209 10.2217/FNL.12.3 © 2012 Future Medicine Ltd ISSN 1479-6708
Future Neurol. (2012) 7(2), 209–224
part of
Future Neurology
TGF-b signaling
The TGF-b superfamily consists of 33 secreted
cytokines in humans, which include TGF-β-1,
-2, -3, BMPs, growth and differentiation fac-
tors (GDFs), activins/inhibins and nodal-related
proteins [1,2] . Most of these members are synthe-
sized as latent proteins, which are proteolytically
cleaved for activation and form functional dimers
that initiate downstream signaling through spe-
cific receptor interactions. These dimeric ligands
bind and assemble heterotetrameric complexes
of two types of transmembrane serine/threo-
nine kinase receptors, designated as the type I
and type II receptors. Five type II receptors,
namely Activin receptor IIA and IIB (ACVR2A,
ACVR2B), TGF-β receptor II (TGFBR2), BMP
receptor II (BMPR2), Müllerian inhibiting sub-
stance receptor II (MISR2) and seven type I
receptors, which are termed activin receptor-
like kinases (ALK 1–7, see TABLE 1 for official
gene symbols) have been identified with differ-
ent combinations of type I/II receptors medi-
ating the activity of different family members
proteins (TABLE 1) [1,2] . Activin initiates signaling
by binding to ACVR2A/B, in combination
with type 1 receptors ALK4 and ALK7. TGF-β
itself mainly uses TGFBR2 and ALK5, with an
exception in endothelial cells in which it can
signal via ALK1. Similar to activin, myostatin
(also known as GDF-8), can bind to ACVR2A,
ACVR2B and ALK4, but is also able to signal via
ALK5 [3,4] . BMP ligands form complexes with
other receptor combinations, namely the type II
receptors BMPR2 or ACVR2A/B with type I
receptors ALK1, ALK2, ALK3 and ALK6 [2] .
Ligand–receptor complex formation leads to
activation of the type I receptor through type II
receptor-mediated phosphorylation of serine and
threonine residues in the GS domain. The acti-
vated type I receptor will subsequently phospho-
rylate the intracellular receptor-regulated Smad
(R-Smad) proteins. Upon association of R-Smads
with the common Smad protein (Smad4), the
heteromeric Smad complexes translocate into the
nucleus, where they regulate the transcription of
a multitude of target genes. Different R-Smads
are activated by different ligands, with activin,
TGF-β and myostatin signaling being mediated
via Smad2 and Smad3, and BMP signaling via
Smad1/5/8 (FIGURE 1) [1] .
In addition to the combination of type I/II
receptors, the TGF-β signaling pathways are
further fine-tuned at multiple levels, for exam-
ple by presence of extracellular antagonists
that modify ligand activity and availability [5] .
Furthermore, several co-receptors can either
increase or decrease the affinity of ligands for
type I/II receptor binding. Tissue specificity of
the TGF-β family is also achieved by spatio-tem-
poral expression of these modulatory proteins.
An overview of TGF-β family members, their
receptors, co-receptors and interacting proteins
is presented in TABLE 1.
Role of TGF-b signaling in adult skeletal
muscle regeneration & regulation of
muscle mass
Postnatal skeletal muscle growth and matura-
tion occurs due to the activity of the muscle pro-
genitor cells, called satellite cells, which have the
TGF-b signaling in Duchenne
muscular dystrophy
Dwi U Kemaladewi
1,2
, Peter A ‘t Hoen
1
, Peter ten Dijke
2
, Gert Jan van Ommen
1
& Willem M Hoogaars*
1
1
Department of Human Genetics, Leiden University Medical Center, Postzone S4-P, PO Box 9600 2300RC
Leiden, The Netherlands
2
Department of Molecular & Cell Biology and Centre for Biomedical Genetics, Leiden University Medical
Center, Postzone S4-P, PO Box 9600 2300RC Leiden, The Netherlands
*Author for correspondence: n Tel.: +31 71 5269420 n Fax: +31 71 5268285 n w.m.h.hoogaars@lumc.nl
The TGF- b protein family consists of secreted multifunctional cytokines that control
diverse processes, such as cell growth and differentiation. Aberrant expression
and downstream signaling of these growth factors have been associated with
multiple diseases, including muscle wasting disorders, such as Duchenne muscular
dystrophy. In this review we discuss recent advances in understanding the role
of TGF- b family members during normal skeletal muscle biology/regeneration
and their role in muscle pathology, with a special focus on Duchenne muscular
dystrophy. In addition, we will highlight progress in the development of potential
therapeutics for Duchenne muscular dystrophy based on intervention of TGF- b
signaling.
Keywords
n activin n BMP n DMD n fibrosis
n muscle regeneration
n myostatin n TGF-b
Review
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