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Restrict the search for
tyrosine
to a specific field?
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Sodium thiophosphate (or sodium monothiophosphate) a biochemical reagent, a specific inhibitor of protein tyrosine phosphatase and a competitive inhibitor of alkaline phosphatase. Thiophosphate was effective in inducing apoptosis in some leukemia cell lines including CEM and K562 and a lymphoma cell line, Raji. In addition, monothiophosphate entered intracellular nucleotide pools and served as an effective precursor for the phosphorylation of nuclear proteins in vivo.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
The isomer of fucosterol, isofucosterol, has been identified as a minor constituent of marine sponge, Gynostemma pentafillum, oat seeds and a few other plants. Isofucosterol of marine sponge is believed to be the biosynthetic precursors of the antiviral orthoesterols and weinbersterols found in the same sponge. Isofucosterol exhibits lipase inhibitory effect, suggesting that it has potential as anti-obesity agent.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Sodium thiophosphate (or sodium monothiophosphate) a biochemical reagent, a specific inhibitor of protein tyrosine phosphatase and a competitive inhibitor of alkaline phosphatase. Thiophosphate was effective in inducing apoptosis in some leukemia cell lines including CEM and K562 and a lymphoma cell line, Raji. In addition, monothiophosphate entered intracellular nucleotide pools and served as an effective precursor for the phosphorylation of nuclear proteins in vivo.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Staurosporine is an alkaloid isolated from the culture broth of Streptomyces staurosporesa. It exerts antimicrobial, hypotensive, and cytotoxic activity. The main biological activity of staurosporine is the inhibition of protein kinases through the prevention of ATP binding to the kinase. This is achieved through the stronger affinity of staurosporine to the ATP-binding site on the kinase. Staurosporine is a prototypical ATP-competitive kinase inhibitor in that it binds to many kinases with high affinity, though with little selectivity. It is a potent, cell permeable protein kinase C inhibitor with an IC50 of 0.7 nM. At higher concentration (1-20 nM), staurosporine also inhibits other kinases such as PKA, PKG, CAMKII and Myosin light chain kinase (MLCK). At 50-100 nM, it is a functional neurotrophin agonist, promoting neurite outgrowth in neuroblastoma, pheochromocytoma and brain primary neuronal cultures. At 0.2- 1 uM, staurosporine induces cell apoptosis. Staurosporine is also a potent GSK-3β inhibitor with a reported IC50 value of 15 nM. In research, staurosporine is used to induce apoptosis. It has been found that one way in which staurosporine induces apoptosis is by activating caspase-3. Staurosporine was discovered to have biological activities ranging from anti-fungal to anti-hypertensive. The interest in these activities resulted in a large investigative effort in chemistry and biology and the discovery of the potential for anti-cancer treatment. Staurosporine induces apoptosis by multiple pathways and that the inhibition of more than one kinase is responsible for its potent activity. Because the mechanism of action of staurosporine is distinct from traditional anticancer drugs, this may warrant further preclinical evaluations of the antitumor potential of new staurosporine derivatives either alone or in combination with death ligands or conventional chemotherapeutic drugs.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
PRT062607 (BIIB-057; P 50515 PRT-2607; PRT062607) is a highly specific and potent inhibitor of spleen tyrosine kinase (Syk). PRT062607 (BIIB-057) has a desirable pharmacokinetics profile and is capable of safely, potently, and selectively suppressing SYK kinase function in humans following once-daily oral dosing. The compound is being evaluated for the treatment of chronic inflammatory diseases; including rheumatoid arthritis, systemic lupus erythematosus, non-Hodgkin's lymphoma and chronic lymphocytic leukaemia. Phase I development is underway in the US and the UK for the treatment of patients with inflammation and cancer. Phase I development is also being conducted in rheumatoid arthritis and systemic lupus erythematosus, presumably in the US.
