Bispecific Estrogen Receptor α Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening

Screening of DNA-Encoded Small Molecule Libraries inside a Living Cell

(2021) Lars K. Petersen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Two-Stage Strategy for Development of Proteolysis Targeting Chimeras and its Application for Estrogen Receptor Degraders

(2020) Brett L. Roberts et al.   ACS Chemical Biology

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

PROTAC Technology: Opportunities and Challenges

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

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

Machine Learning on DNA-Encoded Libraries: A New Paradigm for Hit Finding

(2020) Kevin McCloskey et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Autotaxin Inhibitor for the Treatment of Idiopathic Pulmonary Fibrosis: A Clinical Candidate Discovered Using DNA-Encoded Chemistry

(2020) John W. Cuozzo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Prospecting for molecular glues

(2020) Willem den Besten et al.   Nature Chemical Biology

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

Quantitative Comparison of Enrichment from DNA-Encoded Chemical Library Selections

(2019) John C. Faver et al.   ACS Combinatorial Science

First targeted protein degrader hits the clinic

(2019) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Breast Cancer Treatment

(2019) Adrienne G. Waks et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Targeting Nuclear Receptors with PROTAC degraders

(2019) John J. Flanagan et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Proteolysis targeting chimeras (PROTACs) in ‘beyond rule-of-five’ chemical space: Recent progress and future challenges

(2019) Scott D. Edmondson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Selective oestrogen receptor degraders in breast cancer

(2019) Andrea Gombos   CURRENT OPINION IN ONCOLOGY

Investigational drugs in early stage clinical trials for the treatment of HER2+ breast cancer

(2019) Andrea Gombos et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

PROTAC-Mediated Degradation of Estrogen Receptor in the Treatment of Cancer

(2019) Robert B. Kargbo   ACS Medicinal Chemistry Letters

Development of cell-permeable peptide-based PROTACs targeting estrogen receptor α

(2019) Yuxuan Dai et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs

(2019) Mikihiko Naito et al.   Frontiers in Chemistry

Delineating the role of cooperativity in the design of potent PROTACs for BTK

(2018) Adelajda Zorba et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Global cancer statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries

(2018) Freddie Bray et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Signaling pathways and steroid receptors modulating estrogen receptor α function in breast cancer

(2018) Rasmus Siersbæk et al.   GENES & DEVELOPMENT

Acquired HER2 mutations in ER+ metastatic breast cancer confer resistance to estrogen receptor–directed therapies

(2018) Utthara Nayar et al.   NATURE GENETICS

A “Click Chemistry Platform” for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation

(2017) Ryan P. Wurz 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

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors

(2016) Philip A. Harris et al.   JOURNAL OF MEDICINAL CHEMISTRY

Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition

(2016) Julianty Frost et al.   Nature Communications

ActivatingESR1Mutations Differentially Affect the Efficacy of ER Antagonists

(2016) Weiyi Toy et al.   Cancer Discovery

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

Estrogen receptor mutations and functional consequences for breast cancer

(2015) Christoforos Thomas et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Encoded Library Synthesis Using Chemical Ligation and the Discovery of sEH Inhibitors from a 334-Million Member Library

(2015) Alexander Litovchick et al.   Scientific Reports

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

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

Activating ESR1 mutations in hormone-resistant metastatic breast cancer

(2013) Dan R Robinson et al.   NATURE GENETICS

Jostling for Position: Optimizing Linker Location in the Design of Estrogen Receptor-Targeting PROTACs

(2010) Kedra Cyrus et al.   ChemMedChem

Design, synthesis and selection of DNA-encoded small-molecule libraries

(2009) Matthew A Clark et al.   Nature Chemical Biology