Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents

Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer

(2021) Hidetomo Yokoo et al.   ACS Medicinal Chemistry Letters

Specific non-genetic IAP-based protein erasers (SNIPERs) as a potential therapeutic strategy

(2021) Zonghui Ma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

(2021) Jeremy S. Disch et al.   JOURNAL OF MEDICINAL CHEMISTRY

Peptide Stapling Improves the Sustainability of a Peptide-Based Chimeric Molecule That Induces Targeted Protein Degradation

(2021) Hidetomo Yokoo et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Optimization of a Series of RIPK2 PROTACs

(2021) Afjal H. Miah et al.   JOURNAL OF MEDICINAL CHEMISTRY

E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points

(2021) Aleša Bricelj et al.   Frontiers in Chemistry

VHL-based PROTACs as potential therapeutic agents: Recent progress and perspectives

(2021) Chao Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Developments of CRBN-based PROTACs as potential therapeutic agents

(2021) Chao Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs

(2020) Rishi R. Shah et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Selective inhibition of Ph-positive ALL cell growth through kinase-dependent and independent effects by CDK6-specific PROTACs

(2020) Marco De Dominici et al.   BLOOD

SMAC mimetics and RIPK inhibitors as therapeutics for chronic inflammatory diseases

(2020) Simone Jensen et al.   Science Signaling

Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs

(2020) Niall A. Anderson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and synthesis of selective degraders of EGFRL858R/T790M mutant

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

Novel strategies targeting bromodomain-containing protein 4 (BRD4) for cancer drug discovery

(2020) Dailin Liang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of IAP-recruiting BCL-XL PROTACs as potent degraders across multiple cancer cell lines

(2020) Xuan Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Selective Degradation of Target Proteins by Chimeric Small-Molecular Drugs, PROTACs and SNIPERs

(2020) Minoru Ishikawa et al.   Pharmaceuticals

PROTAC-DB: an online database of PROTACs

(2020) Gaoqi Weng et al.   NUCLEIC ACIDS RESEARCH

Phosphodiesterase-4 enzyme as a therapeutic target in neurological disorders

(2020) Abid Bhat et al.   PHARMACOLOGICAL RESEARCH

Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development

(2020) Katherine A. Donovan et al.   CELL

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

(2020) Shenxin Zeng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

PROTACs to address the challenges facing small molecule inhibitors

(2020) Pedro Martín-Acosta et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes

(2020) James Schiemer et al.   Nature Chemical Biology

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

(2019) Yonghui Sun et al.   LEUKEMIA

Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives

(2019) Hui Cong 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

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

(2019) William Farnaby et al.   Nature Chemical Biology

Targeting IRAK4 for Degradation with PROTACs

(2019) Joao Nunes et al.   ACS Medicinal Chemistry Letters

Therapeutic Potential of Hematopoietic Prostaglandin D2 Synthase in Allergic Inflammation

(2019) Sonja Rittchen et al.   Cells

Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders

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

Simple Structural Modifications Converting a Bona Fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders

(2019) Jiuling Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

p97: An Emerging Target for Cancer, Neurodegenerative Diseases, and Viral Infections

(2019) Donna M. Huryn et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs

(2019) Mikihiko Naito et al.   Frontiers in Chemistry

PROTACs: An Emerging Targeting Technique for Protein Degradation in Drug Discovery

(2018) Shanshan Gu et al.   BIOESSAYS

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

Inhibitors of ER aminopeptidase 1 and 2: from design to clinical application

(2018) Dimitris Georgiadis et al.   CURRENT MEDICINAL CHEMISTRY

Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation

(2018) Nobumichi Ohoka et al.   JOURNAL OF BIOLOGICAL 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

Exercise and prostate cancer: From basic science to clinical applications

(2018) Christian Campos et al.   PROSTATE

Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs

(2018) Sainan An et al.   EBioMedicine

Different Degradation Mechanisms of Inhibitor of Apoptosis Proteins (IAPs) by the Specific and Nongenetic IAP-Dependent Protein Eraser (SNIPER)

(2018) Nobumichi Ohoka et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

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

Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands

(2017) Norihito Shibata et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting the Allosteric Site of Oncoprotein BCR-ABL as an Alternative Strategy for Effective Target Protein Degradation

(2017) Kenichiro Shimokawa et al.   ACS Medicinal Chemistry Letters

Small-Molecule PROTACS: New Approaches to Protein Degradation

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

Development of a peptide-based inducer of nuclear receptors degradation

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

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

FDA Approval of Palbociclib in Combination with Fulvestrant for the Treatment of Hormone Receptor-Positive, HER2-Negative Metastatic Breast Cancer

(2016) A. J. Walker et al.   CLINICAL CANCER RESEARCH

Origin and Functional Evolution of the Cdc48/p97/VCP AAA+ Protein Unfolding and Remodeling Machine

(2016) Dominik Barthelme et al.   JOURNAL OF MOLECULAR BIOLOGY

Small molecules, big targets: drug discovery faces the protein–protein interaction challenge

(2016) Duncan E. Scott et al.   NATURE REVIEWS DRUG DISCOVERY

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

The JAK-STAT Pathway: Impact on Human Disease and Therapeutic Intervention

(2015) John J. O'Shea et al.   Annual Review of Medicine

Structural development of stabilized helical peptides as inhibitors of estrogen receptor (ER)-mediated transcription

(2015) Yosuke Demizu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Targeting CDK4 and CDK6: From Discovery to Therapy

(2015) C. J. Sherr et al.   Cancer Discovery

Understanding the molecular pathogenesis of acute promyelocytic leukemia

(2014) Francesco Lo-Coco et al.   BEST PRACTICE & RESEARCH CLINICAL HAEMATOLOGY

Apremilast is a selective PDE4 inhibitor with regulatory effects on innate immunity

(2014) P.H. Schafer et al.   CELLULAR SIGNALLING

Recent Advances in the Discovery of Small Molecule Inhibitors of Interleukin-1 Receptor-Associated Kinase 4 (IRAK4) as a Therapeutic Target for Inflammation and Oncology Disorders

(2014) Divya Chaudhary et al.   JOURNAL OF MEDICINAL CHEMISTRY

Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders

(2014) Katrina J. Falkenberg et al.   NATURE REVIEWS DRUG DISCOVERY

Cancer cell death induced by novel small molecules degrading the TACC3 protein via the ubiquitin–proteasome pathway

(2014) N Ohoka et al.   Cell Death & Disease

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

Control of apoptosis by the BCL-2 protein family: implications for physiology and therapy

(2013) Peter E. Czabotar et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Double protein knockdown of cIAP1 and CRABP-II using a hybrid molecule consisting of ATRA and IAPs antagonist

(2012) Yukihiro Itoh et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting the von Hippel–Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1α Interaction

(2012) Dennis L. Buckley et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Development of target protein-selective degradation inducer for protein knockdown

(2011) Yukihiro Itoh et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of nuclear receptor-degradation inducers

(2011) Yukihiro Itoh et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy

(2011) Yosuke Demizu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein

(2011) Keiichiro Okuhira et al.   FEBS LETTERS

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

Targeting inhibitor of apoptosis proteins for therapeutic intervention

(2009) Chudi Ndubaku et al.   Future Medicinal Chemistry

Direct inhibition of the NOTCH transcription factor complex

(2009) Raymond E. Moellering et al.   NATURE

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

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

ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor

(2008) C. Tse et al.   CANCER RESEARCH

Small Molecules Destabilize cIAP1 by Activating Auto-ubiquitylation

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