PHOTACs enable optical control of protein degradation

Optical Control of Small Molecule-Induced Protein Degradation

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

Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)

(2019) Jiantao Hu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer

(2019) Xin Han et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2019) Xiuyun Sun et al.   Cell Discovery

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

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

Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models

(2019) M Catarina Silva et al.   eLife

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

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

(2018) Alexandru D. Buhimschi et al.   BIOCHEMISTRY

In Vivo Photopharmacology

(2018) Katharina Hüll et al.   CHEMICAL REVIEWS

Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK)

(2018) Chelsea E. Powell et al.   JOURNAL OF MEDICINAL CHEMISTRY

The dTAG system for immediate and target-specific protein degradation

(2018) Behnam Nabet et al.   Nature Chemical Biology

Plasticity in binding confers selectivity in ligand-induced protein degradation

(2018) Radosław P. Nowak et al.   Nature Chemical Biology

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

Transcription Factors Activate Genes through the Phase-Separation Capacity of Their Activation Domains

(2018) Ann Boija et al.   CELL

Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression

(2018) Yangbing Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

The F-Box Domain-Dependent Activity of EMI1 Regulates PARPi Sensitivity in Triple-Negative Breast Cancers

(2018) Antonio Marzio et al.   MOLECULAR CELL

Dual inhibition of DNMTs and EZH2 can overcome both intrinsic and acquired resistance of myeloma cells to IMiDs in a cereblon-independent manner

(2017) Konstantinos Dimopoulos et al.   Molecular Oncology

PTEN counteracts FBXL2 to promote IP3R3- and Ca2+-mediated apoptosis limiting tumour growth

(2017) Shafi Kuchay et al.   NATURE

Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation

(2017) Calla M Olson et al.   Nature Chemical Biology

BET Proteins as Targets for Anticancer Treatment

(2017) Anastasios Stathis et al.   Cancer Discovery

Oncologic Photodynamic Therapy: Basic Principles, Current Clinical Status and Future Directions

(2017) Demian van Straten et al.   Cancers

Emerging Targets in Photopharmacology

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

Expression of the cereblon binding protein argonaute 2 plays an important role for multiple myeloma cell growth and survival

(2016) Qinqin Xu et al.   BMC CANCER

Novel Irreversible Agonists Acting at the A1 Adenosine Receptor

(2016) Manuela Jörg et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Red-Shifting Azobenzene Photoswitches for in Vivo Use

(2015) Mingxin Dong et al.   ACCOUNTS OF CHEMICAL RESEARCH

HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins

(2015) Dennis L. Buckley et al.   ACS Chemical Biology

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

Photoswitchable Inhibitors of Microtubule Dynamics Optically Control Mitosis and Cell Death

(2015) Malgorzata Borowiak et al.   CELL

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

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

Long wavelength optical control of glutamate receptor ion channels using a tetra-ortho-substituted azobenzene derivative

(2014) A. Rullo et al.   CHEMICAL COMMUNICATIONS

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

(2014) Eric S. Fischer et al.   NATURE

SCF ubiquitin ligase-targeted therapies

(2014) Jeffrey R. Skaar et al.   NATURE REVIEWS DRUG DISCOVERY

General Method for Regulating Protein Stability with Light

(2013) Kimberly M. Bonger et al.   ACS Chemical Biology

Optical Control of TRPV1 Channels

(2013) Marco Stein et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A LOV2 Domain-Based Optogenetic Tool to Control Protein Degradation and Cellular Function

(2013) Christian Renicke et al.   CHEMISTRY & BIOLOGY

A Comprehensive Mathematical Model for Three-Body Binding Equilibria

(2013) Eugene F. Douglass et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Bidirectional Photocontrol of Peptide Conformation with a Bridged Azobenzene Derivative

(2012) Subhas Samanta et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The Development and Application of Optogenetics

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

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

PARP-1 cleavage fragments: signatures of cell-death proteases in neurodegeneration

(2011) Ganta Chaitanya et al.   Cell Communication and Signaling

Impact of linker length on the activity of PROTACs

(2010) Kedra Cyrus et al.   Molecular BioSystems

Double bromodomain-containing gene Brd2 is essential for embryonic development in mouse

(2009) Enyuan Shang et al.   DEVELOPMENTAL DYNAMICS

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