Ahren B. GLP-1-based therapy of type 2 diabetes: GLP-1 mimetics and DPP-IV inhibitors. Curr.Diab.Rep. 2007; 7:340-347.Ahren B. GLP-1-Based Therapy of Type 2 Diabetes: GLP-1 Mimetics and DPP-IV Inhibitors. Curr
in 2009 offered a place for GLP-1 receptor agonists after failure of metformin treatment, as an alternative to sulfonylureas or a basal insulin (considered as the first choice) or as an alternative to pioglitazone (as a second-choice), while no place was retained for DPP-4 inhibitors [57]...
Dipeptidyl peptidase-4 (DPP-4) inhibitors (from now on DPP-4i) are newly available drugs approved for the treatment of type 2 diabetes mellitus, either as monotherapy or in combination with oral agents (metformin, glitazones, and/or sulphonylureas) and insulin (Drucker and Nauck, 2006). ...
DPP-4 has two domains and two subdomains: α/β hydrolase domain (Gln508-Pro766), β-propeller domain (Arg54-Asn497), receptor binding subdomain, and a core subdomain [15]. DPP-4 was first identified as CD26, and is a 110 kD protein that can be found on the cell surface as a ...
[6] 0 1 2 3 Next Section Medscape Diabetes © 2007 Medscape Cite this: GLP Agonists and DPP-IV Inhibitors - Medscape - Aug 10, 2007. Introduction GLP Agonists DPP-IV Inhibitors References CommentsWhat to Read Next on Medscape Recommended Reading Choosing Which Agents to Use in ...
GLP-1有两种活性方式即GLP-1(7-36)酰胺和GLP-1(7-37),其中几乎所有从人类肠道分泌的GLP-1都是酰胺化的,在部分动物如啮齿类和猪体内分泌的是GLP-1(7-37)(2)。DPP-4,也被称为CD26,是一种丝氨酸蛋白酶,它专门从寡肽或蛋白质的氨基端切割二肽,在2号位含有丙氨酸或脯氨酸残基的蛋白质,从而修改或抑制其...
Dr. Pratley discussed the role of DPP-IV inhibitors in the treatment of diabetes. Both GLP-1 and GIP have the amino acid alanine in the second N-terminal position, leading to inactivation by DPP-IV. It is interesting that more than half of secreted GLP-1 is degraded by local DPP-IV ...
DPP-4 inhibitors repress NLRP3 inflammasome and interleukin-1beta via GLP-1 receptor in macrophages through protein kinase C pathway. Cardiovasc Drugs Ther. 2014;28:425–32. Article CAS PubMed Google Scholar Zhuge F, Ni Y, Nagashimada M, Nagata N, Xu L, Mukaida N, et al. DPP-4 ...
阿必鲁肽是两个GLP-1分子的头尾串联,其中第一个分子的C-端与第二个分子的N-端融合。两个GLP-1分子中每一个DPP-4敏感位点均被甘氨酸取代。第二个GLP-1的C-端共价融合于人白蛋白,从而减缓肾脏清除率,并将人体内的半衰期延长至约120h[33],支持每周给...
GLP-1 receptors (GLP-1R) are expressed in the pancreas, heart, brain, lungs, renal proximal tubules, and glomeruli [11, 12]. GLP-1 and dipeptidyl-peptidase 4 (DPP-4) inhibitors can protect against proteinuria and renal disease progression. However, the precise role of renal GLP-1R in ...