Category: Melanoma

Piclidenoson is a First-in-Class and Orally Active A3AR Agonist

One of the main strategies for cancer research is the identification of drugs that can cause apoptotic death in malignant cells. Additionally, Adenosine 5′-triphosphate (ATP), UTP, and adenosine are considered that inhibit the growth of several cancerous cell lines. Adenosine has several physiological and pharmacological functions. It can modulate...

ML786 is an Orally Bioavailable Raf Inhibitor

The mitogen-activated protein kinase (MAPK) signal pathway plays an important role in cells. It also has a response to many different external stimuli and regulates cellular growth, proliferation. The Raf isoform B-Raf is one component of this pathway. Besides, it has a high rate of activating mutation in melanoma...

NHWD-870 is an Orally Active and Selective BET Bromodomain Inhibitor

Brominedomain can recognize acetylated lysine residues. As the “reader” of lysine acetylation, the bromine domain is responsible for the transduction of signals carried by acetylated lysine residues and transforming them into various normal or abnormal phenotypes. Specifically, the bromine domain-containing proteins have a variety of functions. Besides, it ranges...

VERU-111 is an Orally Bioavailable α and β Tubulin Inhibitor

Tubulins play a major role in cell dynamics, thus are important molecular targets for cancer therapy. VERU-111 preferentially represses clinically important, βIII and βIV tubulin isoforms via restoring the expression of miR-200c. VERU-111 (ABI-231) displays optimum activity and has an average IC50 value of 5.2 nM against a large...

PQR530 is an Orally Active and Brain-Penetrant Dual PI3K, mTORC1/2 Inhibitor

Several brain disorders, such as epilepsy, found dysregulation of the PI3K/Akt/mTOR pathway. The PI3K-AKT/mTOR pathway is a central player of intracellular signaling, regulating neuronal survival, growth, and plasticity. Aberrant activation of this signaling pathway drives the progression of malignant tumors. The mutation of growth factor receptors, PI3K, loss of...

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...