The ability to rapidly regulate the functions of specific proteins in living cells is a valuable
tool for biological research. Here we describe a new technique by which the degradation of …

The biological role played by non-BET bromodomains remains poorly understood, and it is
therefore imperative to identify potent and highly selective inhibitors to effectively explore the …

Bivalent chemical degraders provide a catalytic route to selectively degrade disease-
associated proteins. By linking target-specific ligands with E3 ubiquitin ligase recruiting …

Hydroxylation and fluorination of proline alters the pyrrolidine ring pucker and the trans: cis
amide bond ratio in a stereochemistry-dependent fashion, affecting molecular recognition of …

INTRODUCTION Thalidomide, lenalidomide, and pomalidomide are clinically approved
therapies for the treatment of multiple myeloma and other hematologic malignancies. These …

Bifunctional degrader molecules, known as proteolysis-targeting chimeras (PROTACs),
function by recruiting a target to an E3 ligase, forming a target/PROTAC/ligase ternary …

Protein degradation via the use of bivalent chemical degraders provides an alternative
strategy to block protein function and assess the biological roles of putative drug targets …

The field of targeted protein degradation (TPD) has grown exponentially over the past
decade with the goal of developing therapies that mark proteins for destruction leveraging …

Chemical biology strategies for directly perturbing protein homeostasis including the
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …

There is a great deal of excitement around the concept of targeting proteins for degradation
as an alternative to conventional inhibitory small molecules and antibodies. Protein …