Tranilast inhibits the expression of genes related to epithelial-mesenchymal transition and angiogenesis in neurofibromin-deficient cells was written by Harigai, Ritsuko;Sakai, Shigeki;Nobusue, Hiroyuki;Hirose, Chikako;Sampetrean, Oltea;Minami, Noriaki;Hata, Yukie;Kasama, Takashi;Hirose, Takanori;Takenouchi, Toshiki;Kosaki, Kenjiro;Kishi, Kazuo;Saya, Hideyuki;Arima, Yoshimi. And the article was included in Scientific Reports in 2018.Formula: C18H17NO5 This article mentions the following:
Neurofibromatosis type 1 (NF1) is caused by germline mutations in the NF1 gene and is characterized by cafe au lait spots and benign tumors known as neurofibromas. NF1 encodes the tumor suppressor protein neurofibromin, which neg. regulates the small GTPase Ras, with the constitutive activation of Ras signalling resulting from NF1 mutations being thought to underlie neurofibroma development. We previously showed that knockdown of neurofibromin triggers epithelial-mesenchymal transition (EMT) signalling and that such signalling is activated in NF1-associated neurofibromas. With the use of a cell-based drug screening assay, we have now identified the antiallergy drug tranilast (N-(3,4-dimethoxycinnamoyl) anthranilic acid) as an inhibitor of EMT and found that it attenuated the expression of mesenchymal markers and angiogenesis-related genes in NF1-mutated sNF96.2 cells and in neurofibroma cells from NF1 patients. Tranilast also suppressed the proliferation of neurofibromin-deficient cells in vitro more effectively than it did that of intact cells. In addition, tranilast inhibited sNF96.2 cell migration and proliferation in vivo. Knockdown of type III collagen (COL3A1) also suppressed the proliferation of neurofibroma cells, whereas expression of COL3A1 and SOX2 was increased in tranilast-resistant cells, suggesting that COL3A1 and the transcription factor SOX2 might contribute to the development of tranilast resistance. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Formula: C18H17NO5).
2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.Formula: C18H17NO5
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics