Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation

Targeted protein degraders crowd into the clinic

(2021) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Recent Developments in PROTAC‐Mediated Protein Degradation: From Bench to Clinic

(2021) Zhenyi Hu et al.   CHEMBIOCHEM

Unraveling the Role of Linker Design in Proteolysis Targeting Chimeras

(2021) Troy A. Bemis et al.   JOURNAL OF MEDICINAL CHEMISTRY

The PROTACtable genome

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

Ligands for cereblon: 2017–2021 patent overview

(2021) Alexander Kazantsev et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

The PROTAC gold rush

(2021) Ken Garber   NATURE BIOTECHNOLOGY

Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands

(2021) Aleša Bricelj et al.   ACS Medicinal Chemistry Letters

Fundamental aspects of DMPK optimization of targeted protein degraders

(2020) Carina Cantrill et al.   DRUG DISCOVERY TODAY

SuFEx-enabled high-throughput medicinal chemistry

(2020) Seiya Kitamura et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

(2020) Andy Pike et al.   DRUG DISCOVERY TODAY

Optimal linker length for small molecule PROTACs that selectively target p38α and p38β for degradation

(2020) Craig Donoghue et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes

(2020) James Schiemer et al.   Nature Chemical Biology

Solution Conformations Shed Light on PROTAC Cell Permeability

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

Small-Molecule Approaches to Targeted Protein Degradation

(2020) Tyler B. Faust et al.   Annual Review of Cancer Biology-Series

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

Targeted protein degradation: elements of PROTAC design

(2019) Stacey-Lynn Paiva et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Development of targeted protein degradation therapeutics

(2019) Philip P. Chamberlain et al.   Nature Chemical Biology

Targeted protein degradation: expanding the toolbox

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

Plasticity in binding confers selectivity in ligand-induced protein degradation

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

Quantitative Live-Cell Kinetic Degradation and Mechanistic Profiling of PROTAC Mode of Action

(2018) Kristin M. Riching et al.   ACS Chemical Biology

Nanoscale synthesis and affinity ranking

(2018) Nathan J. Gesmundo et al.   NATURE

Structural basis of PROTAC cooperative recognition for selective protein degradation

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

Induced protein degradation: an emerging drug discovery paradigm

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

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Off-Rate Screening (ORS) By Surface Plasmon Resonance. An Efficient Method to Kinetically Sample Hit to Lead Chemical Space from Unpurified Reaction Products

(2014) James B. Murray et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of histone deacetylase 8 selective inhibitors

(2011) Weiping Tang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS