Guanylyl cyclase-A | Transmembrane guanylyl cyclases | IUPHAR/BPS Guide to PHARMACOLOGY

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Guanylyl cyclase-A

Target not currently curated in GtoImmuPdb

Target id: 1747

Nomenclature: Guanylyl cyclase-A

Abbreviated Name: GC-A

Family: Transmembrane guanylyl cyclases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1061 1q21-q22 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
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
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
UniProtKB
Wikipedia
Natural/Endogenous Ligands
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]

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
Dendroaspis natriuretic peptide Hs Agonist 9.7 pKd 8
pKd 9.7 (Kd 2x10-10 M) [8]
Description: Binding affinity for the iodinated peptide.
PL-3994 Hs Agonist 9.0 pKi 2
pKi 9.0 (Ki 1x10-9 M) [2]
PL-3994 Rn Agonist 8.0 pKi 2
pKi 8.0 (Ki 1x10-8 M) [2]
[125I]ANP (human) Hs Agonist - -
atrial natriuretic peptide {Sp: Human} Hs Binding - - 7
[7]
brain natriuretic peptide {Sp: Human} Hs Binding - - 7
[7]
sANP Hs Agonist - - 7
[7]
cenderitide Hs Agonist - - 4
[4]
mutant ANP 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 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) Hs Antagonist 7.5 pKi 3
pKi 7.5 (Ki 3.1x10-8 M) [3]
anantin Hs Antagonist - - 10-11
[10-11]
HS-142-1 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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