2型糖尿病药物的起源

IF 0.4 Q4 ENDOCRINOLOGY & METABOLISM British Journal of Diabetes Pub Date : 2022-12-21 DOI:10.15277/bjd.2022.388
Clifford J Bailey
{"title":"2型糖尿病药物的起源","authors":"Clifford J Bailey","doi":"10.15277/bjd.2022.388","DOIUrl":null,"url":null,"abstract":"The origins of diabetes medications provide an intriguing catalogue of clinical serendipity and scientific design. Use of insulin (beyond 1922) gave recognition to insulin resistance and the categorisation of type 2 diabetes (T2DM). The first sulphonylurea (carbutamide, 1956) emerged from its use as an antibacterial sulphonamide prone to cause hypoglycaemia, and biguanides were first used to treat diabetes in 1957 despite their glucose-lowering properties having been known since the 1920s. Alpha-glucosidase inhibitors arose from a screening programme for amylase inhibitors by Bayer in the 1970s and acarbose was introduced in 1990. The first thiazolidinedione (ciglitazone; not developed) was identified in a screening programme for triglyceride-lowering compounds by Takeda in the late 1970s and gave rise to pioglitazone (approved 1999), although first to market was troglitazone (from Warner Lambert 1997, withdrawn 2000). Exendin, an analogue of the incretin hormone glucagon-like peptide-1 (GLP-1), was identified in 1992 in the saliva of a lizard (Heloderma suspectum), and took until 2005 to be marketed as exenatide. To promote the efficacy of endogenous GLP-1, its rapid inactivation by the enzyme dipeptidylpeptidase-4 (DPP4) was blocked by clever molecular design of the first DPP4 inhibitors (vildagliptin and sitagliptin, approved in 2006). SGLT2 inhibitors are based on phlorizin, identified in apple tree bark (1835) and modified (2000) to avoid intestinal degradation: further modifications to increase selectivity against SGLT2 gave dapagliflozin and canagliflozin - approved 2012 and 2013, respectively, in Europe.","PeriodicalId":42951,"journal":{"name":"British Journal of Diabetes","volume":null,"pages":null},"PeriodicalIF":0.4000,"publicationDate":"2022-12-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"origins of type 2 diabetes medications\",\"authors\":\"Clifford J Bailey\",\"doi\":\"10.15277/bjd.2022.388\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The origins of diabetes medications provide an intriguing catalogue of clinical serendipity and scientific design. Use of insulin (beyond 1922) gave recognition to insulin resistance and the categorisation of type 2 diabetes (T2DM). The first sulphonylurea (carbutamide, 1956) emerged from its use as an antibacterial sulphonamide prone to cause hypoglycaemia, and biguanides were first used to treat diabetes in 1957 despite their glucose-lowering properties having been known since the 1920s. Alpha-glucosidase inhibitors arose from a screening programme for amylase inhibitors by Bayer in the 1970s and acarbose was introduced in 1990. The first thiazolidinedione (ciglitazone; not developed) was identified in a screening programme for triglyceride-lowering compounds by Takeda in the late 1970s and gave rise to pioglitazone (approved 1999), although first to market was troglitazone (from Warner Lambert 1997, withdrawn 2000). Exendin, an analogue of the incretin hormone glucagon-like peptide-1 (GLP-1), was identified in 1992 in the saliva of a lizard (Heloderma suspectum), and took until 2005 to be marketed as exenatide. To promote the efficacy of endogenous GLP-1, its rapid inactivation by the enzyme dipeptidylpeptidase-4 (DPP4) was blocked by clever molecular design of the first DPP4 inhibitors (vildagliptin and sitagliptin, approved in 2006). SGLT2 inhibitors are based on phlorizin, identified in apple tree bark (1835) and modified (2000) to avoid intestinal degradation: further modifications to increase selectivity against SGLT2 gave dapagliflozin and canagliflozin - approved 2012 and 2013, respectively, in Europe.\",\"PeriodicalId\":42951,\"journal\":{\"name\":\"British Journal of Diabetes\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.4000,\"publicationDate\":\"2022-12-21\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"British Journal of Diabetes\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.15277/bjd.2022.388\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"ENDOCRINOLOGY & METABOLISM\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"British Journal of Diabetes","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.15277/bjd.2022.388","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"ENDOCRINOLOGY & METABOLISM","Score":null,"Total":0}
引用次数: 0

