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ACE1 Inhibitor Screening Kit (Colorimetric) (ab283407) can be used to screen/characterize potential inhibitors of ACE1.

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Functional Studies - Angiotensin Converting Enzyme 1 (ACE1) Inhibitor Screening Kit (Colorimetric) (AB283407), expandable thumbnail

Key facts

Detection method

Colorimetric

Sample types

Inhibitor compounds

Target data

Function

Dipeptidyl carboxypeptidase that removes dipeptides from the C-terminus of a variety of circulating hormones, such as angiotensin I, bradykinin or enkephalins, thereby playing a key role in the regulation of blood pressure, electrolyte homeostasis or synaptic plasticity (PubMed:15615692, PubMed:20826823, PubMed:2558109, PubMed:4322742, PubMed:7523412, PubMed:7683654). Composed of two similar catalytic domains, each possessing a functional active site, with different selectivity for substrates (PubMed:10913258, PubMed:1320019, PubMed:1851160, PubMed:19773553, PubMed:7683654, PubMed:7876104). Plays a major role in the angiotensin-renin system that regulates blood pressure and sodium retention by the kidney by converting angiotensin I to angiotensin II, resulting in an increase of the vasoconstrictor activity of angiotensin (PubMed:11432860, PubMed:1851160, PubMed:19773553, PubMed:23056909, PubMed:4322742). Also able to inactivate bradykinin, a potent vasodilator, and therefore enhance the blood pressure response (PubMed:15615692, PubMed:2558109, PubMed:4322742, PubMed:6055465, PubMed:6270633, PubMed:7683654). Acts as a regulator of synaptic transmission by mediating cleavage of neuropeptide hormones, such as substance P, neurotensin or enkephalins (PubMed:15615692, PubMed:6208535, PubMed:6270633, PubMed:656131). Catalyzes degradation of different enkephalin neuropeptides (Met-enkephalin, Leu-enkephalin, Met-enkephalin-Arg-Phe and possibly Met-enkephalin-Arg-Gly-Leu) (PubMed:2982830, PubMed:6270633, PubMed:656131). Acts as a regulator of synaptic plasticity in the nucleus accumbens of the brain by mediating cleavage of Met-enkephalin-Arg-Phe, a strong ligand of Mu-type opioid receptor OPRM1, into Met-enkephalin (By similarity). Met-enkephalin-Arg-Phe cleavage by ACE decreases activation of OPRM1, leading to long-term synaptic potentiation of glutamate release (By similarity). Also acts as a regulator of hematopoietic stem cell differentiation by mediating degradation of hemoregulatory peptide N-acetyl-SDKP (AcSDKP) (PubMed:26403559, PubMed:7876104, PubMed:8257427, PubMed:8609242). Acts as a regulator of cannabinoid signaling pathway by mediating degradation of hemopressin, an antagonist peptide of the cannabinoid receptor CNR1 (PubMed:18077343). Involved in amyloid-beta metabolism by catalyzing degradation of Amyloid-beta protein 40 and Amyloid-beta protein 42 peptides, thereby preventing plaque formation (PubMed:11604391, PubMed:16154999, PubMed:19773553). Catalyzes cleavage of cholecystokinin (maturation of Cholecystokinin-8 and Cholecystokinin-5) and Gonadoliberin-1 (both maturation and degradation) hormones (PubMed:10336644, PubMed:2983326, PubMed:7683654, PubMed:9371719). Degradation of hemoregulatory peptide N-acetyl-SDKP (AcSDKP) and amyloid-beta proteins is mediated by the N-terminal catalytic domain, while angiotensin I and cholecystokinin cleavage is mediated by the C-terminal catalytic region (PubMed:10336644, PubMed:19773553, PubMed:7876104).Angiotensin-converting enzyme, soluble formSoluble form that is released in blood plasma and other body fluids following proteolytic cleavage in the juxtamembrane stalk region.Isoform Testis-specificIsoform produced by alternative promoter usage that is specifically expressed in spermatocytes and adult testis, and which is required for male fertility (PubMed:1651327, PubMed:1668266). In contrast to somatic isoforms, only contains one catalytic domain (PubMed:1651327, PubMed:1668266). Acts as a dipeptidyl carboxypeptidase that removes dipeptides from the C-terminus of substrates (PubMed:1668266, PubMed:24297181). The identity of substrates that are needed for male fertility is unknown (By similarity). May also have a glycosidase activity which releases GPI-anchored proteins from the membrane by cleaving the mannose linkage in the GPI moiety. The GPIase activity was reported to be essential for the egg-binding ability of the sperm (By similarity). This activity is however unclear and has been challenged by other groups, suggesting that it may be indirect (By similarity).

