Sviripa, Vitaliy M.; Burikhanov, Ravshan; Obiero, Josiah M.; Yuan, Yaxia; Nickell, Justin R.; Dwoskin, Linda P.; Zhan, Chang-Guo; Liu, Chunming; Tsodikov, Oleg V.; Rangnekar, Vivek M.; Watt, David S. published the artcile< Par-4 secretion: stoichiometry of 3-arylquinoline binding to vimentin>, Computed Properties of 658-99-1, the main research area is arylquinoline preparation antitumor prostate Par4 secretion vimentin binding.
Advanced prostate tumors usually metastasize to the lung, bone, and other vital tissues and are resistant to conventional therapy. Prostate apoptosis response-4 protein (Par-4) is a tumor suppressor that causes apoptosis in therapy-resistant prostate cancer cells by binding specifically to a receptor, Glucose-regulated protein-78 (GRP78), found only on the surface of cancer cells. 3-Arylquinolines or “”arylquins”” induce normal cells to release Par-4 from the intermediate filament protein, vimentin and promote Par-4 secretion that targets cancer cells in a paracrine manner. A structure-activity study identified arylquins that promote Par-4 secretion, and an evaluation of arylquin binding to the hERG potassium ion channel using a [3H]-dofetilide binding assay permitted the identification of structural features that separated this undesired activity from the desired Par-4 secretory activity. A binding study that relied on the natural fluorescence of arylquins and that used the purified rod domain of vimentin (residues 99-411) suggested that the mechanism behind Par-4 release involved arylquin binding to multiple sites in the rod domain.
Organic & Biomolecular Chemistry published new progress about Antitumor agents. 658-99-1 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H5F2N, Computed Properties of 658-99-1.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts