Waste disposal—An attractive strategy for cancer therapy

Drugging the undruggables: exploring the ubiquitin system for drug development

(2016) Xiaodong Huang et al.   CELL RESEARCH

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

(2016) Kanak Raina et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras

(2016) Honorine Lebraud et al.   ACS Central Science

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

(2015) Michael Zengerle et al.   ACS Chemical Biology

Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL

(2015) Ashton C. Lai et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Small-Molecule-Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging

(2015) Jeffrey L. Gustafson et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

RAD1901

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

Proteasome inhibitors

(2015) Beverly A. Teicher et al.   BIOCHEMICAL PHARMACOLOGY

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS

(2015) Jan Krönke et al.   NATURE

Catalytic in vivo protein knockdown by small-molecule PROTACs

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

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Cancer incidence and mortality worldwide: Sources, methods and major patterns in GLOBOCAN 2012

(2014) Jacques Ferlay et al.   INTERNATIONAL JOURNAL OF CANCER

Small Molecule-facilitated Degradation of ANO1 Protein

(2014) Anke Bill et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Androgens and androgen receptor signaling in prostate tumorigenesis

(2014) Ye Zhou et al.   JOURNAL OF MOLECULAR ENDOCRINOLOGY

Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer

(2014) Irfan A. Asangani et al.   NATURE

Pharmacological targeting of the pseudokinase Her3

(2014) Ting Xie et al.   Nature Chemical Biology

SCF ubiquitin ligase-targeted therapies

(2014) Jeffrey R. Skaar et al.   NATURE REVIEWS DRUG DISCOVERY

An in-tumor genetic screen reveals that the BET bromodomain protein, BRD4, is a potential therapeutic target in ovarian carcinoma

(2014) Maria Giuseppina Baratta et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

MDM2 Small-Molecule Antagonist RG7112 Activates p53 Signaling and Regresses Human Tumors in Preclinical Cancer Models

(2013) C. Tovar et al.   CANCER RESEARCH

Development of hybrid small molecules that induce degradation of estrogen receptor-alpha and necrotic cell death in breast cancer cells

(2013) Keiichiro Okuhira et al.   CANCER SCIENCE

Inhibition of BET Bromodomain Targets Genetically Diverse Glioblastoma

(2013) Z. Cheng et al.   CLINICAL CANCER RESEARCH

Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells

(2013) J. Kronke et al.   SCIENCE

An F876L Mutation in Androgen Receptor Confers Genetic and Phenotypic Resistance to MDV3100 (Enzalutamide)

(2013) M. Korpal et al.   Cancer Discovery

Small-Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α

(2012) Dennis L. Buckley et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Small Molecule Inhibitor of Ubiquitin-Specific Protease-7 Induces Apoptosis in Multiple Myeloma Cells and Overcomes Bortezomib Resistance

(2012) Dharminder Chauhan et al.   CANCER CELL

Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide

(2012) A Lopez-Girona et al.   LEUKEMIA

Place your BETs: the therapeutic potential of bromodomains

(2012) R.K. Prinjha et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Small-molecule hydrophobic tagging–induced degradation of HaloTag fusion proteins

(2011) Taavi K Neklesa et al.   Nature Chemical Biology

Targeting MYC dependence in cancer by inhibiting BET bromodomains

(2011) J. A. Mertz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Two-Headed PROTAC: An Effective New Tool for Targeted Protein Degradation

(2010) Kedra Cyrus  et al.   CHEMBIOCHEM

Strategies for discovering and derisking covalent, irreversible enzyme inhibitors

(2010) Douglas S Johnson et al.   Future Medicinal Chemistry

Protein Knockdown Using Methyl Bestatin−Ligand Hybrid Molecules: Design and Synthesis of Inducers of Ubiquitination-Mediated Degradation of Cellular Retinoic Acid-Binding Proteins

(2010) Yukihiro Itoh et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

RING Domain E3 Ubiquitin Ligases

(2009) Raymond J. Deshaies et al.   Annual Review of Biochemistry

Cancer Preventive Isothiocyanates Induce Selective Degradation of Cellular α- and β-Tubulins by Proteasomes

(2009) Lixin Mi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Building ubiquitin chains: E2 enzymes at work

(2009) Yihong Ye et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

(2008) Ashley R. Schneekloth et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Small Molecules Destabilize cIAP1 by Activating Auto-ubiquitylation

(2008) Keiko Sekine et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Mechanisms of acquired resistance to cetuximab: role of HER (ErbB) family members

(2008) D L Wheeler et al.   ONCOGENE