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Guanylyl cyclase-A

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Target not currently curated in GtoImmuPdb

Target id: 1747

Nomenclature: Guanylyl cyclase-A

Abbreviated Name: GC-A

Family: Transmembrane guanylyl cyclases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1061 1q21.3 NPR1 natriuretic peptide receptor 1
Mouse 1 1057 3 39.23 cM Npr1 natriuretic peptide receptor 1
Rat 1 1057 2q34 Npr1 natriuretic peptide receptor 1
Previous and Unofficial Names Click here for help
ANPA receptor | natriuretic peptide receptor 1 | atrial natriuretic peptide A-type receptor | guanylate cyclase A | atrionatriuretic peptide receptor A | natriuretic peptide receptor-A
Database Links Click here for help
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
atrial natriuretic peptide {Sp: Human}
brain natriuretic peptide {Sp: Human}
mutant ANP
Potency order (Human)
atrial natriuretic peptide (NPPA, P01160) ≥ brain natriuretic peptide (NPPB, P16860) >> C-type natriuretic peptide (NPPC, P23582)  [9]

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
Dendroaspis natriuretic peptide Peptide Hs Agonist 9.7 pKd 8
pKd 9.7 (Kd 2x10-10 M) [8]
Description: Binding affinity for the iodinated peptide.
PL-3994 Peptide Primary target of this compound Click here for species-specific activity table Hs Agonist 9.0 pKi 2
pKi 9.0 (Ki 1x10-9 M) [2]
PL-3994 Peptide Rn Agonist 8.0 pKi 2
pKi 8.0 (Ki 1x10-8 M) [2]
[125I]ANP (human) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist - -
atrial natriuretic peptide {Sp: Human} Peptide Ligand is endogenous in the given species Hs Binding - - 7
[7]
brain natriuretic peptide {Sp: Human} Peptide Approved drug Ligand is endogenous in the given species Hs Binding - - 7
[7]
sANP Peptide Hs Agonist - - 7
[7]
cenderitide Peptide Click here for species-specific activity table Hs Agonist - - 4
[4]
mutant ANP Peptide Ligand is endogenous in the given species Hs Agonist - - 5
[5]
View species-specific agonist tables
Antagonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
A-71915 Peptide Hs Antagonist 9.2 – 9.5 pKi 1
pKi 9.2 – 9.5 (Ki 6.3x10-10 – 3.2x10-10 M) [1]
[Asu7,23']β-ANP-(7-28) Peptide Hs Antagonist 7.5 pKi 3
pKi 7.5 (Ki 3.1x10-8 M) [3]
anantin Peptide Hs Antagonist - - 10-11
[10-11]
HS-142-1 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - - 6
[6]

References

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1. Delporte C, Poloczek P, Gossen D, Tastenoy M, Winand J, Christophe J. (1991) Characterization and regulation of atrial natriuretic peptide (ANP)-R1 receptors in the human neuroblastoma cell line NB-OK-1. Eur J Pharmacol, 207 (1): 81-8. [PMID:1680722]

2. Edelson JD, Makhlina M, Silvester KR, Vengurlekar SS, Chen X, Zhang J, Koziol-White CJ, Cooper PR, Hallam TJ, Hay DW et al.. (2013) In vitro and in vivo pharmacological profile of PL-3994, a novel cyclic peptide (Hept-cyclo(Cys-His-Phe-d-Ala-Gly-Arg-d-Nle-Asp-Arg-Ile-Ser-Cys)-Tyr-[Arg mimetic]-NH(2)) natriuretic peptide receptor-A agonist that is resistant to neutral endopeptidase and acts as a bronchodilator. Pulm Pharmacol Ther, 26 (2): 229-38. [PMID:23154072]

3. Kambayashi Y, Nakajima S, Ueda M, Inouye K. (1989) A dicarba analog of beta-atrial natriuretic peptide (beta-ANP) inhibits guanosine 3',5'-cyclic monophosphate production induced by alpha-ANP in cultured rat vascular smooth muscle cells. FEBS Lett, 248 (1-2): 28-34. [PMID:2542088]

4. Martin FL, Sangaralingham SJ, Huntley BK, McKie PM, Ichiki T, Chen HH, Korinek J, Harders GE, Burnett Jr JC. (2012) CD-NP: a novel engineered dual guanylyl cyclase activator with anti-fibrotic actions in the heart. PLoS ONE, 7 (12): e52422. [PMID:23272242]

5. McKie PM, Cataliotti A, Huntley BK, Martin FL, Olson TM, Burnett Jr JC. (2009) A human atrial natriuretic peptide gene mutation reveals a novel peptide with enhanced blood pressure-lowering, renal-enhancing, and aldosterone-suppressing actions. J Am Coll Cardiol, 54 (11): 1024-32. [PMID:19729120]

6. Morishita Y, Sano T, Ando K, Saitoh Y, Kase H, Yamada K, Matsuda Y. (1991) Microbial polysaccharide, HS-142-1, competitively and selectively inhibits ANP binding to its guanylyl cyclase-containing receptor. Biochem Biophys Res Commun, 176 (3): 949-57. [PMID:1674870]

7. Olson LJ, Lowe DG, Drewett JG. (1996) Novel natriuretic peptide receptor/guanylyl cyclase A-selective agonist inhibits angiotensin II- and forskolin-evoked aldosterone synthesis in a human zona glomerulosa cell line. Mol Pharmacol, 50 (2): 430-5. [PMID:8700153]

8. Singh G, Kuc RE, Maguire JJ, Fidock M, Davenport AP. (2006) Novel snake venom ligand dendroaspis natriuretic peptide is selective for natriuretic peptide receptor-A in human heart: downregulation of natriuretic peptide receptor-A in heart failure. Circ Res, 99 (2): 183-90. [PMID:16778132]

9. Suga S, Nakao K, Hosoda K, Mukoyama M, Ogawa Y, Shirakami G, Arai H, Saito Y, Kambayashi Y, Inouye K. (1992) Receptor selectivity of natriuretic peptide family, atrial natriuretic peptide, brain natriuretic peptide, and C-type natriuretic peptide. Endocrinology, 130 (1): 229-39. [PMID:1309330]

10. Weber W, Fischli W, Hochuli E, Kupfer E, Weibel EK. (1991) Anantin--a peptide antagonist of the atrial natriuretic factor (ANF). I. Producing organism, fermentation, isolation and biological activity. J Antibiot, 44 (2): 164-71. [PMID:1849131]

11. Wyss DF, Lahm HW, Manneberg M, Labhardt AM. (1991) Anantin--a peptide antagonist of the atrial natriuretic factor (ANF). II. Determination of the primary sequence by NMR on the basis of proton assignments. J Antibiot, 44 (2): 172-80. [PMID:1826288]

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