Month: May 2021

Trilaciclib is an Orally Active CDK4 and CDK6 Inhibitor

The cell cycle is a highly conserved process. Additionally, this process must maintain genomic integrity and replicative capacity for proper cell maintenance and proliferation. The cell cycle consists of four distinct phases: G1 or Gap1 phase, G2 or Gap2 phase, and M phase. As we all know, the G1...

Lenalidomide, a Ligand of CRBN, is an Orally Active Immunomodulator

Immunomodulatory imide drugs (IMiDs) are a class of immunomodulatory drugs containing an imide group. The discovery of anti-angiogenic and anti-inflammatory properties promoted the development of Thalidomide analogs. These compounds bind Cereblon (CRBN), the substrate adaptor for the CRBN-CRL4 E3 ubiquitin ligase, and modulate the substrate specificity of the enzyme....

FTI-277 is a Farnesyl Transferase (FTase) Inhibitor

Farnesyl transferase (FTase) is a zinc-dependent enzyme. It adds a 15-carbon isoprenoid called a farnesyl group to proteins bearing a CaaX motif. FTase regulates the activation of oncogenic Ras protein and consequently affects intracellular signal transduction, and cell proliferation. Ras-induced malignant transformation requires Ras farnesylation, a lipid posttranslational modification...

Lonafarnib is an Orally Active FPTase Inhibitor

Farnesyl transferase (FTase) is a zinc-dependent enzyme, which coordinates a zinc cation on its β subunit at the lip of the active site. FTase has two subunits: a 48kDa α-subunit and a 46kDa β-subunit. And it adds a 15-carbon isoprenoid called a farnesyl group to proteins bearing a CaaX...

DT-061 is an Orally Active PP2A Activator

Protein phosphatase 2A (PP2A) comprises a family of serine/threonine phosphatases, minimally containing a well-conserved catalytic subunit. PP2A plays a prominent role in the regulation of specific signal transduction cascades. Additionally, PP2A interacts with a substantial number of other cellular and viral proteins. DT-061 is an orally bioavailable small-molecule activator...

GSK973 is a Highly Selective BET BD2 Inhibitor

The bromodomain and extra-terminal (BET) family of proteins are epigenetic readers of chromatin. The two tandem bromodomains (BD1 and BD2) of each of the four proteins (BRD2, 3, 4, and T) recognize and bind to specific acetylated-lysine residues of histone tails and non-histone proteins. They play a major role...