aminopeptidase a

Firibastat (RB150) is a glutamyl aminopeptidase antagonist and an orally active brain penetrating prodrug of EC33. It is a first-in-class brain aminopeptidase A (APA) inhibitor with a Ki of 200 nM. Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats[1][2].

Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N/CD13 (IC50 = 25 μM). It is selective for AP-N/CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM.

Aminopeptidase N Ligand (CD13) NGR peptide, a polypeptide that targets CD13, functions as a carrier for mediating intracellular transmission and is commonly utilized in cancer research [1][2].

LeucineAminopeptidase, Porcine (EC 3.4.11.1), is a proteolytic enzyme that hydrolyzes peptide bonds adjacent to free amino groups. This enzyme rapidly catalyzes the hydrolysis of peptides containing leucine and can also facilitate the breakdown of various peptides and proteins, releasing other amino acids from the N-terminus.

AminopeptidaseN inhibitor 2 is an APN inhibitor (IC50: 4.3 μM) with antitumor properties.

Glycylproline dipeptidylaminopeptidase is an enzyme that catalyzes the hydrolysis of the N-terminal glycylproline from glycylproline-β-naphthylamide and glycylproline-β-nitroaniline.

Leucine Aminopeptidase (microsomal), Porcine (EC 3.4.11.2), is an enzyme that specifically catalyzes the hydrolysis of N-terminal leucine residues in peptides and proteins.

Aminopeptidase I, Streptomyces griseus (EC 3.4.11.22), exhibits broad substrate specificity, effectively removing N-terminal residues from most proteins, except when the penultimate residue is an imino acid. Aminopeptidase I contains two Zn2+ binding sites.

AminopeptidaseM, Porcine (EC 3.4.11.2), is a metalloprotease that can hydrolyze almost all N-terminal amino acids of unsubstituted oligopeptides. It does not cleave X-Pro bonds or amino acids with blocked N-terminals. AminopeptidaseM is utilized for peptide sequence analysis.

PyroglutamateAminopeptidase, Pyrococcus furiosus (EC 3.4.19.3), is a protein-digesting enzyme. It acts specifically on N-terminal pyroglutamate, cleaving this group from proteins and peptide chains to facilitate Edman degradation.

PyroglutamateAminopeptidase, derived from Thermococcus thioreducens, is a protein-digesting enzyme. It specifically targets the N-terminal pyroglutamate, cleaving it from proteins and peptide chains, thereby facilitating the Edman degradation process.

β-Peptidylaminopeptidase (EC 3.4.11.25) catalyzes the following chemical reaction: it removes N-terminal β-homo amino acids from peptide chains composed of 2 to 6 amino acids.

Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

L(+)-Leucinol is a potent inhibitor of leucine aminopeptidase.

ecMetAP-IN-1 can be used as a QSAR model to study methionine aminopeptidase inhibitor as an anticancer agent using multiple linear regression.

Sar-[D-Phe8]-des-Arg9-Bradykinin acetate is a potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo.

ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor that allosterically activates ERAP1's hydrolysis of fluorogenic and chromogenic amino acid substrates, while competitively inhibiting its activity toward a nonamer peptide representative of physiological substrates.

TP-004 is a potent, reversible inhibitor of methionine aminopeptidase 2 (MetAP2) with an IC50 of 6 nM.

Actinonin is a natural antibacterial agent produced by Streptomyces, also serving as an effective PDF (peptide deformylase) inhibitor and apoptosis inducer. It inhibits APN (Aminopeptidase N), MMPs and heparin α, exhibiting antiproliferative and antitumour activity.

HFI-142 is a small-molecule inhibitor that binds specifically to the active site of aminopeptidase N and suppresses its enzymatic activity. HFI-142 has been demonstrated to inhibit leukotriene A4 biosynthesis in red blood cells, an effect that may offer therapeutic potential for the research in cancer by modulating inflammatory and metabolic pathways implicated in tumor growth and progression. HFI-142 was also shown to inhibit the activity of additional aminopeptidases, including aminopeptidase N, as well as other enzymes associated with protein metabolism.

Puromycin aminonucleoside (NSC 3056) is an aminonucleoside antibiotic and a purine analog of puromycin. It can reversibly inhibit dipeptidyl peptidase and cytosolic alanine aminopeptidase, increase podocyte permeability by regulating ZO-1 in an oxidative stress-dependent manner, induce apoptosis, and promote the secretion of migrasomes. It is commonly used to induce nephrotic syndrome models in research.

TNP-470 is a methionine aminopeptidase-2 inhibitor and an angiogenesis inhibitor.

SB-587094 is a reversible inhibitor of methionine aminopeptidase-2 (MetAP-2).

ERAP1 modulator-1 (Compound 1) is a regulator of endoplasmic reticulum aminopeptidase 1 (ERAP1) with an IC50 of less than 250 nM.