Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors-Reference-Cited by-同舟云学术

Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors

Published:2017-05-09 Issue:10 Volume:60 Page:4386-4402
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

McCoull William¹^ORCID,Abrams Roman D.²,Anderson Erica³,Blades Kevin²,Barton Peter¹,Box Matthew²,Burgess Jonathan²,Byth Kate³,Cao Qing³,Chuaqui Claudio³,Carbajo Rodrigo J.¹,Cheung Tony³,Code Erin³,Ferguson Andrew D.³^ORCID,Fillery Shaun¹,Fuller Nathan O.³,Gangl Eric³,Gao Ning³,Grist Matthew²,Hargreaves David¹,Howard Martin R.¹,Hu Jun³,Kemmitt Paul D.¹,Nelson Jennifer E.²,O’Connell Nichole³,Prince D. Bryan³,Raubo Piotr¹,Rawlins Philip B.¹,Robb Graeme R.¹,Shi Junjie⁴,Waring Michael J.²,Whittaker David²,Wylot Marta¹,Zhu Xiahui³

Affiliation:

1. IMED Oncology and Discovery Sciences, AstraZeneca, 310 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, U.K.

2. IMED Oncology, AstraZeneca, Mereside, Alderley Park, Macclesfield, SK10 4TG, U.K.

3. IMED Oncology and Discovery Sciences, AstraZeneca, Gatehouse Park, Waltham, Massachusetts 02451, United States

4. Pharmaron Beijing Co., Ltd. 6 Taihe Road BDA, Beijing 100176 P. R. China

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.7b00359

Reference25 articles.

1. Roles of BCL6 in normal and transformed germinal center B cells

2. Deregulated BCL6 expression recapitulates the pathogenesis of human diffuse large B cell lymphomas in mice

3. Bcl-6 mediates the germinal center B cell phenotype and lymphomagenesis through transcriptional repression of the DNA-damage sensor ATR

4. Lineage-specific functions of Bcl-6 in immunity and inflammation are mediated by distinct biochemical mechanisms

5. Rationally designed BCL6 inhibitors target activated B cell diffuse large B cell lymphoma

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