Cytoskeletal Signaling

Cytoskeleton refers to the protein fiber network found in eukaryotic cells. It was found relatively later, mainly because that the general sample preparation of electron microscopy was performed under low temperature (0-4 °C) for cell fixation while the cytoskeleton will undergo depolymerization at low temperatures. Until the 1960s, after the use of glutaraldehyde for fixation at room temperature, people come to realize the objective existence of the cytoskeleton.

The cytoskeleton not only play important roles in maintaining the cell shape, tolerating the external force and maintaining the order in terms of internal structure of cells, but also participate into many important life processes (FIG. 1), for example: during the process of cell division, the cytoskeleton will hold the chromosome for segregation; during the cellular material transport, all types of vesicles and organelles can be directed along cytoskeleton; in muscle cells, cytoskeleton can from power system together with its binding proteins; the migration of leukocytes, motility of sperm, the stretching of nerve cell axons and dendritic are all related to cytoskeleton. Furthermore, in plant cells, the cytoskeleton directs the synthesis of the cell wall.

Cytoskeleton consists of microfilament, microtubules and intermediate filaments. Microfilament determines the surface characteristics of the cells, enabling the cells to move and contract. Microtubules determine the position of the membranous organelles (membrane-enclosed organelle) and as the rail of the vesicular transport. Intermediate fiber makes the cells to have tension and anti-shear forces.

Microfilaments, microtubules and intermediate filaments are located in the cytoplasm, also known as the cytoskeleton. They are all comprised of monomeric proteins which bind together via weak non-covalently bond, forming fiber-type polymer. It is easy to undergo assembly and disassembly, which is necessary to achieve its functional characteristics.

Generalized cytoskeleton also includes nucleoskeleton, nuclear lamina and extracellular matrix, forming an integrated network structure through the cell nucleus, cytoplasm and outer cell.

  the major functions of the cytoskeleton
Figure1 the diagram of the major functions of the cytoskeleton

Cytoskeleton is the structural basis of cell function. Upon external stimuli or during the process of cell division and differentiation, cell will undergo related morphological changes. This is inseparable from the regulation of the Cytoskeletal dynamic change via signaling transduction. Cytoskeleton, as the dynamic protein fiber network inside eukaryotic cell, consists of the microfilaments (microfilaments, MF), tubulin (microtubules, MT) and an intermediate fiber (intermediate filaments, IF). MF is the polymer formed through actin polymerization and is widely present in the stress fibers, adhesion focal, pseudopodia and the contractile ring of the eukaryotic cells. Its structure constituent unit, globular actin (G-actin), under the action of ATP and a variety of actin-related proteins, through the continuous conversion of assembly and depolymerization with the filamentous actin (F-actin), participating into the regulation of behaviors of cell morphology, adhesion, migration, and cytokinesis. MT is formed through the polymerization of α-tubulin and β-tubulin. Under the action of microtubule-associated proteins, it assembles to form a hollow tubular structure, playing an important role in intracellular material transport and cytokinesis. MF and MT cytoskeleton are interrelated and interdependent, jointly participating into the regulation of cell behavior (Bailly M, 2002; Miranti C.K, 2002).

Cell migration is the key step during the process of malignant tumor invasion and metastasis. Cytoskeleton and its binding protein is the material basis of cell migration. Cell cytoskeleton is needed for the directional movement of cells. The microfilament cytoskeleton consisting of actions are in particular important during the above process. MF and MT not only play important role in stabilizing the cell morphology, withstanding the external stimulation and maintenance of the order of the internal structure of cells, but also participate in the regulation of cell migration, adhesion, division and intracellular signaling. Among them, the interaction effect between the cAMP-mediated signaling pathway and cytoskeleton are closely related to various cellular behaviors including cell proliferation, apoptosis, adhesion and migration. cAMP-dependent protein kinase A (PKA), as the major cAMP-dependent protein targeting protein, is involved in these processes. PKA can activate the RhoA through phosphorylation. RhoA, after activation, in addition of further activating downstream pathways, also enhances the binding capability to the Rho guanosine diphosphate dissociation inhibitor (RhoGDI,), thus inhibiting the RhoA activity from the opposite direction (Mehlen, P, 2006).

Integrin is an important class of receptor in the cell surface of both adhesion and signal transduction function. It is a kind of hetreodimer which is composed of α and β subunits through non-covalent bonds. Extracellular matrix proteins such as fibronectin, laminin and collagen are its primary ligand; secondly there are also some cell surface molecules, soluble proteins that can also binds to integrins. Through binding to the cytoskeleton, signal transduction and other kinds of protein via its extracellular domain as well as intracellular domain, integrin, like a bridge, mediates the two-way transmission of information inside and outside of the cells. The bidirectional signal transduction between integrin and cytoskeleton, (a) from the cytoskeleton to integrins, integrin can disperse in the cell surface in the absence of binding and is not connected with the actin cytoskeleton. Once binding to the ECM ligand binding, the integrin can contact with the cytoskeleton through its intracellular domain and form clusters. (B) From integrins to the cytoskeleton, integrins can have feedback regulation of cytoskeleton assembly. The integrin-mediated adhesion itself can activate Rho family of small G proteins (Mitra SK, 2005; Larsen M, 2003; Turner CE, 2000).

