inactivates the PRC2 complex
Yupeng He,Sujatha Selvaraju,Michael L. Curtin,Clarissa G. Jakob,Haizhong Zhu,Kenneth M. Comess,Bailin Shaw,Evelyne Lima-Fernandes,Evelyne Lima-Fernandes,Magdalena M. Szewczyk,Dong Cheng,Kelly L Klinge,Huan-Qiu Li,Marina A. Pliushchev,Mikkel Algire,David Maag,Jun Guo,Justin D. Dietrich,Sanjay C. Panchal,Andrew M. Petros,Ramzi F. Sweis,Maricel Torrent,Lance J Bigelow,Guillermo Senisterra,Fengling Li,Steven Kennedy,Qin Wu,Qin Wu,Donald J. Osterling,David Lindley,Wenqing Gao,Scott Galasinski,Dalia Barsyte-Lovejoy,Masoud Vedadi,Masoud Vedadi,Fritz G. Buchanan,Cheryl H. Arrowsmith,Cheryl H. Arrowsmith,Gary G. Chiang,Chaohong Sun,William N. Pappano +40 more
TL;DR: A-395 represents a first-in-class antagonist of PRC2 protein-protein interactions (PPI) for use as a chemical probe to investigate the roles of EED-containing protein complexes.