Adiponectin receptor 1 (AdipoR1) is a
protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residues. Proteins perform a vast array of functions within organisms, including catalysing metabolic reactions, DNA replication, respo ...
which in humans is encoded by the ''ADIPOR1''
gene
In biology, the word gene (from , ; "...Wilhelm Johannsen coined the word gene to describe the Mendelian units of heredity..." meaning ''generation'' or ''birth'' or ''gender'') can have several different meanings. The Mendelian gene is a ba ...
.
It is a member of the
progestin and adipoQ receptor
The progestin and adipoQ receptor (PAQR) family is a group of receptors related to but distinct from the G protein-coupled receptor family, which have the similar seven transmembrane structure, but the N-terminal is located on the inner side of the ...
(PAQR) family, and is also known as PAQR1.
Structure
Similar to
G protein-coupled receptor
G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily-related p ...
s (GPCRs), AdipoR1 also possesses 7
transmembrane domain
A transmembrane domain (TMD) is a membrane-spanning protein domain. TMDs generally adopt an alpha helix topological conformation, although some TMDs such as those in porins can adopt a different conformation. Because the interior of the lipid bil ...
s. However, AdipoR1 is orientated oppositely to GPCRs in the membrane (i.e., cytoplasmic
N-terminus
The N-terminus (also known as the amino-terminus, NH2-terminus, N-terminal end or amine-terminus) is the start of a protein or polypeptide, referring to the free amine group (-NH2) located at the end of a polypeptide. Within a peptide, the ami ...
, extracellular
C-terminus
The C-terminus (also known as the carboxyl-terminus, carboxy-terminus, C-terminal tail, C-terminal end, or COOH-terminus) is the end of an amino acid chain (protein or polypeptide), terminated by a free carboxyl group (-COOH). When the protein is ...
) and does not associate with
G protein
G proteins, also known as guanine nucleotide-binding proteins, are a family of proteins that act as molecular switches inside cells, and are involved in transmitting signals from a variety of stimuli outside a cell to its interior. Their act ...
s.
Function
The
adiponectin receptor
The adiponectin receptors (AdipoRs) include the following two receptors, which are bound and activated by adiponectin:
* Adiponectin receptor 1 (AdipoR1, PAQR1)
* Adiponectin receptor 2 (AdipoR2, PAQR2)
They are members of the progestin and adipo ...
s, AdipoR1 and
AdipoR2
Adiponectin receptor 2 (AdipoR2) is a protein which in humans is encoded by the ''ADIPOR2'' gene. It is a member of the progestin and adipoQ receptor (PAQR) family, and is also known as PAQR2.
Structure
Similar to G protein-coupled receptors (GPCR ...
, serve as receptors for globular and full-length
adiponectin
Adiponectin (also referred to as GBP-28, apM1, AdipoQ and Acrp30) is a protein hormone and adipokine, which is involved in regulating glucose levels as well as fatty acid breakdown. In humans it is encoded by the ''ADIPOQ'' gene and it is produced ...
and mediate increased
AMPK AMPK may refer to:
* AMP-activated protein kinase
5' AMP-activated protein kinase or AMPK or 5' adenosine monophosphate-activated protein kinase is an enzyme (EC 2.7.11.31) that plays a role in cellular energy homeostasis, largely to activate gl ...
and
PPAR-α ligand activities, as well as
fatty acid
In chemistry, particularly in biochemistry, a fatty acid is a carboxylic acid with an aliphatic chain, which is either saturated or unsaturated. Most naturally occurring fatty acids have an unbranched chain of an even number of carbon atoms, fr ...
oxidation and glucose uptake by adiponectin.
In 2016, the University of Tokyo announced that it would launch an investigation into claims of fabrication of AdipoR1 and AdipoR2 identification data, as accused by an anonymous person/group called
Ordinary_researchers In 2010s, a series of separate allegations of scientific misconducts were raised involving several scientific papers from various Japanese universities.
Shigeaki Kato
In February 1996, Shigeaki Kato, who had studied in the laboratory of Pierre Ch ...
.
[University of Tokyo to investigate data manipulation charges against six prominent research groups](_blank)
ScienceInsider, Dennis Normile, Sep 20, 2016
Ligands
Agonists
Peptide
*
Adiponectin
Adiponectin (also referred to as GBP-28, apM1, AdipoQ and Acrp30) is a protein hormone and adipokine, which is involved in regulating glucose levels as well as fatty acid breakdown. In humans it is encoded by the ''ADIPOQ'' gene and it is produced ...
*
ADP-355
*
ADP-399
Non-peptide
*
AdipoRon
AdipoRon is a selective, orally active, synthetic small-molecule agonist of the adiponectin receptor 1 (AdipoR1) and adiponectin receptor 2 (AdipoR2) (Kd = 1.8 μM and 3.1 μM, respectively). It activates AMPK and PPARα signaling and ameliorates ...
*
(–)-Arctigenin
Arctigenin is a lignan found in certain plants of the Asteraceae, including the greater burdock (''Arctium lappa'') and ''Saussurea heteromalla''. It has shown antiviral and anticancer effects in vitro. It is the aglycone of arctiin.
The use of a ...
*
Arctiin
Arctiin is a lignan found in many plants of the family Asteraceae, particularly the greater burdock (''Arctium lappa'') and ''Centaurea imperialis'', and in ''Trachelospermum asiaticum'', ''Saussurea heteromalla'', Retrieved on April 25, 2011. a ...
*
Gramine
Gramine (also called donaxine) is a naturally occurring indole alkaloid present in several plant species. Gramine may play a defensive role in these plants, since it is toxic to many organisms.
Occurrence
Gramine has been found in the giant reed, ...
*
Matairesinol
Matairesinol is an organic compound. It is classified as a lignan, i.e., a type of phenylpropanoid. It is present in some cereals, e.g. rye, and together with Secoisolariciresinol, has attracted much attention for its beneficial nutritional effec ...
Antagonists
Peptide
*
ADP-400
See also
*
Adiponectin receptor
The adiponectin receptors (AdipoRs) include the following two receptors, which are bound and activated by adiponectin:
* Adiponectin receptor 1 (AdipoR1, PAQR1)
* Adiponectin receptor 2 (AdipoR2, PAQR2)
They are members of the progestin and adipo ...
*
Adiponectin receptor 2
Adiponectin receptor 2 (AdipoR2) is a protein which in humans is encoded by the ''ADIPOR2'' gene. It is a member of the progestin and adipoQ receptor (PAQR) family, and is also known as PAQR2.
Structure
Similar to G protein-coupled receptors (GPCR ...
References
External links
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Further reading
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7TM receptors
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