Pyridones have been utilized as privileged scaffolds in drug discovery. Some of the
important roles where this class of heterocycles have found utility in medicinal chemistry …

Malignant carcinomas are often characterized by metastasis, the movement of carcinoma
cells from a primary site to colonize distant organs. For metastasis to occur, carcinoma cells …

Abstract The p21-Activated kinase 1 (PAK1), a member of serine-threonine kinases family,
was initially identified as an interactor of the Rho GTPases RAC1 and CDC42, which affect a …

The p21-activated kinases (PAKs), downstream effectors of Ras-related Rho GTPase Cdc42
and Rac, are serine/threonine kinases. Biologically, PAKs participate in various cellular …

CDC42 GTPases (RHOJ, CDC42, and RHOQ) are overexpressed in multiple tumor types
and activate pathways critical for tumor growth, angiogenesis, and metastasis. Recently, we …

In the current work, we designed and synthesized three families of non-fused and fused
compounds based on cyanopyridone: derivatives of 6-amino-1, 2-dihydropyridine-3, 5 …

Small GTPases of the RAS and RHO families are related signaling proteins that, when
activated by growth factors or by mutation, drive oncogenic processes. While activating …

p21-Activated kinase 1 (PAK1) has attracted much attention as a potential therapeutic target
due to its central role in many oncogenic signaling pathways, its frequent dysregulation in …

Alchemical free-energy methods based on molecular dynamics (MD) simulations have
become important tools to identify modifications of small organic molecules that improve …

Salt-inducible kinases (SIKs) are key metabolic regulators. The imbalance in SIK function is
associated with the development of diverse cancers, including breast, gastric, and ovarian …