Design, Synthesis and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time

Avinash Khanna,Alexandre Cote,Shilpi Arora,Ludivine Moine,Victor S. Gehling,Jehrod Brenneman,Nico Cantone,Jacob I. Stuckey,Shruti Apte,Ashwin Ramakrishnan,Kamil Bruderek,William D. Bradley,James E. Audia,Richard T. Cummings,Robert J. Sims,Patrick Trojer,Julian Levell

Design, Synthesis and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time

2020

Avinash Khanna
Alexandre Cote
Shilpi Arora
Ludivine Moine
Victor S. Gehling
Jehrod Brenneman
Nico Cantone
Jacob I. Stuckey
Shruti Apte
Ashwin Ramakrishnan
Kamil Bruderek
William D. Bradley
James E. Audia
Richard T. Cummings
Robert J. Sims
Patrick Trojer
Julian Levell

Histone methyltransferase EZH2, which is the catalytic subunit of the PRC2 complex, catalyzes the methylation of histone H3K27 - a transcriptionally repressive post-translational modification (PTM)...

Keywords:

PRC2 complex
Histone methyltransferase
Protein subunit
Biology
Residence time
Histone
Biochemistry
EZH2
design synthesis
Methylation

Correction
Source
Cite
Save
Machine Reading By IdeaReader

References

Citations