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Restrict the search for
angiotensin ii
to a specific field?
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
CX-5011, which was synthesized by Cylene Pharmaceutical, possesses an unprecedented selectivity towards the casein kinase II (CK2) versus other kinases. CK2 is a pleiotropic protein kinase, which regulates many survival pathways and plays a global anti-apoptotic function. It is highly expressed in tumor cells, and is presently considered a promising therapeutic target. Recently was discovered, that the ternary mixture containing CX-5011, imatinib and U0126 represents the most effective synergistic combination to counteract chronic myeloid leukaemia CML cell viability. Co-targeting CK2 and MEK protein kinases is a promising strategy to restore responsiveness of resistant CML cells to imatinib.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Veratridine (VTD), an alkaloid derived from the Liliaceae plant shows anti-tumor effects. Veratridine is also an agent that opens voltage dependent Na+ channels, blocks Na+ channel activation, and induces Ca2+ influx. The compound has been observed to be an alkaloid neurotoxin used to amplify sodium permeability. Studies report that Veratridine can trigger exocytosis and induce Ca2+ oscillations. Furthermore, Veratridine has been shown to effect the mitochondrial respiratory chain complexes, induce release of noradrenaline, and increase superoxide anion production. Veratridine competes with BTX binding in a mutually exclusive manner. However, the pharmacological effects of veratridine on Na+ channels are quite different
from those of BTX. First, veratridine reduces the single
Na+ channel conductance drastically whereas BTX does not.
Veratridine therefore is regarded as a partial agonist and BTX
as a full agonist of Na+ channels. Second, under voltage clamp
conditions BTX binds practically irreversibly to Na+
channels whereas veratridine readily dissociates from its binding
site. Both of these drugs, however, bind preferentially
to the open state of Na+ channels. The BTX resistant
Na+ channels in Phyllobates frogs remain sensitive to veratridine. The ceveratrum alkaloids, including Veratridine, have a characteristic hypotensive effect not directly involving the CNS. They slow the heart and lower arterial blood pressure by reflexly stimulating medullary vasomotor centers without decreasing cardiac output (Bezold–Jarisch effect). These agents were introduced in the 1950s as antihypertensive agents; however, they were found to have a narrow therapeutic index and their use was discontinued.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
JTE-607 is a multiple cytokine inhibitor. JTE-607 inhibited inflammatory cytokine production, including tumour necrosis factor (TNF)-alpha, interleukin IL-1beta, IL-6, IL-8, and IL-10, from LPS-stimulated human PBMCs. This compound may be useful for the treatment of various cytokine-mediated diseases such as septic shock without causing immunosuppression. JTE-607 may thus be efficacious in cytokine-mediated lung inflammation such as acute respiratory distress syndrome. JTE-607 inhibits the production of IL-10, IL-1ra and C-reactive protein in a human model of endotoxemia. In a leukaemia model engrafted with U-937 cells, JTE-607 significantly prolonged survival in mice and reduced human cytokine mRNA levels in the bone marrow. These results suggest the usefulness of JTE-607 in therapeutic applications for patients with hypercytokinemia and aggressive acute myelogenous leukaemia cell proliferation. JTE-607 had been in phase II clinical trials for the treatment of systemic inflammatory response syndrome but this study was discontinued.
JTC 801 was developed by Japan Tobacco as a novel opioid receptor-like1 (ORL(1)) receptor antagonist. It was found, that JTC-801 completely antagonized the suppression of nociceptin on the forskolin-induced accumulation of cyclic AMP using ORL(1) receptor expressing HeLa cells in vitro. JTC 801 produced analgesic effects and was studied in phase II of a clinical trial for the treatment of neuropathic, cancer and postoperative pain. Nevertheless, that studies were discontinued.
