Discovery of an orally active VHL-recruiting PROTAC that achieves robust HMGCR degradation and potent hypolipidemic activity in vivo

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

Heart Disease and Stroke Statistics—2020 Update: A Report From the American Heart Association

(2020) Salim S. Virani et al.   CIRCULATION

PROTACs: A novel strategy for cancer therapy

(2020) Jing Liu et al.   SEMINARS IN CANCER BIOLOGY

Recent Progress in PROTACs and Other Chemical Protein Degradation Technologies for the Treatment of Neurodegenerative Disorders

(2020) Shusuke Tomoshige et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Fundamental aspects of DMPK optimization of targeted protein degraders

(2020) Carina Cantrill et al.   DRUG DISCOVERY TODAY

Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy

(2020) Xin Li et al.   Journal of Hematology & Oncology

Degradation versus Inhibition: Development of Proteolysis-Targeting Chimeras for Overcoming Statin-Induced Compensatory Upregulation of 3-Hydroxy-3-methylglutaryl Coenzyme A Reductase

(2020) Mei-Xin Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics

(2020) Sajid Khan et al.   ONCOGENE

PROTAC Technology: Opportunities and Challenges

(2020) Hongying Gao et al.   ACS Medicinal Chemistry Letters

Targeting post-translational modification of transcription factors as cancer therapy

(2020) Meijia Qian et al.   DRUG DISCOVERY TODAY

Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective

(2020) Andy Pike et al.   DRUG DISCOVERY TODAY

Targeting Estrogen Receptor α for degradation with PROTACs: A Promising Approach to Overcome Endocrine Resistance

(2020) Xin Lin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel PDEδ Degraders for the Treatment of KRAS Mutant Colorectal Cancer

(2020) Junfei Cheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)

(2019) Jiantao Hu et al.   JOURNAL OF MEDICINAL CHEMISTRY

In Silico Modeling of PROTAC-Mediated Ternary Complexes: Validation and Application

(2019) Michael L. Drummond et al.   Journal of Chemical Information and Modeling

Diagnosis and Management of Statin Intolerance

(2019) Rodrigo Alonso et al.   Journal of Atherosclerosis and Thrombosis

Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation

(2019) Lijie Peng et al.   ACS Medicinal Chemistry Letters

PROTACs– a game-changing technology

(2019) Markella Konstantinidou et al.   Expert Opinion on Drug Discovery

Endogenous sterol intermediates of the mevalonate pathway regulate HMGCR degradation and SREBP-2 processing

(2019) Liang Chen et al.   JOURNAL OF LIPID RESEARCH

Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders

(2019) Shang Su et al.   JOURNAL OF MEDICINAL CHEMISTRY

Degradation of proteins by PROTACs and other strategies

(2019) Yang Wang et al.   Acta Pharmaceutica Sinica B

Development of a PDEδ-Targeting PROTACs that Impair Lipid Metabolism

(2019) Michael Winzker et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands

(2019) Xin Han et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein

(2019) Haibin Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Mechanisms and regulation of cholesterol homeostasis

(2019) Jie Luo et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Isoflavones enhance pharmacokinetic exposure of active lovastatin acid via the upregulation of carboxylesterase in high-fat diet mice after oral administration of Xuezhikang capsules

(2018) Dong Feng et al.   ACTA PHARMACOLOGICA SINICA

PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies

(2018) Yonghui Sun et al.   CELL RESEARCH

Emerging Role of Precision Medicine in Cardiovascular Disease

(2018) Jane A. Leopold et al.   CIRCULATION RESEARCH

Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

(2018) Chong Qin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Underlying mechanisms for sterol-induced ubiquitination and ER-associated degradation of HMG CoA reductase

(2018) Brittany M. Johnson et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression

(2018) Yangbing Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a potent HMG-CoA reductase degrader that eliminates statin-induced reductase accumulation and lowers cholesterol

(2018) Shi-You Jiang et al.   Nature Communications

Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1

(2017) Andrew P. Crew et al.   JOURNAL OF MEDICINAL CHEMISTRY

Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?

(2017) Ian Churcher   JOURNAL OF MEDICINAL CHEMISTRY

Targeted protein degradation by PROTACs

(2017) Taavi K. Neklesa et al.   PHARMACOLOGY & THERAPEUTICS

Small-Molecule PROTACS: New Approaches to Protein Degradation

(2016) Momar Toure et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Statins increase hepatic cholesterol synthesis and stimulate fecal cholesterol elimination in mice

(2016) Marleen Schonewille et al.   JOURNAL OF LIPID RESEARCH

A Century of Cholesterol and Coronaries: From Plaques to Genes to Statins

(2015) Joseph L. Goldstein et al.   CELL

All for Statins and Statins for All; An Update

(2015) Aris P. Agouridis et al.   CURRENT PHARMACEUTICAL DESIGN

An assessment by the Statin Muscle Safety Task Force: 2014 update

(2014) Robert S. Rosenson et al.   Journal of Clinical Lipidology

The pharmacology of statins

(2014) Cesare R. Sirtori   PHARMACOLOGICAL RESEARCH

Design and Synthesis of Dual-Action Inhibitors Targeting Histone Deacetylases and 3-Hydroxy-3-methylglutaryl Coenzyme A Reductase for Cancer Treatment

(2013) Jhih-Bin Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

A generalized approach to sampling backbone conformations with RosettaDock for CAPRI rounds 13-19

(2010) Aroop Sircar et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

Feedback regulation of cholesterol synthesis: sterol-accelerated ubiquitination and degradation of HMG CoA reductase

(2008) Russell A DeBose-Boyd   CELL RESEARCH