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Alfred A. Rabow
Researcher at AstraZeneca
Publications - 31
Citations - 1360
Alfred A. Rabow is an academic researcher from AstraZeneca. The author has contributed to research in topics: Bicyclic molecule & Estrogen receptor. The author has an hindex of 18, co-authored 30 publications receiving 1206 citations. Previous affiliations of Alfred A. Rabow include Science Applications International Corporation.
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Journal ArticleDOI
AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models
Hazel M. Weir,Robert Hugh Bradbury,Mandy Lawson,Alfred A. Rabow,David Buttar,Rowena Callis,Jon Curwen,Camila de Almeida,Peter Ballard,Micheal Hulse,Craig S. Donald,Lyman Feron,Galith Karoutchi,Philip A. MacFaul,Thomas A. Moss,Richard A. Norman,Stuart E. Pearson,Michael Tonge,Gareth M. Davies,Graeme Walker,Zena Wilson,Rachel Rowlinson,Steve Powell,Claire Sadler,Graham Richmond,Brendon Ladd,Ermira Pazolli,Anne Marie Mazzola,Celina M. D'Cruz,Chris De Savi +29 more
TL;DR: The pharmacologic evidence showed that AZD9496 is an oral, nonsteroidal, selective estrogen receptor antagonist and downregulator in ER(+ breast cells that could provide meaningful benefit to ER(+) breast cancer patients.
Journal ArticleDOI
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-Fluoro-2-Methylpropyl)-3-Methyl-2, 3,4,9-Tetrahydro-1H-Pyrido[3,4-B]Indol-1-Yl)Phenyl)Acrylic Acid (Azd9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.
Chris De Savi,Robert Hugh Bradbury,Alfred A. Rabow,Richard A. Norman,Camila de Almeida,David M. Andrews,Peter Ballard,David Buttar,Rowena Callis,Gordon S. Currie,Jon Curwen,Christopher D. Davies,Craig S. Donald,Lyman Feron,H. Gingell,Steven C. Glossop,Barry R. Hayter,Syeed Hussain,Galith Karoutchi,Scott G. Lamont,Philip A. MacFaul,Thomas A. Moss,Stuart E. Pearson,Michael Tonge,Graeme Walker,Hazel M. Weir,Zena Wilson +26 more
TL;DR: The discovery of an orally bioavailable selective estrogen receptor downregulator (SERD) with equivalent potency and preclinical pharmacology to the intramuscular SERD fulvestrant is described.
Journal ArticleDOI
Mining the National Cancer Institute's tumor-screening database: identification of compounds with similar cellular activities.
TL;DR: This analysis identified relationships between chemotypes of screened agents and their effect on four major classes of cellular activities: mitosis, nucleic acid synthesis, membrane transport and integrity, and phosphatase- and kinase-mediated cell cycle regulation.
Journal ArticleDOI
AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies
Garrett W. Rhyasen,Maureen Hattersley,Yi Yao,Austin Dulak,Wenxian Wang,Philip Petteruti,Ian L. Dale,Scott Boiko,Tony Cheung,Jingwen Zhang,Shenghua Wen,Lillian Castriotta,Deborah Lawson,Michael Collins,Larry Bao,Miika Ahdesmaki,Graeme Walker,Greg O'Connor,Tammie C. Yeh,Alfred A. Rabow,Jonathan R. Dry,Corinne Reimer,Paul Lyne,Gordon B. Mills,Stephen Fawell,Michael J. Waring,Michael Zinda,Edwin Clark,Huawei Chen +28 more
TL;DR: This study establishes AZD5153 as a highly potent, orally available BET/BRD4 inhibitor and provides a rationale for clinical development in hematologic malignancies.
Journal ArticleDOI
Potent and selective bivalent inhibitors of BET bromodomains
Michael J. Waring,Michael J. Waring,Huawei Chen,Alfred A. Rabow,Graeme Walker,Romel Bobby,Scott Boiko,Rob H. Bradbury,Rowena Callis,Edwin Clark,Ian L. Dale,Danette L. Daniels,Austin Dulak,Liz Flavell,Geoff Holdgate,Thomas A. Jowitt,Alexey Kikhney,Mark S. B. McAlister,Jacqui Méndez,Derek Ogg,Joe Patel,Philip Petteruti,Graeme R. Robb,Matthew B. Robers,Sakina Saif,Natalie Stratton,Dmitri I. Svergun,Wenxian Wang,David Whittaker,David Matthew Wilson,Yi Yao +30 more
TL;DR: The discovery and characterization of probe compound biBET, capable of engaging both bromodomains simultaneously in a bivalent, in cis binding mode, illustrates a novel concept in ligand design-simultaneous targeting of two separate domains with a drug-like small molecule-providing precedent for a potentially more effective paradigm for developing ligands for other multi-domain proteins.