Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity

SPR-Measured Dissociation Kinetics of PROTAC Ternary Complexes Influence Target Degradation Rate

(2019) Michael J. Roy et al.   ACS Chemical Biology

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

High-Throughput Cysteine Scanning To Identify Stable Antibody Conjugation Sites for Maleimide- and Disulfide-Based Linkers

(2018) Rachana Ohri et al.   BIOCONJUGATE CHEMISTRY

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors

(2018) Steven D. Fidanze et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

An Anti-CLL-1 Antibody-Drug Conjugate for the Treatment of Acute Myeloid Leukemia

(2018) Bing Zheng et al.   CLINICAL CANCER RESEARCH

Intratumoral Payload Concentration Correlates with the Activity of Antibody–Drug Conjugates

(2018) Donglu Zhang et al.   MOLECULAR CANCER THERAPEUTICS

Induced protein degradation of anaplastic lymphoma kinase (ALK) by proteolysis targeting chimera (PROTAC)

(2018) Chung Hyo Kang et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Two Decades under the Influence of the Rule of Five and the Changing Properties of Approved Oral Drugs

(2018) Michael D. Shultz   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Brd4 for cancer therapy: inhibitors and degraders

(2018) Yingchao Duan et al.   MedChemComm

MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53

(2018) John Hines et al.   CANCER RESEARCH

Investigational BET bromodomain protein inhibitors in early stage clinical trials for acute myelogenous leukemia (AML)

(2017) Thorsten Braun et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

In VivoKnockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs)

(2017) Nobumichi Ohoka et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

(2017) Kwok-Ho Chan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Drug Discovery Targeting Bromodomain-Containing Protein 4

(2017) Zhiqing Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells

(2017) D T Saenz et al.   LEUKEMIA

BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cells

(2017) B Sun et al.   LEUKEMIA

Modulating Therapeutic Activity and Toxicity of Pyrrolobenzodiazepine Antibody–Drug Conjugates with Self-Immolative Disulfide Linkers

(2017) Thomas H. Pillow et al.   MOLECULAR CANCER THERAPEUTICS

BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment

(2017) Georg E. Winter et al.   MOLECULAR CELL

Strategies and challenges for the next generation of antibody–drug conjugates

(2017) Alain Beck et al.   NATURE REVIEWS DRUG DISCOVERY

Decoupling stability and release in disulfide bonds with antibody-small molecule conjugates

(2017) Thomas H. Pillow et al.   Chemical Science

Custom-Designed Affinity Capture LC-MS F(ab′)2 Assay for Biotransformation Assessment of Site-Specific Antibody Drug Conjugates

(2016) Dian Su et al.   ANALYTICAL CHEMISTRY

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

BET inhibitors in the treatment of hematologic malignancies: current insights and future prospects

(2016) Hidayatullah Munshi et al.   OncoTargets and Therapy

Bromodomain inhibitor OTX015 in patients with acute leukaemia: a dose-escalation, phase 1 study

(2016) Céline Berthon et al.   Lancet Haematology

Bromodomain inhibitor OTX015 in patients with lymphoma or multiple myeloma: a dose-escalation, open-label, pharmacokinetic, phase 1 study

(2016) Sandy Amorim et al.   Lancet Haematology

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

(2015) Michael Zengerle et al.   ACS Chemical Biology

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

Antibody-Drug Conjugates: An Emerging Concept in Cancer Therapy

(2014) Ravi V. J. Chari et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Targeting bromodomains: epigenetic readers of lysine acetylation

(2014) Panagis Filippakopoulos et al.   NATURE REVIEWS DRUG DISCOVERY

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE