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  • Title: [Introduction of mutations in insulin molecule: positive and negative mutations].
    Author: Ksenofontova OI.
    Journal: Biomed Khim; 2014; 60(4):430-7. PubMed ID: 25249526.
    Abstract:
    Introduction of mutations in an insulin molecule is one of the important approaches to drug development for treatment of diabetes mellitus. Generally, usage of mutations is aimed at activation of insulin and insulin receptor interaction. Such mutations can be considered as positive. Mutations that reduce the binding efficacy are negative. There are neutral mutations as well. This article considers both natural mutations that are typical for various members of the insulin superfamily and artificial ones which are introduced to improve the insulin pharmacological characteristics. Data presented here can be useful in developing new effective insulin analogues for treatment of diabetes mellitus. Vvedenie mutatsiĭ v molekulu insulina iavliaetsia odnim iz vazhneĭshikh podkhodov pri razrabotke lekarstv dlia lecheniia sakharnogo diabeta. Kak pravilo, ispol'zovanie mutatsiĭ napravleno na aktivizatsiiu vzaimodeĭstviia insulina i insulinovogo retseptora. Takie mutatsii mozhno nazvat' “polozhitel'nymi”. Mutatsii, snizhaiushchie éffektivnost' sviazyvaniia, iavliaiutsia “otritsatel'nymi”. Takzhe sushchestvuiut neĭtral'nye mutatsii. V dannoĭ stat'e rassmatrivaiutsia kak estestvennye mutatsii, kharakternye dlia razlichnykh predstaviteleĭ insulinovogo supersemeĭstva, tak i iskusstvennye mutatsii, vvedenie kotorykh sposobstvuet uluchsheniiu farmakologicheskikh kharakteristik insulina. Dannye, obobshchennye v étoĭ stat'e, mogut byt' polezny pri razrabotke novykh éffektivnykh analogov insulina dlia lecheniia sakharnogo diabeta.
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