Stimuli-activatable PROTACs for precise protein degradation and cancer therapy

E3 ligase ligand optimization of Clinical PROTACs

(2023) Hanrui Jiang et al.   Frontiers in Chemistry

Cancer-Specific Delivery of Proteolysis-Targeting Chimeras (PROTACs) and Their Application to Cancer Immunotherapy

(2023) Yujeong Moon et al.   Pharmaceutics

PROTACs: Promising approach for anticancer therapy

(2023) Simran Deep Kaur et al.   CANCER LETTERS

Advancing Strategies for Proteolysis-Targeting Chimera Design

(2023) Minglei Li et al.   Journal of Medicinal Chemistry

Protein degraders enter the clinic — a new approach to cancer therapy

(2023) Deborah Chirnomas et al.   Nature Reviews Clinical Oncology

Metal-free bioorthogonal click chemistry in cancer theranostics

(2022) Dan Wu et al.   CHEMICAL SOCIETY REVIEWS

Phase 1/2 study of ARV-110, an androgen receptor (AR) PROTAC degrader, in metastatic castration-resistant prostate cancer (mCRPC).

(2022) Xin Gao et al.   JOURNAL OF CLINICAL ONCOLOGY

Rational Design for Nitroreductase (NTR)-Responsive Proteolysis Targeting Chimeras (PROTACs) Selectively Targeting Tumor Tissues

(2022) Shi Shi et al.   JOURNAL OF MEDICINAL CHEMISTRY

PROTAC targeted protein degraders: the past is prologue

(2022) Miklós Békés et al.   NATURE REVIEWS DRUG DISCOVERY

Enzyme-Catalyzed Activation of Pro-PROTAC for Cell-Selective Protein Degradation

(2022) Chunjing Liang et al.   CCS Chemistry

Non-small molecule PROTACs (NSM-PROTACs): Protein degradation kaleidoscope

(2022) Sinan Ma et al.   Acta Pharmaceutica Sinica B

Engineered bioorthogonal POLY-PROTAC nanoparticles for tumour-specific protein degradation and precise cancer therapy

(2022) Jing Gao et al.   Nature Communications

Radiotherapy-Triggered Proteolysis Targeting Chimera Prodrug Activation in Tumors

(2022) Chunrong Yang 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

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy

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

Mutant-selective degradation by BRAF-targeting PROTACs

(2021) Shanique Alabi et al.   Nature Communications

Cancer Selective Target Degradation by Folate-Caged PROTACs

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

Targeted protein degraders crowd into the clinic

(2021) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Semiconducting polymer nano-PROTACs for activatable photo-immunometabolic cancer therapy

(2021) Chi Zhang et al.   Nature Communications

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

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

The PROTACtable genome

(2021) Melanie Schneider et al.   NATURE REVIEWS DRUG DISCOVERY

Polyprodrug Nanomedicines: An Emerging Paradigm for Cancer Therapy

(2021) Kuikun Yang et al.   ADVANCED MATERIALS

Development of photocontrolled BRD4 PROTACs for tongue squamous cell carcinoma (TSCC)

(2021) Zhenzhen Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The PROTAC gold rush

(2021) Ken Garber   NATURE BIOTECHNOLOGY

Radiotherapy as a tool to elicit clinically actionable signalling pathways in cancer

(2021) Giulia Petroni et al.   Nature Reviews Clinical Oncology

A Fluorescent Probe for Rapid, High-Contrast Visualization of Folate-Receptor-Expressing Tumors In Vivo

(2020) Koji Numasawa et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Proteolysis‐targeting chimeras in drug development: A safety perspective

(2020) Kevin Moreau et al.   BRITISH JOURNAL OF PHARMACOLOGY

Optical Control of Small Molecule-Induced Protein Degradation

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

Stress- and ubiquitylation-dependent phase separation of the proteasome

(2020) Sayaka Yasuda et al.   NATURE

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

Engineering nanomedicines through boosting immunogenic cell death for improved cancer immunotherapy

(2020) Jing Gao et al.   ACTA PHARMACOLOGICA SINICA

First-in-human phase I study of ARV-110, an androgen receptor (AR) PROTAC degrader in patients (pts) with metastatic castrate-resistant prostate cancer (mCRPC) following enzalutamide (ENZ) and/or abiraterone (ABI).

