Discovery of 2-aryl and 2-pyridinylbenzothiazoles endowed with antimicrobial and aryl hydrocarbon receptor agonistic activities

Synthesis and Antimicrobial Activities of His(2-aryl)-Arg and Trp-His(2-aryl) Classes of Dipeptidomimetics.

In this communication, we report the design, synthesis and in vitro antimicrobial activity of ultra short peptidomimetics. Besides producing promising antibacterial activities against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA), the dipeptidomimetics exhibited high antifungal activity against C. neoformans with IC50 values in the range of 0.16-19 μg/mL. The most potent anal...

Aryl Hydrocarbon Receptor Activation

Aryl Hydrocarbon Receptor and Stem Cells

From the biochemical point of view, the aryl hydrocarbon receptor (AHR) is a highly conserved, developmentally regulated, and ligand-activated member of the bHLH/PAS family of transcription factors. The AHR was originally discovered because of the human and animal toxicity of its most potent and persistent ligand, 2,3,7,8-tetrachlorodibenzo-pdioxin, usually just referred to as “dioxin.” The can...

Aryl hydrocarbon receptor and lung cancer.

The leading cause of lung cancer is exposure to cigarette smoke and other environmental pollutants, which include formaldehyde, acrolein, benzene, dioxin, and polycyclic aromatic hydrocarbons (PAHs). PAHs and dioxins are exogenous ligands that directly bind to the aryl hydrocarbon receptor (AhR), a transcription factor that activates xenobiotic metabolism, histone modification (an important ste...

The Aryl Hydrocarbon Receptor and Tumor Immunity

The aryl hydrocarbon receptor (AhR) is an important cytosolic, ligand-dependent transcription factor. Emerging evidence suggests the promoting role of the AhR in the initiation, promotion, progression, invasion, and metastasis of cancer cells. Studies on various tumor types and tumor cell lines have shown high AhR expression, suggesting that AhR is activated constitutively in tumors and facilit...