Proteases (Di- and tripeptidyl)

Proteases (Di- and tripeptidyl)

Di- and tripeptidyl peptidases (EC 3.4.14.-) make up an individual class of aminopeptidases. DPP4 (EC 3.4.14.5) is also known as adenosine deaminase complexing protein 2 or CD26 (cluster of differentiation 26). It is an antigenic enzyme expressed on the surface of most cell types and is associated with immune regulation, signal transduction and apoptosis. It is an intrinsic membrane glycoprotein and a serine exopeptidase that cleaves X-proline dipeptides from the N-terminus of polypeptides. Additionally, it has been proven to be implicated in the pathogenesis of type 2 diabetes. Butabindide oxalate (Axon 1228) has proven to inhibit the cholecystokinin-8 (CCK-8)-inactivating peptidase, which is in fact a membrane-bound isoform of tripeptidyl peptidase II (EC 3.4.14.10). CCK-8 in its sulfated form functions as a neurotransmitter. It is released in response to ingestion of food and is involved in the control of food digestion through regulation of gallbladder contraction, pancreatic secretion, and contraction of the pyloric sphincter to delay gastric emptying. Inhibition of the enzyme therefore could be an opportunity to treat obesity related metabolic diseases.

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  • Butabindide oxalate
    1228
    Butabindide oxalate
    The price depends on the options chosen on the product page

    From $115.50

  • Vildagliptin
    1631
    Vildagliptin
    The price depends on the options chosen on the product page

    From $66.00

  • Linagliptin
    2354
    Linagliptin
    The price depends on the options chosen on the product page

    From $99.00

  • Trelagliptin succinate
    2470
    Trelagliptin succinate
    The price depends on the options chosen on the product page

    From $159.50

  • AZD7986
    2766
    AZD7986
    The price depends on the options chosen on the product page

    From $154.00

  • Sitagliptin
    3251
    Sitagliptin
    The price depends on the options chosen on the product page

    From $55.00

  • Teneligliptin hydrobromide
    3309
    Teneligliptin hydrobromide
    The price depends on the options chosen on the product page

    From $55.00

  • Alogliptin benzoate
    3310
    Alogliptin benzoate
    The price depends on the options chosen on the product page

    From $71.50

  • NDMC101
    3438
    NDMC101
    The price depends on the options chosen on the product page

    From $99.00

  • Perindopril erbumine
    3492
    Perindopril erbumine
    The price depends on the options chosen on the product page

    From $66.00

  • Quinapril hydrochloride
    3655
    Quinapril hydrochloride
    The price depends on the options chosen on the product page

    From $55.00

  • MLN-4760
    4433
    MLN-4760
    The price depends on the options chosen on the product page

    From $220.00

12 Items

More About Proteases (Di- and tripeptidyl)

Di- and tripeptidyl peptidases (EC 3.4.14.-) make up an individual class of aminopeptidases. DPP4 (EC 3.4.14.5) is also known as adenosine deaminase complexing protein 2 or CD26 (cluster of differentiation 26). It is an antigenic enzyme expressed on the surface of most cell types and is associated with immune regulation, signal transduction and apoptosis. It is an intrinsic membrane glycoprotein and a serine exopeptidase that cleaves X-proline dipeptides from the N-terminus of polypeptides. Additionally, it has been proven to be implicated in the pathogenesis of type 2 diabetes[1]. Butabindide oxalate (Axon 1228) has proven to inhibit the cholecystokinin-8 (CCK-8)-inactivating peptidase, which is in fact a membrane-bound isoform of tripeptidyl peptidase II (EC 3.4.14.10). CCK-8 in its sulfated form functions as a neurotransmitter. It is released in response to ingestion of food and is involved in the control of food digestion through regulation of gallbladder contraction, pancreatic secretion, and contraction of the pyloric sphincter to delay gastric emptying. Inhibition of the enzyme therefore could be an opportunity to treat obesity related metabolic diseases[2].

[1] Vildagliptin, a dipetidyl peptidase-IV inhibitor, improves model-assessed β-cell function in patients with type 2 diabetes. A. Mari et al. J. Clin. Endocrinol. Metab. 2005, 90, 4888-4894.
[2] Inhibitors of Tripeptidyl Peptidase II. 3. Derivation of Butabindide by Successive Structure Optimizations Leading to a Potential General Approach to Designing Exopeptidase Inhibitors. C.R. Ganellin et al. J. Med. Chem., 2005, 48, 7333-7342.

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