(2020) Daniel Peter Petrylak et al.   JOURNAL OF CLINICAL ONCOLOGY

Azo-PROTAC: Novel Light-Controlled Small-Molecule Tool for Protein Knockdown

(2020) Yu-Hui Jin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Exploiting the folate receptor α in oncology

(2020) Mariana Scaranti et al.   Nature Reviews Clinical Oncology

Hydrogen peroxide reactivity and specificity in thiol-based cell signalling

(2020) Christine C. Winterbourn   BIOCHEMICAL SOCIETY TRANSACTIONS

Targeted protein degradation as a powerful research tool in basic biology and drug target discovery

(2020) Tao Wu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Intact or in Pieces? A Look at How Clinically Approved, Biodegradable Block Co-Polymers Affect Blood Components

(2020) Lauren Maghak et al.   ACS Biomaterials-Science & Engineering

Engineering Prodrug Nanomedicine for Cancer Immunotherapy

(2020) Bin Yang et al.   Advanced Science

Quantitative Mapping of Glutathione within Intracranial Tumors through Interlocked MRI Signals of a Responsive Nanoprobe

(2020) Peisen Zhang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development

(2020) Katherine A. Donovan et al.   CELL

Acid-activatible micelleplex delivering siRNA-PD-L1 for improved cancer immunotherapy of CDK4/6 inhibition

(2020) Jing Gao et al.   CHINESE CHEMICAL LETTERS

Light-triggered release of photocaged therapeutics - Where are we now?

(2019) Joana M. Silva et al.   JOURNAL OF CONTROLLED RELEASE

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

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

Sign Inversion in Photopharmacology: Incorporation of Cyclic Azobenzenes in Photoswitchable Potassium Channel Blockers and Openers

(2019) Julie B. Trads et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Principles and applications of optogenetics in developmental biology

(2019) Daniel Krueger et al.   DEVELOPMENT

Light-Induced Protein Degradation with Photocaged PROTACs

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

Enzyme-Instructed Activation of Pro-protein Therapeutics In Vivo

(2019) Jin Chang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeted protein degradation: expanding the toolbox

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

Cellular quality control by the ubiquitin-proteasome system and autophagy

(2019) Christian Pohl et al.   SCIENCE

Evolution of Cereblon-Mediated Protein Degradation as a Therapeutic Modality

(2019) Philip P. Chamberlain et al.   ACS Medicinal Chemistry Letters

Glutathione-Responsive Self-Assembled Magnetic Gold Nanowreath for Enhanced Tumor Imaging and Imaging-Guided Photothermal Therapy

(2018) Yijing Liu et al.   ACS Nano

Structure and Function of the 26S Proteasome

(2018) Jared A.M. Bard et al.   Annual Review of Biochemistry

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

(2018) Alexandru D. Buhimschi et al.   BIOCHEMISTRY

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

(2018) Shanshan Gu et al.   BIOESSAYS

In Vivo Photopharmacology

(2018) Katharina Hüll et al.   CHEMICAL REVIEWS

Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK)

(2018) Chengwei Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The expanding role of prodrugs in contemporary drug design and development

(2018) Jarkko Rautio et al.   NATURE REVIEWS DRUG DISCOVERY

Principles of Ubiquitin-Dependent Signaling

(2018) Eugene Oh et al.   Annual Review of Cell and Developmental Biology

Defining the human C2H2 zinc finger degrome targeted by thalidomide analogs through CRBN

(2018) Quinlan L. Sievers et al.   SCIENCE

How Big Is Too Big for Cell Permeability?

(2017) Pär Matsson et al.   JOURNAL OF MEDICINAL 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

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

(2017) Ian Churcher   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

Prostate cancer–associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4

(2017) Xiangpeng Dai et al.   NATURE MEDICINE

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

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

Targeted protein degradation by PROTACs

(2017) Taavi K. Neklesa et al.   PHARMACOLOGY & THERAPEUTICS

Waste disposal—An attractive strategy for cancer therapy

(2017) Jemilat Salami et al.   SCIENCE

Emerging Targets in Photopharmacology

(2016) Michael M. Lerch et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Emerging nanomedicine approaches fighting tumor metastasis: animal models, metastasis-targeted drug delivery, phototherapy, and immunotherapy

(2016) Chao Liang et al.   CHEMICAL SOCIETY REVIEWS

Antibody–drug conjugates for cancer therapy

(2016) Anish Thomas et al.   LANCET ONCOLOGY

Induced protein degradation: an emerging drug discovery paradigm

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

Aptamers as targeted therapeutics: current potential and challenges

(2016) Jiehua Zhou 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

A Generic Platform for Cellular Screening Against Ubiquitin Ligases

(2016) Timurs Maculins et al.   Scientific Reports

Deoxynyboquinones as NQO1-Activated Cancer Therapeutics

(2015) Elizabeth I. Parkinson et al.   ACCOUNTS OF CHEMICAL RESEARCH

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

(2015) Michael Zengerle et al.   ACS Chemical Biology

Hypoxia and hypoxia inducible factors in tumor metabolism

(2015) Wen Zeng et al.   CANCER LETTERS

Nitroreductase-triggered activation of a novel caged fluorescent probe obtained from methylene blue

