Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation

RAD1901

(2015) Fiona Garner et al.   ANTI-CANCER DRUGS

Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts

(2015) Andiliy Lai et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2015) Chris De Savi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Emergence of Constitutively Active Estrogen Receptor-  Mutations in Pretreated Advanced Estrogen Receptor-Positive Breast Cancer

(2014) R. Jeselsohn et al.   CLINICAL CANCER RESEARCH

D538G Mutation in Estrogen Receptor- : A Novel Mechanism for Acquired Endocrine Resistance in Breast Cancer

(2013) K. Merenbakh-Lamin et al.   CANCER RESEARCH

Bazedoxifene Exhibits Antiestrogenic Activity in Animal Models of Tamoxifen-Resistant Breast Cancer: Implications for Treatment of Advanced Disease

(2013) S. E. Wardell et al.   CLINICAL CANCER RESEARCH

Rapid parameterization of small molecules using the force field toolkit

(2013) Christopher G. Mayne et al.   JOURNAL OF COMPUTATIONAL CHEMISTRY

ESR1 ligand-binding domain mutations in hormone-resistant breast cancer

(2013) Weiyi Toy et al.   NATURE GENETICS

Activating ESR1 mutations in hormone-resistant metastatic breast cancer

(2013) Dan R Robinson et al.   NATURE GENETICS

Endocrine-Therapy-Resistant ESR1 Variants Revealed by Genomic Characterization of Breast-Cancer-Derived Xenografts

(2013) Shunqiang Li et al.   Cell Reports

Automation of the CHARMM General Force Field (CGenFF) I: Bond Perception and Atom Typing

(2012) K. Vanommeslaeghe et al.   Journal of Chemical Information and Modeling

HDX Workbench: Software for the Analysis of H/D Exchange MS Data

(2012) Bruce D. Pascal et al.   JOURNAL OF THE AMERICAN SOCIETY FOR MASS SPECTROMETRY

Overview of theCCP4 suite and current developments

(2011) Martyn D. Winn et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Exploration of Dimensions of Estrogen Potency

(2011) M. Jeyakumar et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Design and Structure of Stapled Peptides Binding to Estrogen Receptors

(2011) Chris Phillips et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

TmoleX-A graphical user interface for TURBOMOLE

(2010) Claudia Steffen et al.   JOURNAL OF COMPUTATIONAL CHEMISTRY

NFκB selectivity of estrogen receptor ligands revealed by comparative crystallographic analyses

(2008) Kendall W Nettles et al.   Nature Chemical Biology