Although many kinds of therapies are applied in the clinic, drug-resistance is a major and
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …

Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been
developed for inducing the protein degradation by a targeting molecule. This technology …

B-cell lymphoma extra large (BCL-XL) is a well-validated cancer target. However, the on-
target and dose-limiting thrombocytopenia limits the use of BCL-XL inhibitors, such as …

Background Patients with advanced T cell lymphomas (TCLs) have limited therapeutic
options and poor outcomes in part because their TCLs evade apoptosis through …

The immunomodulatory drugs (IMiDs) thalidomide, lenalidomide, and pomalidomide, all
approved for the treatment of multiple myeloma, induce targeted ubiquitination and …

Inducing post-translational protein knockdown is an important approach to probe biology
and validate drug targets. An efficient strategy to achieve this involves expression of a …

Successful mapping of the human genome has sparked a widespread interest in
deciphering functional information encoded in gene sequences. However, because of the …

To understand gene function, the encoding DNA or mRNA transcript can be manipulated
and the consequences observed. However, these approaches do not have a direct effect on …

We have developed a novel bioorthogonal reaction that can selectively displace fluorine
substitutions alpha to amide bonds. This fluorine–thiol displacement reaction (FTDR) allows …

Allele-specific chemical genetics enables selective inhibition within families of highly-
conserved proteins. The four BET (bromodomain & extra-terminal domain) proteins–BRD2 …