TP103检测试剂盒

TP103检测试剂盒

DPP4,DPPIV,二肽基肽酶4,二肽基肽酶IV,ADCP-2,CD26,ADABP,ADCP2,TP103

货号BML-AK499

DPPIV drug discovery kit   Enzo lifescience BML-AK499；二肽基肽酶 4 /二肽基肽酶IV  检测试剂盒，原装进口，现货供应！

The DPPIV Drug Discovery Kit is a complete assay systemdesigned to screen DPPIV inhibitors, providing enough material to perform atleast 96 assays. DPPIV (DPP4, CD26) is a member of the class of proteases knownas prolyl peptidases, which cleave proteins after proline residues and isthought to play roles in diabetes, cancer, and autoimmune diseases, making it atarget for drug discovery.

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

Cleavage of the p-nitroaniline (pNA) from the colorimetric substrate increasesabsorbance at 405 nm. The fluorimetric assay is based on the cleavage of7-amino-4-methylcoumarin (AMC) moiety from the C-terminus of the peptidesubstrate, which increases its fluorescence intensity at 460 nm. The kit isuseful to screen inhibitors of DPPIV, a potential therapeutic target. A DPPIVinhibitor, P32/98 (K_I=130 nM12), is included for use as a control.Other DPP enzymes are available for specificity profiling.

TP103检测试剂盒

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ProductLiterature References

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

Discovery and preclinical profile ofSaxagliptin (BMS-477118): a highly potent, long-acting, orally activedipeptidyl 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 itsrole in cancer: B. et al.;Histol. Histopathol. 19,1345 (2004), Abstract;

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

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

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

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

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

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

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

On the regulatory role of dipeptidylpeptidase IV (=CD=adenosine deaminase complexing protein) on adenosinedeaminase 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 andpost-proline cleaving enzyme in sera from osteoporotic patients: H. Gotoh et al.; Clin. Chem. 34, 2499 (1988), Abstract;

TP103检测试剂盒

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二肽基肽酶(dipeptidyl peptidase ，DPP)

二肽基肽酶(dipeptidylpeptidase ，DPP)是蛋白酶家族中的脯基肽酶成员，其可剪切含脯氨酸的蛋白，其中DPPIV (DPP4, CD26),是一种丝氨酸二肽基肽酶，其剪切靶多肽（细胞趋化因子如CXCL11和肽类激素如GLP-1）N端的X-Ala or X-Pro基. CD26是一种高度保守、分布于多种细胞的，具有跨膜域和很短的胞质域，但常被剪切和释放作为可溶性环化4型，常形成自身二聚体或与FAP形成异二聚体。DPPⅣ的天然底物多种多样，在体内执行多种重要功能。它还是细胞膜受体和共刺激分子，从而参与机体的免疫调节、细胞移行、细胞黏附和细胞调亡过程，故与多种疾病的发病有关。各种DPP-IV抑制剂对II型糖尿病、自身免疫性疾病及细胞增殖性疾病（肿瘤）的治疗具有重要意义。DPP-4是重要的药物开发靶点，其中DPP-IV抑制剂Januvia磷酸西他列汀Sitagliptin  phosphate已作为抗糖尿病药物上市。

DPP相关产品：（biomol）

TP103检测试剂盒