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Structure Chemical Name CAS MF
Triclabendazole Triclabendazole 68786-66-3 C14H9Cl3N2OS
NOCODAZOLE NOCODAZOLE 31430-18-9 C14H11N3O3S
Ispinesib Ispinesib 336113-53-2 C30H33ClN4O2
Dynasore Dynasore 304448-55-3 C18H14N2O4
Ganetespib Ganetespib 888216-25-9 C20H20N4O3
Elesclomol Elesclomol 488832-69-5 C19H20N4O2S2
Luminespib Luminespib 747412-49-3 C26H31N3O5
NVP-BEP800 NVP-BEP800 847559-80-2 C21H23Cl2N5O2S
17-DMAG 17-DMAG 467214-21-7 C32H49ClN4O8
SB 743921 SB 743921 940929-33-9 C31H34Cl2N2O3
Epothilone A Epothilone A 152044-53-6 C26H39NO6S
BIIB-021 BIIB-021 848695-25-0 C14H15ClN6O
cilengitide cilengitide 188968-51-6 C27H40N8O7
KW-2478 KW-2478 819812-04-9 C30H42N2O9
9-Cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8H-purin-8-one 9-Cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8H-purin-8-one 1124329-14-1 C24H32N6O3
4-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)-2-((1r,4r)-4-hydroxycyclohexylamino)benzamide 4-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)-2-((1r,4r)-4-hydroxycyclohexylamino)benzamide 908112-43-6 C23H27F3N4O3
PF-04929113 PF-04929113 908115-27-5 C25H30F3N5O4
6-Amino-8-[(6-iodo-1,3-benzodioxol-5-yl)thio]-N-(1-methylethyl)-9H-purine-9-propanamine 6-Amino-8-[(6-iodo-1,3-benzodioxol-5-yl)thio]-N-(1-methylethyl)-9H-purine-9-propanamine 873436-91-0 C18H21IN6O2S
IPA-3 IPA-3 42521-82-4 C20H14O2S2
Vinflunine Tartrate Vinflunine Tartrate 1201898-17-0 C49H60F2N4O14
N-[4-(2,4-Dimethylphenyl)-2-thiazolyl]benzamidehydrochloride N-[4-(2,4-Dimethylphenyl)-2-thiazolyl]benzamidehydrochloride 313553-47-8 C18H16N2OS
VER-49009 VER-49009 940289-57-6 C19H18ClN3O4
6-(2-Chloro-4-thiazol-5-yl-phenyl)-8-ethyl-2-[4-(4-Methyl-piperazin-1-yl)-phenylaMino]-8H-pyrido[2,3-d]pyriMidin-7-one 6-(2-Chloro-4-thiazol-5-yl-phenyl)-8-ethyl-2-[4-(4-Methyl-piperazin-1-yl)-phenylaMino]-8H-pyrido[2,3-d]pyriMidin-7-one 1286739-19-2 C29H28ClN7OS
CK-636 CK-636 442632-72-6 C16H16N2OS
N-(4-Mesitylthiazol-2-yl)benzaMide N-(4-Mesitylthiazol-2-yl)benzaMide 1001753-24-7 C19H18N2OS
NVP-HSP990(HSP990) NVP-HSP990(HSP990) 934343-74-5 C20H18FN5O2
(S)-2-(8-(2-(6-(methylamino)pyridin-2-yl)ethoxy)-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl)acetic acid (S)-2-(8-(2-(6-(methylamino)pyridin-2-yl)ethoxy)-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl)acetic acid 205678-31-5 C22H24F3N3O4
Onalespib Onalespib 912999-49-6 C24H31N3O3
VER-50589 VER-50589 747413-08-7 C19H17ClN2O5
PF-3758309 PF-3758309 898044-15-0 C25H30N8OS
5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide 5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide 1253584-84-7 C22H22N4O7
MPI-0479605 MPI-0479605 1246529-32-7 C22H29N7O
XL888 XL888 1149705-71-4 C29H37N5O3
CW069 CW069 1594094-64-0 C23H21IN2O3
TAI-1 TAI-1 1334921-03-7 C24H21N3O3S
ARQ 621 ARQ 621 1095253-39-6 C28H24Cl2FN5O2
CH5138303 CH5138303 959763-06-5 C19H18ClN5O2S
A 205804 A 205804 251992-66-2 C15H12N2OS2
3-(2,4-Dichloro-5-methoxyphenyl)-2,3-dihydro-2-thioxo-4(1H)-quinazolinone 3-(2,4-Dichloro-5-methoxyphenyl)-2,3-dihydro-2-thioxo-4(1H)-quinazolinone 338967-87-6 C15H10Cl2N2O2S
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