APLNR

Synonyms

AGTRL1, Angiotensin receptor-like 1, Apelin receptor, APJ, APLNR, G-Protein Coupled Receptor HG11, Angiotensin II Receptor-Like 1, APJ (Apelin) Receptor, G Protein-Coupled Receptor APJ, G-Protein Coupled Receptor APJ, HG11 Orphan Receptor, APJ Receptor, APJR, HG11, Apelin Receptors, FLJ90771

Description

APLNR (Apelin receptor) is a receptor for apelin receptor early endogenous ligand (APELA) and apelin (APLN) hormones coupled to G proteins that inhibit adenylate cyclase activity. Plays a key role in early development such as gastrulation, blood vessels formation and heart morphogenesis by acting as a receptor for APELA hormone. May promote angioblast migration toward the embryonic midline, i.e. the position of the future vessel formation, during vasculogenesis. Promotes sinus venosus (SV)-derived endothelial cells migration into the developing heart to promote coronary blood vessel development. Plays also a role in various processes in adults such as regulation of blood vessel formation, blood pressure, heart contractility and heart failure.Alternative coreceptor with CD4 for HIV-1 infection; may be involved in the development of AIDS dementia.

KO Status

RenMab: F0

RenLite: F1 (+/-)

Drug Information

Drugs in clinical trials: 3
Latest Research Phase: Phase 1 Clinical

Drug Name

Code

Phase

Company

Indications

Clinical Trials

Apelin-13

Apelin-13, 65-77-Apelin

Phase 1 Clinical

Centre Hospitalier Universitaire (Chu) De Toulouse

Diabetes Mellitus, Type 2

MM-07

MM-07

Phase 1 Clinical

University Of Cambridge

Pulmonary Arterial Hypertension

Azelaprag

AMG-986, BGE-105

Phase 1 Clinical

Amgen Inc

Heart Failure

Apelin

Pending

University Of Cambridge, Astrazeneca Plc

Diabetes Mellitus, Type 2

References


Title

Authors

Source

A human gene that shows identity with the gene encoding the angiotensin receptor is located on chromosome 11

O'Dowd B.F., Heiber M., Chan A., Heng H.H.Q., Tsui L.-C., Kennedy J.L., Shi X., Petronis A., George S.R., Nguyen T.,

Gene 136:355-360(1993)

The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)

The MGC Project Team,

Genome Res. 14:2121-2127(2004)

Apelin, the natural ligand of the orphan seven-transmembrane receptor APJ, inhibits human immunodeficiency virus type 1 entry

Cayabyab M., Hinuma S., Farzan M., Choe H., Fukusumi S., Kitada C., Nishizawa N., Hosoya M., Nishimura O., Messele T., Pollakis G., Goudsmit J., Fujino M., Sodroski J.,

J. Virol. 74:11972-11976(2000)

Elabela-apelin receptor signaling pathway is functional in mammalian systems

Wang Z., Yu D., Wang M., Wang Q., Kouznetsova J., Yang R., Qian K., Wu W., Shuldiner A., Sztalryd C., Zou M., Zheng W., Gong D.W.,

Sci. Rep. 5:8170-8170(2015)

Elabela/Toddler is an endogenous agonist of the apelin APJ receptor in the adult cardiovascular system, and exogenous administration of the peptide compensates for the downregulation of its expression in pulmonary arterial hypertension

Yang P., Read C., Kuc R.E., Buonincontri G., Southwood M., Torella R., Upton P.D., Crosby A., Sawiak S.J., Carpenter T.A., Glen R.C., Morrell N.W., Maguire J.J., Davenport A.P.,

Circulation 135:1160-1173(2017)

A human gene that shows identity with the gene encoding the angiotensin receptor is located on chromosome 11.

O'Dowd B.F., Heiber M., Chan A., Heng H.H.Q., Tsui L.-C., Kennedy J.L., Shi X., Petronis A., George S.R., Nguyen T.,

Gene 136:355-360(1993)

The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).

The MGC Project Team,

Genome Res. 14:2121-2127(2004)

Apelin, the natural ligand of the orphan seven-transmembrane receptor APJ, inhibits human immunodeficiency virus type 1 entry.

Cayabyab M., Hinuma S., Farzan M., Choe H., Fukusumi S., Kitada C., Nishizawa N., Hosoya M., Nishimura O., Messele T., Pollakis G., Goudsmit J., Fujino M., Sodroski J.,

J. Virol. 74:11972-11976(2000)

Elabela-apelin receptor signaling pathway is functional in mammalian systems.

Wang Z., Yu D., Wang M., Wang Q., Kouznetsova J., Yang R., Qian K., Wu W., Shuldiner A., Sztalryd C., Zou M., Zheng W., Gong D.W.,

Sci. Rep. 5:8170-8170(2015)

Elabela/Toddler is an endogenous agonist of the apelin APJ receptor in the adult cardiovascular system, and exogenous administration of the peptide compensates for the downregulation of its expression in pulmonary arterial hypertension.

Yang P., Read C., Kuc R.E., Buonincontri G., Southwood M., Torella R., Upton P.D., Crosby A., Sawiak S.J., Carpenter T.A., Glen R.C., Morrell N.W., Maguire J.J., Davenport A.P.,

Circulation 135:1160-1173(2017)