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

Optical Control of Small Molecule-Induced Protein Degradation

(2020) Yuta Naro et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

PHOTACs enable optical control of protein degradation

(2020) Martin Reynders et al.   Science Advances

Very low intensity ultrasounds as a new strategy to improve selective delivery of nanoparticles-complexes in cancer cells

(2019) Rossella Loria et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Developing potent PROTACs tools for selective degradation of HDAC6 protein

(2019) Zixuan An et al.   Protein & Cell

The BAF complex in development and disease

(2019) Amelie Alfert et al.   Epigenetics & Chromatin

Degradation of Bruton’s tyrosine kinase mutants by PROTACs for potential treatment of ibrutinib-resistant non-Hodgkin lymphomas

(2019) Yonghui Sun et al.   LEUKEMIA

Emerging roles of and therapeutic strategies targeting BRD4 in cancer

(2019) Mary E. White et al.   CELLULAR IMMUNOLOGY

PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding

(2019) Christopher P. Tinworth et al.   ACS Chemical Biology

From Inhibition to Degradation: Targeting the Anti-apoptotic Protein Myeloid Cell Leukemia 1 (MCL1)

(2019) James William Papatzimas et al.   JOURNAL OF MEDICINAL CHEMISTRY

Acquired Resistance to BET-PROTACs(Proteolysis Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 ligase Complexes

(2019) Lu Zhang et al.   MOLECULAR CANCER THERAPEUTICS

Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation

(2019) George M Burslem et al.   CANCER RESEARCH

BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

(2019) William Farnaby et al.   Nature Chemical Biology

Development and Clinical Trials of Nucleic Acid Medicines for Pancreatic Cancer Treatment

(2019) Keiko Yamakawa et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands

(2019) Ziqian Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of targeted protein degradation therapeutics

(2019) Philip P. Chamberlain et al.   Nature Chemical Biology

Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable PhotoPROTACs

(2019) Patrick Pfaff et al.   ACS Central Science

A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo

(2019) Longchuan Bai et al.   CANCER CELL

Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity

(2019) Thomas H. Pillow et al.   ChemMedChem

BRD4 PROTAC as a novel therapeutic approach for the treatment of vemurafenib resistant melanoma: Preformulation studies, formulation development and in vitro evaluation

(2019) Drishti Rathod et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Light-Induced Protein Degradation with Photocaged PROTACs

(2019) Gang Xue et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeted protein degradation: expanding the toolbox

(2019) Matthieu Schapira et al.   NATURE REVIEWS DRUG DISCOVERY

PROTAC induced-BET protein degradation exhibits potent anti-osteosarcoma activity by triggering apoptosis

(2019) Chengcheng Shi et al.   Cell Death & Disease

Structure-Based Design of a Macrocyclic PROTAC

(2019) Andrea Testa et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

Targeting the C481S Ibrutinib-Resistance Mutation in Bruton’s Tyrosine Kinase Using PROTAC-Mediated Degradation

(2018) Alexandru D. Buhimschi et al.   BIOCHEMISTRY

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

STAT3, stem cells, cancer stem cells and p63

(2018) Michaela Galoczova et al.   CELLULAR & MOLECULAR BIOLOGY LETTERS

Design and synthesis of novel bispecific molecules for inducing BRD4 protein degradation

(2018) Shihui Wang et al.   CHEMICAL RESEARCH IN CHINESE UNIVERSITIES

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

Protein targeting chimeric molecules specific for bromodomain and extra-terminal motif family proteins are active against pre-clinical models of multiple myeloma

(2018) Xiaohui Zhang et al.   LEUKEMIA

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

Abstract 5236: ARV-110: An androgen receptor PROTAC degrader for prostate cancer

(2018) Taavi Neklesa et al.   CANCER RESEARCH

STAT3 is a master regulator of epithelial identity and KRAS-driven tumorigenesis

(2018) Stephen D'Amico et al.   GENES & DEVELOPMENT

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

(2018) John Hines et al.   CANCER RESEARCH

FLT3 inhibitors in acute myeloid leukemia

(2018) Mei Wu et al.   Journal of Hematology & Oncology

Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion

(2018) George M. Burslem et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

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

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

(2017) Bing Zhou 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 Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment

