Category: Melanoma

Cilengitide is a Selective Integrin Inhibitor for αvβ3 and αvβ5 Receptor

Integrins are heterodimeric cell surface adhesion receptors that consist of two noncovalently associated alpha and beta subunits. In particular, Integrins are heterodimeric transmembrane proteins composed of one α and one β subunit. Especially, Integrins are crucially important because they are the main receptor proteins that cells use to bind...

SRX3207 is an Orally Active and First-in-Class Dual Syk/PI3K Inhibitor

Macrophages (MΦ) not only play a role in host defense and tumor growth, metastasis, and immunosuppression. Many studies have demonstrated that targeting the molecular pathways/signaling nodes in the MΦs that regulate the transition of protumorigenic MΦs into anti-tumorigenic MΦs will activate the immune response in cancer. Syk kinase has...

MYLS22 is a Selective Optic Atrophy 1 (OPA1) Inhibitor

Optic neuropathy is damage to the optic nerve from any cause. Specifically, damage and death of these nerve cells, or neurons, leads to characteristic features of optic neuropathy. Angiogenesis requires an internal mitochondrial membrane mitochondrial fusion protein optic atrophy 1 (OPA1). Besides, mitochondrion fusion is controlled by mitochondrion fusion...

BAY-985 is an Orally Active and ATP-Competitive TBK1/IKKε Inhibitor

The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homolog IKKε plays an important role in cellular pathways. And, as we all know, these kinases belong to the nuclear factor κB family. In this article, we will introduce a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε,...

IACS-8803 is a Cyclic Dinucleotide STING Agonist

The stimulator of interferon genes (STING) is an innate pattern recognition receptor natively exists in the endoplasmic reticulum (ER). STING has a great effect on host defense through supervising pathogenic or damage-associated nucleic acids. Since the generation of optimal adaptive anti-tumor immune responses requires the STING signal, activation of...

CCG-222740 is a Selective Rho/MRTF Pathway Inhibitor

Pancreatic cancer is one of the most lethal cancers, is characterized by a strong fibro-inflammatory reaction composed mainly of cancer-associated fibroblasts. Pancreatic stellate cells (PSCs) present in the pancreas tumor microenvironment. PSCs can excrete essential amino acids and cytokines to maintain an immunosuppressive environment. CCG-222740 is a potent and...