Emerging TACnology: Heterobifunctional Small Molecule Inducers of Targeted Posttranslational Protein Modifications

PROTAC targeted protein degraders: the past is prologue

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

Deubiquitinase-targeting chimeras for targeted protein stabilization

(2022) Nathaniel J. Henning et al.   Nature Chemical Biology

TF-DUBTACs Stabilize Tumor Suppressor Transcription Factors

(2022) Jing Liu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Radiotherapy-Triggered Proteolysis Targeting Chimera Prodrug Activation in Tumors

(2022) Chunrong Yang et al.   Journal of the American Chemical Society

Degradation of lipid droplets by chimeric autophagy-tethering compounds

(2021) Yuhua Fu et al.   CELL RESEARCH

Targeted Protein Acetylation in Cells Using Heterobifunctional Molecules

(2021) Wesley W. Wang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

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

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

Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective

(2020) Andy Pike et al.   DRUG DISCOVERY TODAY

Phosphorylation-Inducing Chimeric Small Molecules

(2020) Sachini U. Siriwardena et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Lysosome-targeting chimaeras for degradation of extracellular proteins

(2020) Steven M. Banik et al.   NATURE

First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo

(2020) Mingming Wei et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Solution Conformations Shed Light on PROTAC Cell Permeability

(2020) Yoseph Atilaw et al.   ACS Medicinal Chemistry Letters

The PROTAC technology in drug development

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

Visualization and Analysis of Epiproteome Dynamics

(2019) Sandeep Kaur et al.   JOURNAL OF MOLECULAR BIOLOGY

Rapid and Reversible Knockdown of Endogenously Tagged Endosomal Proteins via an Optimized HaloPROTAC Degrader

(2019) Hannah Tovell et al.   ACS Chemical Biology

Targeted Protein Internalization and Degradation by ENDosome TArgeting Chimeras (ENDTACs)

(2019) Dhanusha A. Nalawansha et al.   ACS Central Science

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

Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable PhotoPROTACs

(2019) Patrick Pfaff et al.   ACS Central Science

Degradation of proteins by PROTACs and other strategies

(2019) Yang Wang et al.   Acta Pharmaceutica Sinica B

Bifunctional chemical probes inducing protein–protein interactions

(2019) Chiara Maniaci et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Light-Induced Protein Degradation with Photocaged PROTACs

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

Heterobifunctional Molecules Induce Dephosphorylation of Kinases–A Proof of Concept Study

(2019) Sayumi Yamazoe et al.   JOURNAL OF MEDICINAL CHEMISTRY

AUTACs: Cargo-Specific Degraders Using Selective Autophagy

(2019) Daiki Takahashi et al.   MOLECULAR CELL

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

(2019) Sajid Khan et al.   NATURE MEDICINE

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

(2018) Shanshan Gu et al.   BIOESSAYS

Cargo recognition and degradation by selective autophagy

(2018) Damián Gatica et al.   NATURE CELL BIOLOGY

PTMD: A Database of Human Disease-associated Post-translational Modifications

(2018) Haodong Xu et al.   GENOMICS PROTEOMICS & BIOINFORMATICS

Selective Degradation of Polo-like Kinase 1 by a Hydrophobically Tagged Inhibitor of the Polo-Box Domain

(2018) Stefan Rubner et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Structural basis of PROTAC cooperative recognition for selective protein degradation

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

DrugBank 5.0: a major update to the DrugBank database for 2018

(2017) David S Wishart et al.   NUCLEIC ACIDS RESEARCH

Targeted protein degradation by PROTACs

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

Boc3Arg-Linked Ligands Induce Degradation by Localizing Target Proteins to the 20S Proteasome

(2016) Yuntao Shi et al.   ACS Chemical Biology

Efficient protein knockdown of HaloTag-fused proteins using hybrid molecules consisting of IAP antagonist and HaloTag ligand

(2016) Shusuke Tomoshige et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Induced protein degradation: an emerging drug discovery paradigm

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

UniProt: the universal protein knowledgebase

(2016)   NUCLEIC ACIDS RESEARCH

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

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

Small-Molecule-Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging

(2015) Jeffrey L. Gustafson et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

HaloTag Technology: A Versatile Platform for Biomedical Applications

(2015) Christopher G. England et al.   BIOCONJUGATE CHEMISTRY

Development of small molecules targeting the pseudokinase Her3

(2015) Sang Min Lim et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Oral Selective Estrogen Receptor Downregulators (SERDs), a Breakthrough Endocrine Therapy for Breast Cancer

(2015) Donald P. McDonnell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Degradation of HaloTag-fused nuclear proteins using bestatin-HaloTag ligand hybrid molecules

(2015) Shusuke Tomoshige et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Pharmacological targeting of the pseudokinase Her3

(2014) Ting Xie et al.   Nature Chemical Biology

Non-histone protein methylation as a regulator of cellular signalling and function

(2014) Kyle K. Biggar et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Emerging Principles for the Therapeutic Exploitation of Glycosylation

(2014) Martin Dalziel et al.   SCIENCE

Cullin-RING Ligases as Attractive Anti-cancer Targets

(2013) Yongchao Zhao et al.   CURRENT PHARMACEUTICAL DESIGN

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

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

(2012) Christopher A. Lipinski et al.   ADVANCED DRUG DELIVERY REVIEWS

Identification of Hydrophobic Tags for the Degradation of Stabilized Proteins

(2012) Hyun Seop Tae et al.   CHEMBIOCHEM

Inhibitor Mediated Protein Degradation

(2012) Marcus J.C. Long et al.   CHEMISTRY & BIOLOGY

Deciphering a global network of functionally associated post-translational modifications

(2012) Pablo Minguez et al.   Molecular Systems Biology

Post-translational modification: nature's escape from genetic imprisonment and the basis for dynamic information encoding

(2012) Sudhakaran Prabakaran et al.   Wiley Interdisciplinary Reviews-Systems Biology and Medicine

Small-molecule hydrophobic tagging–induced degradation of HaloTag fusion proteins

(2011) Taavi K Neklesa et al.   Nature Chemical Biology

Targeting the Undruggable Proteome: The Small Molecules of My Dreams

(2010) Craig M. Crews   CHEMISTRY & BIOLOGY

HaloTag7: A genetically engineered tag that enhances bacterial expression of soluble proteins and improves protein purification

(2009) Rachel Friedman Ohana et al.   PROTEIN EXPRESSION AND PURIFICATION