(Q39785596)

14 September 2017

Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2 (English)

1 reference

14 September 2017

10

Patrick Trojer

1 reference

14 September 2017

Christopher G Nasveschuk

1

1 reference

14 September 2017

Alexandre Gagnon

2

1 reference

14 September 2017

Shivani Garapaty-Rao

3

1 reference

14 September 2017

Srividya Balasubramanian

4

1 reference

14 September 2017

Robert Campbell

5

1 reference

14 September 2017

Christina Lee

6

1 reference

14 September 2017

Feng Zhao

7

1 reference

14 September 2017

Louise Bergeron

8

1 reference

14 September 2017

Richard Cummings

9

1 reference

14 September 2017

James E Audia

11

1 reference

14 September 2017

Brian K Albrecht

12

1 reference

14 September 2017

Jean-Christophe P Harmange

13

1 reference

14 September 2017

14 January 2014

1 reference

ACS Medicinal Chemistry Letters

14 September 2017

1 reference

14 September 2017

5

1 reference

14 September 2017

4

1 reference

14 September 2017

378-383

1 reference

Improving the plausibility of success with inefficient metrics

14 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

Identification of EZH2 and EZH1 small molecule inhibitors with selective impact on diffuse large B cell lymphoma cell growth

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

The Polycomb complex PRC2 and its mark in life

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

Somatic mutations at EZH2 Y641 act dominantly through a mechanism of selectively altered PRC2 catalytic activity, to increase H3K27 trimethylation

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

Small molecule conformational preferences derived from crystal structure data. A medicinal chemistry focused analysis

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

The road map to oral bioavailability: an industrial perspective

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

EZH2 is a marker of aggressive breast cancer and promotes neoplastic transformation of breast epithelial cells

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

The polycomb group protein EZH2 is involved in progression of prostate cancer

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens

22 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

Interpreting steep dose-response curves in early inhibitor discovery

17 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4027731

The thermodynamic basis for the use of lipophilic efficiency (LipE) in enthalpic optimizations

20 August 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/24900844

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

A687V EZH2 is a gain-of-function mutation found in lymphoma patients

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/24900844

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1021/ML400494B

1 reference

14 September 2017

1 reference

14 September 2017

1 reference