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Literature summary for 3.1.4.1 extracted from

  • Patel, S.D.; Habeski, W.M.; Cheng, A.C.; de la Cruz, E.; Loh, C.; Kablaoui, N.M.
    Quinazolin-4-piperidin-4-methyl sulfamide PC-1 inhibitors: alleviating hERG interactions through structure based design (2009), Bioorg. Med. Chem. Lett., 19, 3339-3343.
    View publication on PubMed

Application

Application Comment Organism
drug development the enzyme is a possible target for drug design in treatment of calcium pyrophosphate dehydrate deposition disease. PC-1 interferes with insulin receptor signaling, a link between mutations in PC-1 and insulin resistance. PC-1 inhibitors may therefore also have use in treating diabetic patients Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
dofetilide
-
Homo sapiens
N-(2-[1-[2-(2-methyl-1H-imidazol-1-yl)pyrimidin-4-yl]piperidin-4-yl]ethyl)sulfuric diamide
-
Homo sapiens
N-(2-[1-[6-(2-methyl-1H-imidazol-1-yl)pyrimidin-4-yl]piperidin-4-yl]ethyl)sulfuric diamide
-
Homo sapiens
N-[2-(1-[6,7-dimethoxy-2-[(E)-2-(pyridin-3-yl)ethenyl]quinazolin-4-yl]piperidin-4-yl)ethyl]sulfuric diamide
-
Homo sapiens
N-[2-[1-(2-ethyl-6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
-
Homo sapiens
N-[2-[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide enzyme binding, structure modelling, overview Homo sapiens
N-[2-[1-(6-chloroquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
-
Homo sapiens
N-[2-[1-(7-chloroquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
-
Homo sapiens
N-[2-[1-(7-methoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane PC-1 is a class II transmembrane glycoprotein Homo sapiens 16020
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + H2O Homo sapiens
-
AMP + diphosphate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
glycoprotein PC-1 is a class II transmembrane glycoprotein Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
chondrocyte high expression level Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O
-
Homo sapiens AMP + diphosphate
-
?

Synonyms

Synonyms Comment Organism
More the enzyme belongs to a family of enzymes with nucleoside triphosphate pyrophophohydrolase, NTPPPH, activity Homo sapiens
NPP-1
-
Homo sapiens
PC-1
-
Homo sapiens
plasma cell membrane protein-1
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000035
-
-
Homo sapiens N-[2-(1-[6,7-dimethoxy-2-[(E)-2-(pyridin-3-yl)ethenyl]quinazolin-4-yl]piperidin-4-yl)ethyl]sulfuric diamide
0.000036
-
-
Homo sapiens N-[2-[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
0.000187
-
-
Homo sapiens N-[2-[1-(7-methoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
0.000214
-
-
Homo sapiens N-[2-[1-(2-ethyl-6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
0.0006
-
-
Homo sapiens N-(2-[1-[6-(2-methyl-1H-imidazol-1-yl)pyrimidin-4-yl]piperidin-4-yl]ethyl)sulfuric diamide
0.00245
-
-
Homo sapiens N-(2-[1-[2-(2-methyl-1H-imidazol-1-yl)pyrimidin-4-yl]piperidin-4-yl]ethyl)sulfuric diamide
0.00598
-
-
Homo sapiens N-[2-[1-(6-chloroquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
0.01
-
above Homo sapiens N-[2-[1-(7-chloroquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide

General Information

General Information Comment Organism
malfunction PC-1 is the major source of the elevated phosphate levels in chondrocytes and fibroblasts of patients with familial calcium pyrophosphate dehydrate deposition disease, CPPD. CPPD crystals may be a hallmark of the pathology of osteoarthritis Homo sapiens