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 …

Abstract The RAF-MEK-ERK signaling cascade is a well-characterized MAPK pathway
involved in cell proliferation and survival. The three-layered MAPK signaling cascade is …

Abstract RAS (KRAS, NRAS and HRAS) is the most frequently mutated gene family in
cancers, and, consequently, investigators have sought an effective RAS inhibitor for more …

Generative deep learning is resha** drug design. Chemical language models (CLMs)–
which generate molecules in the form of molecular strings–bear particular promise for this …

The mitogen-activated protein kinases (MAPKs) in mammals include c-Jun NH 2-terminal
kinase (JNK), p38 MAPK, and extracellular signal-regulated kinase (ERK). These enzymes …

Abstract The RAS–RAF–MEK–ERK signalling pathway is hyperactivated in a high
percentage of tumours, most frequently owing to activating mutations of the KRAS, NRAS …

The development of therapies for the treatment of neurological cancer faces a number of
major challenges including the synthesis of small molecule agents that can penetrate the …

Drugs that function through covalent bond formation represent a considerable fraction of our
repository of effective medicines but safety concerns and the complexity of develo** …

Protein kinases have emerged as one of the most successful families of drug targets. To
date, most selective kinase inhibitors have been discovered serendipitously either through …

There are over 500 human kinases ranging from very well-studied to almost completely
ignored. Kinases are tractable and implicated in many diseases, making them ideal targets …