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・ Discovery Airways
・ Discovery and Configuration Protocol
・ Discovery and development of ACE inhibitors
・ Discovery and development of angiotensin receptor blockers
・ Discovery and development of antiandrogens
・ Discovery and development of beta-blockers
・ Discovery and development of beta2 agonists
・ Discovery and development of cephalosporins
・ Discovery and development of cyclooxygenase 2 inhibitors
・ Discovery and development of direct thrombin inhibitors
・ Discovery and development of gliflozins
・ Discovery and development of HIV-protease inhibitors
・ Discovery and development of integrase inhibitors
・ Discovery and development of matrix metalloproteinase inhibitors
・ Discovery and development of memantine and related compounds
Discovery and development of neuraminidase inhibitors
・ Discovery and development of non-nucleoside reverse-transcriptase inhibitors
・ Discovery and development of nucleoside and nucleotide reverse-transcriptase inhibitors
・ Discovery and development of phosphodiesterase 5 inhibitors
・ Discovery and development of proton pump inhibitors
・ Discovery and development of statins
・ Discovery and development of steroidal aromatase inhibitors
・ Discovery and development of triptans
・ Discovery and development of TRPV1 antagonists
・ Discovery and development of tubulin inhibitors
・ Discovery and exploration of the Solar System
・ Discovery and Launch
・ Discovery Arcade (Disneyland Paris)
・ Discovery Atlas
・ Discovery Aviation Model 201


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Discovery and development of neuraminidase inhibitors : ウィキペディア英語版
Discovery and development of neuraminidase inhibitors

Neuraminidase inhibitors inhibit enzymatic activity of the enzyme neuraminidase (sialidase). These type of inhibitors have been introduced as anti-influenza drugs as they prevent the virus from exiting infected cells and thus stop further spreading of the virus. Neuraminidase inhibitors for human neuraminidase (hNEU) have the potential to be useful drugs as the enzyme plays a role in several signaling pathways in cells and is implicated in diseases such as diabetes and cancer.〔Christopher W. Cairo. (2014) Inhibitors of the human neuraminidase enzymes. ''Med. Chem. Commun''., 2014, 5, 1067.DOI: 10.1039/c4md00089g〕
== History ==

The first neuraminidase Inhibitors (NAIs) were synthesized in 1960s by Edmond et al.,〔Edmond, J. D., Johnston, R. G., Kidd, D., Rylance, H. J. and Sommerville, R. G. (1966) The Inhibition Of Neuraminidase And Antiviral Action. ''Br. J. Pharmacol. Chemother''., 1966, 27: 415–426. doi: 10.1111/j.1476-5381.1966.tb01673.x〕 through an attempt to understand the catalytic mechanism of the neuraminidase enzyme. They discovered that N-substituted oxamic acids had enzyme inhibitory properties. Then it was found that the synthetic compound 2-deoxy-2,3-didehydro-N-acetylneuraminic acid (Neu5Ac2en or DANA) which is an analogue of N-acetylneuraminic acid (Neu5Ac), inhibits the release of virus progeny in tissue culture but no antiviral activity in animals was detected.〔Kim, Choung U, Xiaowu Chen, and Dirk B Mendel. Neuraminidase inhibitors as anti-influenza virus agents. ''Antiviral chemistry & chemotherapy'' 10.4 (1999): 41-154〕〔von Itzstein, Mark. The war against influenza: discovery and development of sialidase inhibitors. ''Nature reviews Drug discovery'' 6.12 (2007): 967-974〕
In early 1990s, the determination of biological crystal structure of influenza virus surface protein led to the discovery of the active site and provided the opportunities to discover and design new and specific inhibitors.

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