Protein posttranslational modifications (PTMs) refer to the breaking or generation of covalent
bonds on the backbones or amino acid side chains of proteins and expand the diversity of …

Drugs that function through allosteric inhibition of kinase signaling represent a promising
approach for the targeted discovery of therapeutics. The majority of developed allosteric …

Small-molecule kinase inhibitors are invaluable targeted therapeutics for the treatment of
various human diseases, especially cancers. While the majority of approved and developed …

Abstract Background Receptor tyrosine kinases (RTKs) are signaling enzymes responsible
for the transfer of Adenosine triphosphate (ATP) γ-phosphate to the tyrosine residues …

New thiazolylpyrazolyl coumarin derivatives were synthesized and tested for their anticancer
potential in vitro against five different human cell lines, including breast MCF-7, lung A549 …

Head and neck cancers (HNC) represent the seventh most frequent cancer worldwide, with
squamous cell carcinomas as the most frequent histologic subtype. Standard treatment for …

To date, five cancer treatment modalities have been defined. The three traditional modalities
of cancer treatment are surgery, radiotherapy, and conventional chemotherapy, and the two …

MAP kinase-interacting kinases (MNK1 and MNK2) are often activated downstream of ERK
and p38 MAPK in the MAP kinase family. The role of MNKs in the development and …

Understanding protein conformational variability remains a challenge in drug discovery. The
issue arises in protein kinases, whose multiple conformational states can affect the binding …

As described in the previous chapter, most kinase inhibitors that have been developed for
use in the clinic act by blocking ATP binding; however, there is growing interest in identifying …