Bioorthogonal PROTAC Prodrugs Enabled by On-Target Activation

Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond

(2022) Yue Zhong et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The mutation of BCOR is highly recurrent and oncogenic in mature T-cell lymphoma

(2021) Jin Hyun Kang et al.   BMC CANCER

Development of Antibody-Based PROTACs for the Degradation of the Cell-Surface Immune Checkpoint Protein PD-L1

(2021) Adam D. Cotton et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties

(2021) Peter S. Dragovich et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeted drug delivery strategies for precision medicines

(2021) Mandana T. Manzari et al.   Nature Reviews Materials

Cancer Selective Target Degradation by Folate-Caged PROTACs

(2021) Jing Liu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Unleashing the Power of Bond Cleavage Chemistry in Living Systems

(2021) Jie Wang et al.   ACS Central Science

Aptamer‐PROTAC Conjugates (APCs) for Tumor‐Specific Targeting in Breast Cancer

(2021) Shipeng He et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Introduction: Click Chemistry

(2021) Neal K. Devaraj et al.   CHEMICAL REVIEWS

Improved Anti-Triple Negative Breast Cancer Effects of Docetaxel by RGD-Modified Lipid-Core Micelles

(2021) Rujing Chen et al.   International Journal of Nanomedicine

Smart Nano‐PROTACs Reprogram Tumor Microenvironment for Activatable Photo‐metabolic Cancer Immunotherapy

(2021) Chi Zhang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity,

(2021) Dongwen Lv et al.   Nature Communications

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

Optical Control of Small Molecule-Induced Protein Degradation

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

Light-induced control of protein destruction by opto-PROTAC

(2020) Jing Liu et al.   Science Advances

PHOTACs enable optical control of protein degradation

(2020) Martin Reynders et al.   Science Advances

Antibody–PROTAC Conjugates Enable HER2-Dependent Targeted Protein Degradation of BRD4

(2020) Marı́a Maneiro et al.   ACS Chemical Biology

Targeting Strategies for Tissue-Specific Drug Delivery

(2020) Zongmin Zhao et al.   CELL

Fluorescent RGD-based pro-apoptotic peptide conjugates as mitochondria-targeting probes for enhanced anticancer activities

(2020) Syed Faheem Askari Rizvi et al.   BIOMEDICINE & PHARMACOTHERAPY

DT2216—a Bcl-xL-specific degrader is highly active against Bcl-xL-dependent T cell lymphomas

(2020) Yonghan He et al.   Journal of Hematology & Oncology

Lysosome-targeting chimaeras for degradation of extracellular proteins

(2020) Steven M. Banik et al.   NATURE

Zerumbone Induces Apoptosis in Breast Cancer Cells by Targeting αvβ3 Integrin upon Co-Administration with TP5-iRGD Peptide

(2019) Eltayeb E. M. Eid et al.   MOLECULES

BCOR involvement in cancer

(2019) Annalisa Astolfi et al.   Epigenomics

Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable PhotoPROTACs

(2019) Patrick Pfaff et al.   ACS Central Science

Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity

(2019) Thomas H. Pillow et al.   ChemMedChem

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

Shining a Light on Proteolysis Targeting Chimeras

(2019) Ellen Teichmann et al.   ACS Central Science

Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα)

(2019) Peter S. Dragovich et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Recent progress in biomedical applications of RGD‐based ligand: From precise cancer theranostics to biomaterial engineering: A systematic review

(2019) Mohsen Alipour et al.   JOURNAL OF BIOMEDICAL MATERIALS RESEARCH PART A

A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity

(2019) Sajid Khan et al.   NATURE MEDICINE

Unraveling Tetrazine-Triggered Bioorthogonal Elimination Enables Chemical Tools for Ultrafast Release and Universal Cleavage

(2018) Jonathan C. T. Carlson et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Enrichment-triggered prodrug activation demonstrated through mitochondria-targeted delivery of doxorubicin and carbon monoxide

(2018) Yueqin Zheng et al.   Nature Chemistry

Identification of thioredoxin-interacting protein (TXNIP) as a downstream target for IGF1 action

(2018) Karthik Nagaraj et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

αvβ3 Integrin Is Required for Efficient Infection of Epithelial Cells with Human Adenovirus Type 26

(2018) Davor Nestić et al.   JOURNAL OF VIROLOGY

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

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

Controlled in-cell activation of RNA therapeutics using bond-cleaving bio-orthogonal chemistry

(2017) Irfan Khan et al.   Chemical Science

The impact of receptor recycling on the exocytosis of αvβ3 integrin targeted gold nanoparticles

(2017) Yanan Cui et al.   Oncotarget

Optimized Tetrazine Derivatives for Rapid Bioorthogonal Decaging in Living Cells

(2016) Xinyuan Fan et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Development and application of bond cleavage reactions in bioorthogonal chemistry

(2016) Jie Li et al.   Nature Chemical Biology

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai 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

Conformationally strained trans-cyclooctene with improved stability and excellent reactivity in tetrazine ligation

(2014) Ampofo Darko et al.   Chemical Science

BODIPY-Tetrazine Derivatives as Superbright Bioorthogonal Turn-on Probes

(2013) Jonathan C. T. Carlson et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Click to Release: Instantaneous Doxorubicin Elimination upon Tetrazine Ligation

(2013) Ron M. Versteegen et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

MiR-134-mediated β1 integrin expression and function in mesenchymal stem cells

(2013) David M. Poitz et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Inverse electron demand Diels–Alder (iEDDA)-initiated conjugation: a (high) potential click chemistry scheme

(2013) Astrid-Caroline Knall et al.   CHEMICAL SOCIETY REVIEWS

The Functions and Applications of RGD in Tumor Therapy and Tissue Engineering

(2013) Fen Wang et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Radiolabelled RGD peptides for imaging and therapy

(2012) F. C. Gaertner et al.   EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING

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

Design and Synthesis of Highly Reactive Dienophiles for the Tetrazine–trans-Cyclooctene Ligation

(2011) Michael T. Taylor et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Tetrazine-Based Cycloadditions: Application to Pretargeted Live Cell Imaging

(2008) Neal K. Devaraj et al.   BIOCONJUGATE CHEMISTRY

Tetrazine Ligation: Fast Bioconjugation Based on Inverse-Electron-Demand Diels−Alder Reactivity

(2008) Melissa L. Blackman et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY