Nimotuzumab is a Humanized IgG1 Monoclonal Antibody Targeting EGFR

The epidermal growth factor receptor (EGFR) is a transmembrane protein. The dimerization of EGFR stimulates the activity of intracellular protein tyrosine kinase. Therefore, several tyrosine (y) residues in the C-terminal domain of EGFR undergo autophosphorylation. These include y992, y1045, y1068, y1148, and y1173, as shown in the adjacent chart....

XY028-140 is a Selective CDK4 and CDK6 PROTAC Degrader

CDKs (Cyclin-dependent kinases) are the families of protein kinases first discovered for their role in regulating the cell cycle. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase. The four major mechanisms...

GGTI-2154 is a Selective Geranylgeranyltransferase I (GGTase I) Inhibitor

The Ras superfamily of low molecular weight GDP/GTP-binding GTPases is critical in the regulation of many important biological events. They include the cell division cycle, survival and death, differentiation, and development. These GTPases also show a relation with oncogenesis, Ras and Rho proteins mediate malignant transformation, invasion, and metastasis....

Inupadenant is an Orally Active and Highly Selective A2A Receptor Antagonist

Adenosine receptors (AR), including P1 purinergic receptors, belong to G protein-coupled receptors (GPCR). Specifically, Adenosine is an autogenous acid in all tissues and body fluids. Besides, AR contains four subtypes, A1, A2A, A2B, and A3. They are activated by extracellular adenosine and play a central role in a wide...

ABBV-744 is a First-in-Class, Orally Active and Selective BET BDII Inhibitor

The proteins of BET (bromodomain and extra-terminal) domain family are epigenetic readers. BET domain family proteins bind acetylated histones through their bromodomains to regulate gene transcription. BET domain family proteins consist of BRD2, BRD3, BRD4 and BRDT. They contain BDI, BDII and the extra-terminal (ET) domain. Interestingly, BDII of...

DP-C-4 is a CRBN-Based dual PROTAC for EGFR and PARP

Proteolysis targeting chimera (PROTAC) is a bifunctional small molecule. Interestingly, dual PROPACs are dual-targeted degradation molecules that combine the concepts of PROTAC and dual-targeting. Dual PROPACs degrade two completely different pathway targets while simultaneously taking advantage of both PROTAC and dual-target drugs. Thus, dual PROPACs not only achieve the...

SJ6986 is a Selective and Orally Active GSPT1/2 Degrader

Targeted protein degradation (TPD) is a novel chemical biology approach. Molecular glues (MGs) are small molecules that can bind to E3 ligase and change their surface and specificity, leading to the recruitment, ubiquitination, and subsequent degradation of substrates that are normally not targeted by the ligase (neosubstrates). Immunomodulatory imide...