摘要

糖尿病药物的起源提供了一个有趣的临床偶然性和科学设计目录。胰岛素的使用(1922年以后)使人们认识到胰岛素抵抗和2型糖尿病(T2DM)的分类。第一个磺脲类药物(carbutamide, 1956年)是作为一种容易引起低血糖的抗菌磺胺类药物而出现的,而双胍类药物在1957年首次被用于治疗糖尿病,尽管它们的降血糖特性早在20世纪20年代就已为人所知。α -葡萄糖苷酶抑制剂起源于20世纪70年代拜耳公司对淀粉酶抑制剂的筛选计划,阿卡波糖于1990年引入。第一噻唑烷二酮(西格列酮;(未开发)在20世纪70年代末武田在一个降低甘油三酯化合物的筛选项目中发现,并产生了吡格列酮(1999年批准),尽管首先上市的是曲格列酮(1997年来自Warner Lambert, 2000年撤回)。Exendin是一种胰高血糖素样肽-1 (GLP-1)的类似物,于1992年在蜥蜴(Heloderma suectum)的唾液中被发现,直到2005年才以艾塞那肽的名称上市。为了提高内源性GLP-1的疗效,通过巧妙的分子设计,首批DPP4抑制剂(2006年批准的维格列汀和西格列汀)阻断了其被二肽基肽酶-4 (DPP4)快速失活的过程。SGLT2抑制剂的基础是在苹果树皮中发现的phlorizin(1835年),并进行了修饰(2000年)以避免肠道降解:进一步修饰以增加对SGLT2的选择性,使达格列净和卡格列净分别于2012年和2013年在欧洲获得批准。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
origins of type 2 diabetes medications
The origins of diabetes medications provide an intriguing catalogue of clinical serendipity and scientific design. Use of insulin (beyond 1922) gave recognition to insulin resistance and the categorisation of type 2 diabetes (T2DM). The first sulphonylurea (carbutamide, 1956) emerged from its use as an antibacterial sulphonamide prone to cause hypoglycaemia, and biguanides were first used to treat diabetes in 1957 despite their glucose-lowering properties having been known since the 1920s. Alpha-glucosidase inhibitors arose from a screening programme for amylase inhibitors by Bayer in the 1970s and acarbose was introduced in 1990. The first thiazolidinedione (ciglitazone; not developed) was identified in a screening programme for triglyceride-lowering compounds by Takeda in the late 1970s and gave rise to pioglitazone (approved 1999), although first to market was troglitazone (from Warner Lambert 1997, withdrawn 2000). Exendin, an analogue of the incretin hormone glucagon-like peptide-1 (GLP-1), was identified in 1992 in the saliva of a lizard (Heloderma suspectum), and took until 2005 to be marketed as exenatide. To promote the efficacy of endogenous GLP-1, its rapid inactivation by the enzyme dipeptidylpeptidase-4 (DPP4) was blocked by clever molecular design of the first DPP4 inhibitors (vildagliptin and sitagliptin, approved in 2006). SGLT2 inhibitors are based on phlorizin, identified in apple tree bark (1835) and modified (2000) to avoid intestinal degradation: further modifications to increase selectivity against SGLT2 gave dapagliflozin and canagliflozin - approved 2012 and 2013, respectively, in Europe.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
British Journal of Diabetes
British Journal of Diabetes ENDOCRINOLOGY & METABOLISM-
自引率
16.70%
发文量
15
期刊最新文献
qualitative study of the experiences of individuals who did not complete the NHS Low Calorie Diet Programme Pilot fresh start with high hopes: a qualitative evaluation of experiences of the Total Diet Replacement phase of the NHS Low Calorie Diet Programme pilot Supporting remission of type 2 diabetes in the real world Re:Mission study. Evaluating the NHS Low Calorie Diet pilot - an overview of service user data collection methods Participant experiences during the NHS Low Calorie Diet Programme pilot. Findings from an online survey
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1