Targets

ACE2

Alternative names

What's included?

100 Test
Components
96 Well UV Transparent Plate
1 x 1 Unit
ACE Assay Buffer
1 x 25 mL
ACE1 Enzyme II
1 x 200 µL
ACE1 Inhibitor
1 x 100 µL
Colorimetric Substrate
1 x 1 Vial

Recommended products

ACE1 Inhibitor Screening Kit (Colorimetric) (ab283407) can be used to screen/characterize potential inhibitors of ACE1.

Key facts

Detection method

Colorimetric

Sample types

Inhibitor compounds

Assay Platform

Microplate (12 x 8 well strips)

Storage

Shipped at conditions

Blue Ice

Appropriate short-term storage conditions

-20°C

Appropriate long-term storage conditions

-20°C

Storage information

-20°C

Notes

ACE1 Inhibitor Screening Kit (Colorimetric) (ab283407) can be used to screen/characterize potential inhibitors of ACE1.

The kit utilizes the ability of an active ACE1 to hydrolyze a synthetic substrate, which results in the decrease in OD at 345 nm. In the presence of Captopril, an ACE1 specific inhibitor, the ACE1 enzymatic activity is greatly reduced and there is no significant decrease in the OD at 345 nm.

The assay kit provides a rapid, simple and reliable test for high-throughput screening of ACE1 inhibitors.

This product is manufactured by BioVision, an Abcam company and was previously called K719 ACE1 Inhibitor Screening Kit (Colorimetric). K719-100 is the same size as the 100 test size of ab283407.

Supplementary info

This supplementary information is collated from multiple sources and compiled automatically.

Activity summary

Angiotensin Converting Enzyme 1 also known as ACE1 or ACE is an important enzyme in the renin-angiotensin system. This enzyme exhibits a significant role in blood pressure regulation. ACE1 is a zinc-metallopeptidase with a molecular weight of approximately 130 kDa. It converts angiotensin I into the potent vasoconstrictor angiotensin II a critical function in cardiovascular physiology. ACE1 is widely expressed in endothelial cells particularly in the lungs kidneys and the small intestine.

Biological function summary

The enzyme generates angiotensin II by cleaving angiotensin I. Angiotensin II an important effector peptide impacts cardiovascular and renal systems influencing vasoconstriction and fluid balance. While not directly forming a complex ACE1's activity increases the potency of angiotensin II which binds to angiotensin II receptors to exert its effects therefore indirectly forming a functional signaling complex.

Pathways

ACE1 plays a central role in the renin-angiotensin system and the kallikrein-kinin system. The enzyme's activity boosts angiotensin II production which connects it to the regulation of blood pressure via the renin-angiotensin pathway. ACE1 also indirectly interacts with proteins like bradykinin by degrading them modulating kinin-related functions and influencing inflammation and tension in vascular smooth muscle.

Associated diseases and disorders

Understanding ACE1 is important for addressing hypertension and congestive heart failure. ACE1's conversion of angiotensin I to angiotensin II means overactivity can cause elevated blood pressure leading to hypertension. This makes ACE inhibitors such as lisinopril and ramipril therapeutic for these conditions. Furthermore its connection with aldosterone production places ACE1 in relevance to heart failure as excessive aldosterone can cause detrimental remodeling of cardiac tissue.

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1 product image

  • Functional Studies - Angiotensin Converting Enzyme 1 (ACE1) Inhibitor Screening Kit (Colorimetric) (ab283407), expandable thumbnail

    Functional Studies - Angiotensin Converting Enzyme 1 (ACE1) Inhibitor Screening Kit (Colorimetric) (ab283407)

    Inhibition of ACE1 activity by Captopril. IC50 was calculated to be 6.61 nM.

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Product protocols

For this product, it's our understanding that no specific protocols are required. You can:

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