Until the discovery of leptin in 1994 by the group led
by Jeffrey Friedman
1
, white adipose tissue (WAT) was
considered only an energy storage tissue. In the past dec-
ade WAT has been recognized to be a very active tissue
and an unexpected source of bioactive peptides, termed
adipokines
2,3
. In addition to their metabolic activities,
it is now well known that these adipose-derived factors
represent a new family of compounds that are also syn-
thesized in tissues other than WAT (such as placenta
trophoblasts, amnion cells, cartilage or bone)
4
, and
that could participate in several processes including
inflammation and immunity
5–7
.
Leptin is mainly produced by adipocytes and, in
physiological conditions, its circulating levels correlate
positively with WAT mass. Therefore, leptin is consid-
ered a proinflammatory adipokine given that it seems
to contribute to the so-called ‘low-grade inflammatory
state’ in overweight and obese people
8
. Leptin is a 16 kDa
non-glycosylated protein encoded by the LEP gene (the
human homologue of murine Lep, also known as ob)
1
and exerts its biological actions by binding to its recep-
tor (LEPR), which belongs to the class I cytokine recep-
tor superfamily. There are several receptor isoforms:
a soluble isoform, isoforms with short cytoplasmic
domains, and a long isoform, which is found in almost
all tissues and which seems to be the only isoform capable
of transducing the leptin signal
9
. Similar to other class I
cytokine receptors, the long form of LEPR transmits
extracellular signals through the Janus kinase (JAK) and
signal transducer and activator of transcription (STAT)
signalling pathway
10
(FIG. 1). Most immune cell types
express LEPR at their surface, which suggests a role for
leptin in immune responses
11
.
Currently, leptin could be considered a link between
the neuroendocrine and immune systems
12,13
. This hor-
mone acts in the brain as an energy homeostasis reg-
ulating factor that triggers a decrease in food intake
and an increase in energy consumption by inducing
anorexigenic factors and suppressing orexigenic factors
14
.
Its own synthesis is mainly regulated by food intake and
eating-related hormones, but also depends on energy
status, sex hormones (leptin synthesis can be suppressed
by testosterone and increased by oestrogen and proges-
terone)
15
and a wide range of inflammatory mediators
(increased or suppressed by proinflammatory cytokines
depending on whether their action is acute or chronic)
16
.
1
SERGAS (Servizo Galego de
Saude) and IDIS (Instituto de
Investigación Sanitaria de
Santiago), The NEIRID Group
(Neuroendocrine Interactions
in Rheumatology and
Inflammatory Diseases),
Santiago University Clinical
Hospital, Building C, Trav.
Choupana, Santiago de
Compostela 15706, Spain.
Correspondence to O.G.
oreste.gualillo@sergas.es
doi:10.1038/nrrheum.2016.209
Published online 5 Jan 2017
Anorexigenic factors
Mediators that reduce food
intake by acting on
hypothalamic receptors
Orexigenic factors
Mediators that induce appetite
and stimulate food intake
Leptin in the interplay of
inflammation, metabolism and
immune system disorders
Vanessa Abella
1
, Morena Scotece
1
, Javier Conde
1
, Jesús Pino
2
, Miguel Angel
Gonzalez-Gay
3
, Juan J. Gómez-Reino
4
, Antonio Mera
4
, Francisca Lago
5
, Rodolfo Gómez
1
and Oreste Gualillo
1
Abstract | Leptin is one of the most relevant factors secreted by adipose tissue and the forerunner
of a class of molecules collectively called adipokines. Initially discovered in 1994, its crucial role as
a central regulator in energy homeostasis has been largely described during the past 20 years.
Once secreted into the circulation, leptin reaches the central and peripheral nervous systems and
acts by binding and activating the long form of leptin receptor (LEPR), regulating appetite and
food intake, bone mass, basal metabolism, reproductive function and insulin secretion, among
other processes. Research on the regulation of different adipose tissues has provided important
insights into the intricate network that links nutrition, metabolism and immune homeostasis.
The neuroendocrine and immune systems communicate bi‑directionally through common
ligands and receptors during stress responses and inflammation, and control cellular immune
responses in several pathological situations including immune‑inflammatory rheumatic diseases.
This Review discusses the latest findings regarding the role of leptin in the immune system and
metabolism, with particular emphasis on its effect on autoimmune and/or inflammatory
rheumatic diseases, such as rheumatoid arthritis and osteoarthritis.
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