Triazol: a privileged scaffold for proteolysis targeting chimeras

The PROTAC technology in drug development

(2019) Yutian Zou et al.   CELL BIOCHEMISTRY AND FUNCTION

Medicinal chemistry approaches of poly ADP-Ribose polymerase 1 (PARP1) inhibitors as anticancer agents - A recent update

(2019) Priyancy G. Jain et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A chemical approach for global protein knockdown from mice to non-human primates

(2019) Xiuyun Sun et al.   Cell Discovery

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

(2019) Yonghui Sun et al.   LEUKEMIA

Proteolysis-targeting chimeras for targeting protein for degradation

(2019) Jianguo Qi et al.   Future Medicinal Chemistry

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

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

Treatment of Prostate Cancers and Kennedy’s Disease by PROTAC-Androgen Receptor Degradation

(2019) Robert B. Kargbo   ACS Medicinal Chemistry Letters

Click chemistry-assisted synthesis of novel aminonaphthoquinone-1,2,3-triazole hybrids and investigation of their cytotoxicity and cancer cell cycle alterations

(2019) Maryam Gholampour et al.   BIOORGANIC CHEMISTRY

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

(2018) Shanshan Gu et al.   BIOESSAYS

Development of the first small molecule histone deacetylase 6 (HDAC6) degraders

(2018) Ka Yang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review

(2018) Chengyuan Liang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Biotin conjugated organic molecules and proteins for cancer therapy: A review

(2018) Santanu Maiti et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Strategies to overcome resistance mutations of Bruton's tyrosine kinase inhibitor ibrutinib

(2018) Linyi Liu et al.   Future Medicinal Chemistry

Rational application of drug promiscuity in medicinal chemistry

(2018) Yicheng Mei et al.   Future Medicinal Chemistry

Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity

(2018) Jinlei Bian et al.   BIOORGANIC CHEMISTRY

Imidazopyridine linked triazoles as tubulin inhibitors, effectively triggering apoptosis in lung cancer cell line

(2018) Ibrahim Bin Sayeed et al.   BIOORGANIC CHEMISTRY

Chemically induced degradation of CK2 by proteolysis targeting chimeras based on a ubiquitin–proteasome pathway

(2018) Hong Chen et al.   BIOORGANIC CHEMISTRY

HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors

(2018) Rekha Sangwan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

(2018) Sainan An et al.   EBioMedicine

Proteolysis Targeting Chimera (PROTAC): A Paradigm-Shifting Approach in Small Molecule Drug Discovery

(2018) Pingyuan Wang et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

The role of microRNAs in photodynamic therapy of cancer

(2017) Sherien M. El-Daly et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Towards antibody-drug conjugates and prodrug strategies with extracellular stimuli-responsive drug delivery in the tumor microenvironment for cancer therapy

(2017) Nicolas Joubert et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Small molecules and their role in effective preclinical target validation

(2017) Michael A Clegg et al.   Future Medicinal Chemistry

A comprehensive look of poly(ADP-ribose) polymerase inhibition strategies and future directions for cancer therapy

(2017) Chandan Kumar et al.   Future Medicinal 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

Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?

(2017) Ian Churcher   JOURNAL OF MEDICINAL CHEMISTRY

Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals)

(2017) Matthias Schiedel 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

Structural basis of PROTAC cooperative recognition for selective protein degradation

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

Waste disposal—An attractive strategy for cancer therapy

(2017) Jemilat Salami et al.   SCIENCE

Small-Molecule PROTACS: New Approaches to Protein Degradation

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

Drugging Undruggable Molecular Cancer Targets

(2016) John S. Lazo et al.   Annual Review of Pharmacology and Toxicology

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

Cu-Catalyzed Click Reaction in Carbohydrate Chemistry

(2016) Vinod K. Tiwari et al.   CHEMICAL REVIEWS

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

Identification of Polo-like kinase 1 interaction inhibitors using a novel cell-based assay

(2016) Karine Normandin et al.   Scientific Reports

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

(2016) Honorine Lebraud et al.   ACS Central Science

Optimized Plk1 PBD Inhibitors Based on Poloxin Induce Mitotic Arrest and Apoptosis in Tumor Cells

(2015) Andrej Scharow et al.   ACS Chemical Biology

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

(2015) Michael Zengerle et al.   ACS Chemical Biology

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Emerging drugs in refractory colorectal cancer

(2015) Stefania Nobili et al.   Future Medicinal Chemistry

Targeting ubiquitination for cancer therapies

(2015) John Kenneth Morrow et al.   Future Medicinal Chemistry

Targeting autophagy to overcome drug resistance in cancer therapy

(2015) Ankit Kumar et al.   Future Medicinal Chemistry

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

Small-Molecule Control of Intracellular Protein Levels through Modulation of the Ubiquitin Proteasome System

(2014) Dennis L. Buckley et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Therapeutic potentials of gene silencing by RNA interference: Principles, challenges, and new strategies

(2014) Yan Deng et al.   GENE

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

(2014) Eric S. Fischer et al.   NATURE

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

Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs

(2013) J. Hines et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Direct Evidence of a Dinuclear Copper Intermediate in Cu(I)-Catalyzed Azide-Alkyne Cycloadditions

(2013) B. T. Worrell et al.   SCIENCE

Histone deacetylase inhibitors in the treatment of cancer: overview and perspectives

(2012) Giuseppe Giannini et al.   Future Medicinal Chemistry

Greasy tags for protein removal

(2012) Taavi K. Neklesa et al.   NATURE

B-Cell Receptor Pathobiology and Targeting in NHL

(2012) Ines M. Macias-Perez et al.   Current Oncology Reports

Global cancer statistics

(2011) Ahmedin Jemal et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Structure-based systems biology for analyzing off-target binding

(2011) Lei Xie et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

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

Antagonists Induce a Conformational Change in cIAP1 That Promotes Autoubiquitination

(2011) E. C. Dueber et al.   SCIENCE

Current chemotherapies for recurrent/metastatic head and neck cancer

(2010) Yann Molin et al.   ANTI-CANCER DRUGS

Targeting the Undruggable Proteome: The Small Molecules of My Dreams

(2010) Craig M. Crews   CHEMISTRY & BIOLOGY

Monoclonal antibodies in the treatment of metastatic colorectal cancer: A review

(2010) Jolien Tol et al.   CLINICAL THERAPEUTICS

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

Development trends for human monoclonal antibody therapeutics

(2010) Aaron L. Nelson et al.   NATURE REVIEWS DRUG DISCOVERY

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

Leveraging therapeutic potential of multi-targeted siRNA inhibitors

(2009) Qing Ge et al.   Future Medicinal Chemistry

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

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

Targeting steroid hormone receptors for ubiquitination and degradation in breast and prostate cancer

(2008) A Rodriguez-Gonzalez et al.   ONCOGENE