Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation | Zendy

Omer Gilan | Zendy; Inmaculada Rioja | Zendy; Kathy Knezevic | Zendy; Matthew Bell | Zendy; Miriam M. Yeung | Zendy; Nicola Harker | Zendy; Enid Y.N. Lam | Zendy; Chunwa Chung | Zendy; Paul Bamborough | Zendy; M. Petretich | Zendy; Marjeta Urh | Zendy; Stephen J. Atkinson | Zendy; Anna K. Bassil | Zendy; Emma J. Roberts | Zendy; Dane Vassiliadis | Zendy; Marian L. Burr | Zendy; Alex Preston | Zendy; Christopher R. Wellaway | Zendy; Thilo Werner | Zendy; James R. Gray | Zendy; AnneMarie Michon | Zendy; Thomas Gobbetti | Zendy; Vinod Kumar | Zendy; Peter E. Soden | Zendy; Andrea Haynes | Zendy; Johanna Vappiani | Zendy; David F. Tough | Zendy; S. Taylor | Zendy; SarahJane Dawson | Zendy; Marcus Bantscheff | Zendy; Matthew Lindon | Zendy; Gerard Drewes | Zendy; Emmanuel H. Demont | Zendy; Danette L. Daniels | Zendy; Paola Grandi | Zendy; Rab K. Prinjha | Zendy; Mark A. Dawson | Zendy

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Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation

Author(s) -

Omer Gilan,

Inmaculada Rioja,

Kathy Knezevic,

Matthew Bell,

Miriam M. Yeung,

Nicola Harker,

Enid Y.N. Lam,

Chunwa Chung,

Paul Bamborough,

M. Petretich,

Marjeta Urh,

Stephen J. Atkinson,

Anna K. Bassil,

Emma J. Roberts,

Dane Vassiliadis,

Marian L. Burr,

Alex Preston,

Christopher R. Wellaway,

Thilo Werner,

James R. Gray,

AnneMarie Michon,

Thomas Gobbetti,

Vinod Kumar,

Peter E. Soden,

Andrea Haynes,

Johanna Vappiani,

David F. Tough,

S. Taylor,

SarahJane Dawson,

Marcus Bantscheff,

Matthew Lindon,

Gerard Drewes,

Emmanuel H. Demont,

Danette L. Daniels,

Paola Grandi,

Rab K. Prinjha,

Mark A. Dawson

Publication year - 2020

Publication title -

science

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 12.556

H-Index - 1186

eISSN - 1095-9203

pISSN - 0036-8075

DOI - 10.1126/science.aaz8455

Subject(s) - cancer , chemistry , medicine

Bromodomain inhibitors revisited Bromodomain and extraterminal domain (BET) proteins contribute to the pathogenesis of cancer and immune diseases through their effects on transcriptional regulation. BET proteins contain two nearly identical bromodomains, BD1 and BD2, structural modules that have attracted great interest as targets for drug development. First-generation drugs that inhibited both BD1 and BD2 showed promising therapeutic activity in preclinical models but proved to be less efficacious in clinical trials. Gilanet al. took a different approach and designed drugs that selectively inhibited BD1 or BD2 (see the Perspective by Filippakopoulos and Knapp). They found that BD1 and BD2 inhibitors altered gene expression in different ways and that BD2 inhibitors had greater therapeutic activity than BD1 inhibitors in preclinical models of inflammation and autoimmune disease.Science , this issue p.387 ; see also p.367

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