(2015) Jungeun Bae et al.   CHEMICAL COMMUNICATIONS

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Optogenetics

(2015) Jens Duebel et al.   CURRENT OPINION IN OPHTHALMOLOGY

Prime time for PROTACs

(2015) Raymond J Deshaies   Nature Chemical Biology

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

Optogenetics: 10 years of microbial opsins in neuroscience

(2015) Karl Deisseroth   NATURE NEUROSCIENCE

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

ortho-Fluoroazobenzenes: Visible Light Switches with Very Long-LivedZIsomers

(2014) Christopher Knie et al.   CHEMISTRY-A EUROPEAN JOURNAL

Ado-trastuzumab Emtansine (T-DM1): An Antibody–Drug Conjugate (ADC) for HER2-Positive Breast Cancer

(2014) John M. Lambert et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2014) Eric S. Fischer et al.   NATURE

Targeting Protein-Protein Interaction by Small Molecules

(2013) Lingyan Jin et al.   Annual Review of Pharmacology and Toxicology

Pharmacological Inactivation of Skp2 SCF Ubiquitin Ligase Restricts Cancer Stem Cell Traits and Cancer Progression

(2013) Chia-Hsin Chan et al.   CELL

Folate-Based Near-Infrared Fluorescent Theranostic Gemcitabine Delivery

(2013) Zhigang Yang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Catalase Abrogates  -Lapachone-Induced PARP1 Hyperactivation-Directed Programmed Necrosis in NQO1-Positive Breast Cancers

(2013) E. A. Bey et al.   MOLECULAR CANCER THERAPEUTICS

Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells

(2013) J. Kronke et al.   SCIENCE

The Myeloma Drug Lenalidomide Promotes the Cereblon-Dependent Destruction of Ikaros Proteins

(2013) G. Lu et al.   SCIENCE

Small-Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α

(2012) Dennis L. Buckley et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Bioorthogonal Copper-Free Click Chemistry In Vivo for Tumor-Targeted Delivery of Nanoparticles

(2012) Heebeom Koo et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Photoremovable Protecting Groups in Chemistry and Biology: Reaction Mechanisms and Efficacy

(2012) Petr Klán et al.   CHEMICAL REVIEWS

o-Fluoroazobenzenes as Readily Synthesized Photoswitches Offering Nearly Quantitative Two-Way Isomerization with Visible Light

(2012) David Bléger et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

The Development and Application of Optogenetics

(2011) Lief Fenno et al.   Annual Review of Neuroscience

The transferrin receptor and the targeted delivery of therapeutic agents against cancer

(2011) Tracy R. Daniels et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

The secret life of kinases: functions beyond catalysis

(2011) Jens Rauch et al.   Cell Communication and Signaling

Wavelength-Selective Caged Surfaces: How Many Functional Levels Are Possible?

(2011) Verónica San Miguel et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF

(2010) Sonja J. Heidorn et al.   CELL

Targeting the Undruggable Proteome: The Small Molecules of My Dreams

(2010) Craig M. Crews   CHEMISTRY & BIOLOGY

Vitamin B12in drug delivery: breaking through the barriers to a B12bioconjugate pharmaceutical

(2010) Susan M Clardy et al.   Expert Opinion on Drug Delivery

Impact of linker length on the activity of PROTACs

(2010) Kedra Cyrus et al.   Molecular BioSystems

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

(2010) Georgia Hatzivassiliou et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Chemical genetics screen for enhancers of rapamycin identifies a specific inhibitor of an SCF family E3 ubiquitin ligase

(2010) Mariam Aghajan et al.   NATURE BIOTECHNOLOGY

Delivering nanomedicine to solid tumors

(2010) Rakesh K. Jain et al.   Nature Reviews Clinical Oncology

Identification of a Primary Target of Thalidomide Teratogenicity

(2010) T. Ito et al.   SCIENCE

The 26 S Proteasome: From Basic Mechanisms to Drug Targeting

(2009) Ami Navon et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Highly Efficient ReversibleZ−EPhotoisomerization of a Bridged Azobenzene with Visible Light through Resolved S1(nπ*) Absorption Bands

(2009) Ron Siewertsen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

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

Diversity of degradation signals in the ubiquitin–proteasome system

(2008) Tommer Ravid et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY