DPPIV drug discovery kit    Enzo lifescience BML-AK499；二肽基肽酶 4 /二肽基肽酶IV  檢測試劑盒，*，現(xiàn)貨供應！

The DPPIV Drug Discovery Kit is a complete assay system designed to screen DPPIV inhibitors, providing enough material to perform at least 96 assays. DPPIV (DPP4, CD26) is a member of the class of proteases known as prolyl peptidases, which cleave proteins after proline residues and is thought to play roles in diabetes, cancer, and autoimmune diseases, making it a target for drug discovery.

The kit contains both a chromogenic substrate (H-Gly-Pro-pNA; K_m=114 µM) and a fluorogenic substrate (H-Gly-Pro-AMC; K_m=50 µM).

Cleavage of the p-nitroaniline (pNA) from the colorimetric substrate increases absorbance at 405 nm. The fluorimetric assay is based on the cleavage of 7-amino-4-methylcoumarin (AMC) moiety from the C-terminus of the peptide substrate, which increases its fluorescence intensity at 460 nm. The kit is useful to screen inhibitors of DPPIV, a potential therapeutic target. A DPPIV inhibitor, P32/98 (K_I=130 nM12), is included for use as a control. Other DPP enzymes are available for specificity profiling.

Product Specification

相關文獻：

Product Literature References

16, 17-Dihydro-17b-hydroxy isomitraphylline alkaloid as an inhibitor of DPP-IV, and its effect on incretin hormone and β-cell proliferation in diabetic rat: A. Shukla, et al.; Eur. J. Pharm. 47, 512 (2012), Application(s): Measurement of inhibition of DPPIV by DHIM, Abstract;

Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes: D. J. Augeri et al.; J. Med. Chem. 48, 5025 (2005), Abstract;

CD26/dipeptidyl peptidase IV and its role in cancer: B. et al.; Histol. Histopathol. 19, 1345 (2004), Abstract;

CD26/dipeptidyl peptidase IV: a regulator of immune function and a potential molecular target for therapy: U. Aytac et al.; Curr. Drug. Targets Immune Endocr. Metabol. Disord. 4, 11 (2004), Abstract;

Dipeptidyl peptidase IV inhibitors for the treatment of diabetes: A. E. Weber et al.; J. Med. Chem. 47, 4135 (2004),Abstract;

N-linked glycosylation of dipeptidyl peptidase IV (CD26): effects on enzyme activity, homodimer formation, and adenosine deaminase binding: K. Aertgeerts et al.; Protein Sci. 13, 145 (2004), Abstract;

Dipeptidyl peptidase IV (CD26) activity in the hematopoietic system: differences between the membrane-anchored and the released enzyme activity: D. A. Pereira et al.; Braz. J. Med. Biol. Res. 36, 567 (2003), Abstract;

Dipeptidyl peptidase IV inhibitor treatment stimulates beta-cell survival and islet neogenesis in streptozotocin-induced diabetic rats: J. A. Pospisilik et al.; Diabetes 52, 741 (2003), Abstract;

Prolyl peptidases: a serine protease subfamily with high potential for drug discovery: J. S. Rosenblum et al.; Curr. Opin. Chem. Biol. 7, 496 (2003), Abstract;

Structural basis of proline-specific exopeptidase activity as observed in human dipeptidyl peptidase-IV: R. Thoma et al.; Structure 11, 947 (2003), Abstract;

On the regulatory role of dipeptidyl peptidase IV (=CD=adenosine deaminase complexing protein) on adenosine deaminase activity: I. Ben-Shooshan; Biochim. Biophys. Acta. 1587, 21 (2002), Abstract;

Human serum dipeptidyl peptidase IV (DPPIV) and its unique properties: H. Shibuya-Saruta; J. Clin. Lab. Anal. 10, 435 (1996), Abstract;

Activity of dipeptidyl peptidase IV and post-proline cleaving enzyme in sera from osteoporotic patients: H. Gotoh et al.; Clin. Chem. 34, 2499 (1988), Abstract;

========================================================

二肽基肽酶(dipeptidyl peptidase ，DPP)

二肽基肽酶(dipeptidyl peptidase ，DPP)是蛋白酶家族中的脯基肽酶成員，其可剪切含脯氨酸的蛋白，其中DPPIV (DPP4, CD26),是一種絲氨酸二肽基肽酶，其剪切靶多肽（細胞趨化因子如CXCL11和肽類激素如GLP-1）N端的X-Ala or X-Pro基. CD26是一種高度保守、分布于多種細胞的，具有跨膜域和很短的胞質(zhì)域，但常被剪切和釋放作為可溶性環(huán)化4型，常形成自身二聚體或與FAP形成異二聚體。DPPⅣ的天然底物多種多樣，在體內(nèi)執(zhí)行多種重要功能。它還是細胞膜受體和共刺激分子，從而參與機體的免疫調(diào)節(jié)、細胞移行、細胞黏附和細胞調(diào)亡過程，故與多種疾病的發(fā)病有關。各種DPP-IV抑制劑對II型糖尿病、自身免疫性疾病及細胞增殖性疾?。[瘤）的治療具有重要意義。DPP-4是重要的藥物開發(fā)靶點，其中DPP-IV抑制劑Januvia磷酸西他列汀Sitagliptin  phosphate已作為抗糖尿病藥物上市。

DPP相關產(chǎn)品：（biomol）