The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …

Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …

Binding kinetic parameters can be correlated with drug efficacy, which in recent years led to
the development of various computational methods for predicting binding kinetic rates and …

A dominant assumption in pharmacology throughout the 20th century has been that in vivo
target occupancy—and attendant pharmacodynamics—depends on the systemic …

Focal adhesion kinase (FAK, also known as PTK2) is a tyrosine kinase that regulates
integrin and growth factor signaling pathways and is involved in the migration, proliferation …

The prediction of drug–target binding and unbinding kinetics that occur on time scales
between milliseconds and several hours is a prime challenge for biased molecular …

Target residence time plays a crucial role in the pharmacological activity of small molecule
inhibitors. Little is known, however, about the underlying causes of inhibitor residence time …

The cervix is the lowermost part of the uterus that connects to the vagina, and cervical
cancer is a malignant cervix tumour. One of this cancer's most important risk factors is HPV …

There is a growing appreciation of the importance of drug-target binding kinetics for lead
optimization. For G protein-coupled receptors (GPCRs), which mediate signaling over a …

Kinases are the ideal druggable targets for diseases and especially were highlighted on
cancer therapy. Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase and its …