Tag: Cell-cycle

NU6102 is a Potent CDK1 and CDK2 Inhibitor

CDKs remain attractive targets for anti-proliferative cancer chemotherapy. they play a central role in cell division and growth.  Amongst the cell cycle CDKs, CDK2 has attracted the most attention and its exploitation as a drug target based on structure-based drug design. In this article, we will introduce a potent...

Afatinib is an Irreversible and Orally Active EGFR Family Inhibitor

Lung cancer continues to be the leading cause of cancer-related mortality. Members of the ERBB receptor tyrosine kinase family include EGFR, HER2, HER3, and HER4. They present an attractive option for targeted therapy in patients with NSCLC, due to observed patterns of oncogenic mutation of EGFR and HER2. In addition, esophageal...

HJC0416 is a Highly Potent and Orally Active STAT3 Inhibitor

Signal transducer and activator of transcription 3 (STAT3) is involved in the regulation of early embryonic development, angiogenesis, immune response, cell proliferation, and apoptosis. Additionally, STAT3 overexpresses in many cancers. As a result, it becomes an attractive therapeutic target for various cancer treatment studies. However, despite much intensive researches...

ZINC69391 is a Specific Rac1 Inhibitor and Apoptosis Inducer

Rho-GTPases are molecular switches that cycle between an inactive GDP-bound form and an active GTP-bound form. Guanine nucleotide exchange factors (GEFs) catalyze nucleotide exchange and mediate activation in this cycle, While GTPase-activating proteins (GAPs) stimulate GTP hydrolysis and inactivate the GTPase. Only the active GTP-bound state binds to downstream...

LCH-7749944 is a Potent PAK4 Inhibitor and Induces Apoptosis

P21-activated kinase 4 (PAK4) is a serine/threonine protein kinase and has related to the regulation of cytoskeleton recombine, cell proliferation, gene transcription, carcinogenic transformation, cell invasion. Moreover, PAK4 overexpression, mutations, genetic amplification were detected in a variety of human tumors, making it a potential therapeutic target. Specifically, The p21-activated kinases...

Ro 90-7501, a Radiosensitizer, is an Aβ42 Fibril Assembly and PP5 Inhibitor

Cervical cancer is one of the most common cancers among women worldwide. Ro 90-7501 is an inhibitor of the amyloid β42 (Aβ42) fibril assembly. It is associated with Alzheimer’s disease. The usual method for Cervical cancer treatment is Radiotherapy, especially for locally advanced cancer. However, the treatment results are...

SD-36 is a Selective PROTAC STAT3 Degrader

Proteolysis targeting chimera (PROTAC) technology has been a type of therapeutics that induces targeted protein degradation. Signal transducer and activator of transcription 3 (STAT3) is an attractive cancer therapeutic target. In this study, Longchuan Bai, et al developed a potent and specific PROTAC degrader of STAT3 and evaluate its...