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

FDA-Approved Oligonucleotide Therapies in 2017

(2017) Cy A. Stein et al.   MOLECULAR THERAPY

Structural basis of PROTAC cooperative recognition for selective protein degradation

(2017) Morgan S Gadd et al.   Nature Chemical Biology

Delivery technologies for genome editing

(2017) Hao Yin et al.   NATURE REVIEWS DRUG DISCOVERY

Waste disposal—An attractive strategy for cancer therapy

(2017) Jemilat Salami et al.   SCIENCE

FLT3 activating mutations display differential sensitivity to multiple tyrosine kinase inhibitors

(2017) Bao Nguyen et al.   Oncotarget

Hydrophobic tagging-mediated degradation of Alzheimer's disease related Tau

(2017) Na Gao et al.   RSC Advances

Immunomodulatory Effect of Flavonoids of Blueberry (Vaccinium corymbosum L.) Leaves via the NF-κB Signal Pathway in LPS-Stimulated RAW 264.7 Cells

(2017) Dazhi Shi et al.   Journal of Immunology Research

Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand

(2016) Yosuke Demizu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Protein Knockdown Technology: Application of Ubiquitin Ligase to Cancer Therapy

(2016) Nobumichi Ohoka et al.   CURRENT CANCER DRUG TARGETS

Ubiquilin-mediated Small Molecule Inhibition of Mammalian Target of Rapamycin Complex 1 (mTORC1) Signaling

(2016) Rory T. Coffey et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

Cornerstones of CRISPR–Cas in drug discovery and therapy

(2016) Christof Fellmann et al.   NATURE REVIEWS DRUG DISCOVERY

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

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Oligonucleotide Therapies: The Past and the Present

(2015) Karin E. Lundin et al.   HUMAN GENE THERAPY

Knocking down disease: a progress report on siRNA therapeutics

(2015) Anders Wittrup et al.   NATURE REVIEWS GENETICS

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

B-Cell Receptor Signaling in Diffuse Large B-Cell lymphoma

(2015) Ryan M. Young et al.   SEMINARS IN HEMATOLOGY

Essential role of BRG, the ATPase subunit of BAF chromatin remodeling complexes, in leukemia maintenance

(2014) M. Buscarlet et al.   BLOOD

Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide

(2014) Eric S. Fischer et al.   NATURE

Regulation of STAT signaling by acetylation

(2013) Shougang Zhuang   CELLULAR SIGNALLING

Inhibitor of Apoptosis (IAP) Proteins-Modulators of Cell Death and Inflammation

(2013) J. Silke et al.   Cold Spring Harbor Perspectives in Biology

Inhibitor Mediated Protein Degradation

(2012) Marcus J.C. Long et al.   CHEMISTRY & BIOLOGY

Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia

(2012) Catherine C. Smith et al.   NATURE

BCR-ABL uncouples canonical JAK2-STAT5 signaling in chronic myeloid leukemia

(2012) Oliver Hantschel et al.   Nature Chemical Biology

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

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

Reversible Resistance Induced by FLT3 Inhibition: A Novel Resistance Mechanism in Mutant FLT3-Expressing Cells

(2011) Ellen Weisberg et al.   PLoS One

Mcl-1; the molecular regulation of protein function

(2010) Luke W. Thomas et al.   FEBS LETTERS

Results of the CONFIRM Phase III Trial Comparing Fulvestrant 250 mg With Fulvestrant 500 mg in Postmenopausal Women With Estrogen Receptor–Positive Advanced Breast Cancer

(2010) Angelo Di Leo et al.   JOURNAL OF CLINICAL ONCOLOGY

Protacs for Treatment of Cancer

(2010) Kathleen M Sakamoto   PEDIATRIC RESEARCH

Bruton’s tyrosine kinase (Btk): function, regulation, and transformation with special emphasis on the PH domain

(2009) Abdalla J. Mohamed et al.   IMMUNOLOGICAL REVIEWS

Quality Control Against Misfolded Proteins in the Cytosol: A Network for Cell Survival

(2009) H. Kubota   JOURNAL OF BIOCHEMISTRY