Page last updated: 2024-10-24

vascular associated smooth muscle contraction

Definition

Target type: biologicalprocess

A process, occurring in the vascular tissue, whereby actin/myosin complex activity generates force through ATP hydrolysis resulting in a change in smooth muscle geometry. This process is always coupled to chemo-mechanical energy conversion. [GOC:mtg_muscle, MA:0002718]

Vascular associated smooth muscle contraction is a complex process that involves the coordinated interaction of various proteins and signaling pathways. It is essential for maintaining blood pressure, regulating blood flow, and controlling the movement of fluids through the circulatory system. The process begins with an increase in intracellular calcium levels, which can be triggered by various stimuli, including neurotransmitters, hormones, and mechanical stretch. Elevated calcium levels bind to calmodulin, activating the enzyme myosin light chain kinase (MLCK). MLCK then phosphorylates the regulatory light chain of myosin, enabling myosin to interact with actin filaments. This interaction forms cross-bridges between the myosin and actin, leading to the sliding of these filaments past each other, which ultimately results in muscle contraction. The strength and duration of the contraction are regulated by the balance between MLCK activity and myosin light chain phosphatase (MLCP) activity. MLCP dephosphorylates the regulatory light chain, promoting muscle relaxation. In addition to the calcium-dependent pathway, other signaling pathways also play a role in smooth muscle contraction, including the Rho-kinase pathway, which enhances MLCK activity, and the nitric oxide pathway, which activates MLCP and promotes relaxation. These complex interactions ensure that vascular associated smooth muscle cells can respond appropriately to various stimuli and maintain proper vascular function.'
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Proteins (1)

ProteinDefinitionTaxonomy
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alphaA phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha that is encoded in the genome of human. [PRO:DNx, UniProtKB:O00443]Homo sapiens (human)

Compounds (12)

CompoundDefinitionClassesRoles
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first sourcechromones;
morpholines;
organochlorine compound
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector
pi103PI103: pyridofuropyrimidine antineoplastic; a potent inhibitor of class I phosphatidylinositide 3-kinases (PI3K); structure in first sorucearomatic amine;
morpholines;
organic heterotricyclic compound;
phenols;
tertiary amino compound
antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor
idelalisibidelalisib : A member of the class of quinazolines that is 5-fluoro-3-phenylquinazolin-4-one in which the hydrogen at position 2 is replaced by a (1S)-1-(3H-purin-6-ylamino)propyl group. used for for the treatment of refractory indolent non-Hodgkin's lymphoma and relapsed chronic lymphocytic leukemia.

idelalisib: an antineoplastic agent and p110delta inhibitor; structure in first source
aromatic amine;
organofluorine compound;
purines;
quinazolines;
secondary amino compound
antineoplastic agent;
apoptosis inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
zstk474ZSTK-474 : A triamino-1,3,5-triazine that is 1,3,5-triazine in which two of the hydrogens have been replaced by morpholin-4-yl groups while the third hydrogen has been replaced by a 2-(difluoromethyl)benzimidazol-1-yl group. It is an inhibitor of phosphatidylinositol 3-kinase.benzimidazoles;
morpholines;
organofluorine compound;
triamino-1,3,5-triazine
antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
dactolisibdactolisib : An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment.

dactolisib: antineoplastic agent that inhibits both phosphatidylinositol 3-kinase and mTOR
imidazoquinoline;
nitrile;
quinolines;
ring assembly;
ureas
antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor
gdc 0941pictrelisib : A sulfonamide composed of indazole, morpholine, and methylsulfonyl-substituted piperazine rings bound to a thienopyrimidine ring.indazoles;
morpholines;
piperazines;
sulfonamide;
thienopyrimidine
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
gdc 0980
ch 5132799CH 5132799: structure in first source
torin 1torin 1 : A member of the class of pyridoquinolines that is 9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2-one bearing an additional 4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl substituent at position 1. It is a potent inhibitor of mTOR and exhibits anti-cancer properties.N-acylpiperazine;
N-arylpiperazine;
organofluorine compound;
pyridoquinoline;
quinolines
antineoplastic agent;
mTOR inhibitor
gdc-0032
torin 2torin 2 : A member of the class of pyridoquinolines that is benzo[h][1,6]naphthyridin-2-one carrying additional 3-(trifluoromethyl)phenyl and 6-aminopyridin-3-yl substituents at positions 1 and 9 respectively. It is a potent inhibitor of mTOR and exhibits anti-cancer properties.aminopyridine;
organofluorine compound;
primary amino compound;
pyridoquinoline
antineoplastic agent;
mTOR inhibitor
sar405SAR405: a Vps34 inhibitor with antineoplastic activity; structure in first source