Clinically acquired resistance is a major challenge in cancer therapies with small-molecule
kinase inhibitors (SMKIs). Gatekeeper mutations in the ATP-binding pocket of kinases are …

DNA-encoded libraries have emerged as a widely used resource for the discovery of
bioactive small molecules, and offer substantial advantages compared with conventional …

Highlights•Cancer kills over 8 million people each year, and arthritis affects over 300
million.•Both cancer and arthritis involve tissue degradation, invasion, and …

Background Liver cancer is one of the leading causes of cancer-related death worldwide.
Dihydrotanshinone I (DHI) was shown to inhibit the growth of several types of cancer …

Cyclic peptides have long tantalized drug designers with their potential ability to combine
the best attributes of antibodies and small molecules. An ideal cyclic peptide drug candidate …

ATP-competitive inhibitors that demonstrate exquisite selectivity for specific members of the
human kinome have been developed. Despite this success, the identification of highly …

This chapter will discuss the recent literature of macrocycles and drug-like property space
moving beyond the rule of five (bRo5). Trends in chemical classes that fall within this …

Hck, a Src family nonreceptor tyrosine kinase (SFK), has recently been established as an
attractive pharmacological target to improve pulmonary function in COVID-19 patients. Hck …

Abstract c-Met has been an attractive target of prognostic and therapeutic studies in various
cancers. TPX-0022 is a macrocyclic inhibitor of c-Met, c-Src and CSF1R kinases and is …

Chapter 13 360 become highly skilled in developing bespoke ATP competitive kinase
inhibitors, 1, 2 which achieve selectivity by targeting distinguishing features of their active …