Month: May 2022

Marimastat (BB2516) is a Broad Spectrum and Orally Active Inhibitor of MMPs

Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs (Matrix metalloproteinases). Marimastat (BB2516) is an angiogenesis and metastasis inhibitor, which limits the growth and production of blood vessels. Besides, As an antimetastatic agent, it prevents malignant cells from breaching the basement membranes. Marimastat (BB2516) shows potent...

Namodenoson (CF-102) is a Selective A3 Adenosine Receptor (A3AR) Agonist

The adenosine A3 receptor (A3AR) comes from the cloning from rat, sheep and human sources. In vitro stimulation of this adenosine receptor subtype shows it inhibits adenylyl cyclase. It also stimulates phospholipase C and inositol-1,4,5-triphosphate (IP3) will form. In vivo activation of the A3 receptor, it also mediates heart...

Temoporfin is a Secondā€generation Photosensitizer for Cancer

Photodynamic therapy (PDT), a phototherapy, is a minimally invasive therapeutic procedure. PDT consists of three essential components-photosensitizer, light and oxygen. None of these is individually toxic, but together they initiate a photochemical reaction that culminates in the generation of a highly-reactive product termed singlet oxygen. Singlet oxygen can rapidly...

Seliciclib (Roscovitine) is an Orally Active and Selective CDKs Inhibitor

Cyclin-dependent kinases (CDKs) are serine/threonine kinases whose activity depends on a regulatory subunit-a cyclin. Based on the sequence of the kinase domain, CDKs belong to the CMGC group of kinases, along with MAPKs, Gsk3β, DYRK family and CDK-like kinases. There are around 20 Cyclin-dependent kinases (CDK1-20) known till date....

Vistusertib (AZD2014) is an ATP Competitive mTOR Inhibitor

mTOR is an atypical serine threonine kinase involved in regulating major cellular functions, such as nutrients sensing, growth, and proliferation. mTOR is part of the multiprotein complexes mTORC1 and mTORC2. mTORC1 and mTORC2 have been shown to play critical yet functionally distinct roles in the regulation of cellular processes....

Epoxomicin is a Selective and Irreversible Inhibitor of Proteasome

Epoxomicin (BU-4061T) is a potent, selective and irreversible proteasome inhibitor. Epoxomicin can cross the blood-brain barrier and has strongly antitumor and anti-inflammatory activity. Proteasome is a 700 kDa, cylindrical-shaped multicatalytic protease complex. It has 28 subunits and organizes into four rings. Besides, Eukaryote 20S proteasome has three major proteolytic...

5-Azacytidine, a Nucleoside Analogue of Cytidine, Inhibits DNA Methylation

In the mammalian genome, DNA methylation is an epigenetic mechanism involving the transfer of a methyl group onto the C5 position of the cytosine to form 5-methylcytosine. DNA methylation regulates gene expression by recruiting proteins involved in gene repression or by inhibiting the binding of transcription factor(s) to DNA....