Category: Breast Cancer

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....

GL0388 Activates Bax and Induce Bax-Mediated Apoptosis

Bax is a member of the bcl-2 gene family. Specifically, BCL2 family members are relevant to a variety of anti-apoptotic or pro-apoptotic regulators. The expression of this gene is regulated by the tumor suppressor gene p53. Besides, Bax interacts with mitochondrial voltage-dependent anion channel VDAC and induces its opening....

Proxalutamide (GT0918) is a Potent Androgen Receptor (AR) Antagonist

Androgen receptors (ARs) mediate cell differentiation and development of prostate cancer. The target is a common therapeutic target in prostate cancer. Proxalutamide (GT0918) design is based on the core structure of MDV3100 but is optimized by computer-aided design. It is an innovative compound for prostate cancer and advanced breast...

Capivasertib (AZD5363) is an Orally Active pan-AKT Kinase Inhibitor

Akt/PKB (Protein kinase B), usually called Akt, is a serine/threonine protein kinase with antiapoptotic activity. In addition, Akt consists of three isoforms: PKBα/Akt1, PKBβ/Akt2 and PKBγ/Akt3. Catalytically active Akt regulates the function of numerous substrates involved in cell survival, growth, proliferation, metabolism and protein synthesis. Akt possesses a protein...

Venadaparib (IDX-1197) is a Potent and Selective PARP Inhibitor

PARP is an enzyme that involved in a number of cellular processes such as DNA repair, and programmed cell death. The PARP family comprises 17 members. They have all very different structures and functions in the cell. Importantly, the main role is to detect and signal single-strand DNA breaks...

Motesanib is a potent ATP-Competitive Inhibitor of VEGFR1/2/3

There are numerous growth factors involved in tumor angiogenesis, but foremost among them is the family of vascular endothelial growth factors (VEGFs). The VEGF family includes VEGFA, VEGFB, VEGFC, VEGFD, and placenta growth factor (PGF). These ligands bind with different affinities to three endothelial receptor tyrosine kinases (RTKs), such...

NCGC00378430 is a Potent SIX1/EYA2 Interaction Inhibitor

The Sine oculis homeobox homolog 1 (SIX1)/eyes absent (EYA) transcription complex plays a key role in the development of multiple organs. Specifically, members of the SIX gene family encode proteins characterized by different DNA binding homologous domains and upstream six domains. This may involve determining DNA binding specificity and...