Dual-function antiandrogen/HDACi hybrids based on enzalutamide and entinostat

Resistance to second-generation androgen receptor antagonists in prostate cancer

(2021) Keith T. Schmidt et al.   Nature Reviews Urology

The Role of Cancer-Associated Fibroblasts in Prostate Cancer Tumorigenesis

(2020) Francesco Bonollo et al.   Cancers

Paradigm Shift of “Classical” HDAC Inhibitors to “Hybrid” HDAC inhibitors in Therapeutic Interventions

(2020) Gargi Nikhil Vaidya et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeting prostate cancer cells with enzalutamide‐HDAC inhibitor hybrid drug 2‐75

(2019) Wen‐Yang Hu et al.   PROSTATE

Genome-wide analysis of androgen receptor binding and transcriptomic analysis in mesenchymal subsets during prostate development

(2019) Claire Nash et al.   Disease Models & Mechanisms

Aminoalkylation of [1.1.1]Propellane Enables Direct Access to High-Value 3-Alkylbicyclo[1.1.1]pentan-1-amines

(2019) Jonathan M. E. Hughes et al.   ORGANIC LETTERS

Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - a new hybrid design paradigm

(2018) Anthony F. Palermo et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Molecular underpinnings of enzalutamide resistance

(2018) Stefan Prekovic et al.   ENDOCRINE-RELATED CANCER

Efficacy of hybrid vitamin D receptor agonist/histone deacetylase inhibitors in vitamin D-resistant triple-negative 4T1 breast cancer

(2018) Krikor Bijian et al.   JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY

Genome-wide analysis of AR binding and comparison with transcript expression in primary human fetal prostate fibroblasts and cancer associated fibroblasts

(2018) Claire Nash et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Structure of the homodimeric androgen receptor ligand-binding domain

(2017) Marta Nadal et al.   Nature Communications

Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors

(2016) Pradeep S. Jadhavar et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting the androgen receptor in metastatic castrate-resistant prostate cancer: A review

(2016) Archana Anantharaman et al.   UROLOGIC ONCOLOGY-SEMINARS AND ORIGINAL INVESTIGATIONS

Optimization of histone deacetylase inhibitor activity in non-secosteroidal vitamin D-receptor agonist hybrids

(2015) Dainis Kaldre et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids

(2015) Rodrigo Mendoza-Sanchez et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Selectively Targeting Prostate Cancer with Antiandrogen Equipped Histone Deacetylase Inhibitors

(2013) Berkley E. Gryder et al.   ACS Chemical Biology

PXD101 potentiates hormonal therapy and prevents the onset of castration-resistant phenotype modulating androgen receptor, HSP90, and CRM1 in preclinical models of prostate cancer

(2013) Giovanni Luca Gravina et al.   ENDOCRINE-RELATED CANCER

Overcoming mutation-based resistance to antiandrogens with rational drug design

(2013) Minna D Balbas et al.   eLife

Synthetically Accessible Non-Secosteroidal Hybrid Molecules Combining Vitamin D Receptor Agonism and Histone Deacetylase Inhibition

(2012) Joshua Fischer et al.   CHEMISTRY & BIOLOGY

The androgen receptor fuels prostate cancer by regulating central metabolism and biosynthesis

(2011) Charles E Massie et al.   EMBO JOURNAL

New Hormonal Therapies for Castration-Resistant Prostate Cancer

(2011) Elahe A. Mostaghel et al.   ENDOCRINOLOGY AND METABOLISM CLINICS OF NORTH AMERICA

Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids

(2010) Marc Lamblin et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides

(2010) Jerome C. Bressi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Ano-Aminoanilide Analogue of 1α,25-Dihydroxyvitamin D3Functions as a Strong Vitamin D Receptor Antagonist

(2010) Marc Lamblin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure−Activity Relationship for Thiohydantoin Androgen Receptor Antagonists for Castration-Resistant Prostate Cancer (CRPC)

(2010) Michael E. Jung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemical phylogenetics of histone deacetylases

(2010) James E Bradner et al.   Nature Chemical Biology

An in vitro model for preclinical testing of endocrine therapy combinations for prostate cancer

(2010) Minja J. Pfeiffer et al.   PROSTATE

Development of Androgen Receptor Antagonists with Promising Activity in Castration-Resistant Prostate Cancer

(2009) Howard C. Shen et al.   CANCER CELL

Histone Deacetylases Are Required for Androgen Receptor Function in Hormone-Sensitive and Castrate-Resistant Prostate Cancer

(2009) D. S. Welsbie et al.   CANCER RESEARCH

Induction of bicalutamide sensitivity in prostate cancer cells by an epigenetic Purα-mediated decrease in androgen receptor levels

(2009) XiaoMei Liu et al.   PROSTATE

Development of a Second-Generation Antiandrogen for Treatment of Advanced Prostate Cancer

(2009) C. Tran et al.   SCIENCE

Defining the molecular action of HDAC inhibitors and synergism with androgen deprivation in ERG-positive prostate cancer

(2008) Mari Björkman et al.   INTERNATIONAL JOURNAL OF CANCER

Histone Deacetylase Inhibitors: From Bench to Clinic

(2008) Marielle Paris et al.   JOURNAL OF MEDICINAL CHEMISTRY

Incorporation of histone deacetylase inhibition into the structure of a nuclear receptor agonist

(2008) L. E. Tavera-Mendoza et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA