Abstract:
The present invention provides a method of identifying an agent which modulates an activity of a protein, wherein the protein is represented by the amino acid sequence of SEQ ID NO: 1 or has at least 90% amino acid sequence identity to SEQ ID NO: 1 and transports chloride ions across a cell membrane, comprising: (a) exposing cells which express the protein to the agent; and (b) measuring degree of chloride ion transport in the exposed cells, wherein a change in the degree of chloride ion transport compared to control cells, which express the protein but not exposed to the agent, is indicative of an agent capable of modulating an activity of the protein. The agents identified by this method can be used for the prevention or treatment of various diseases caused by the dysfunction of calcium activated chloride channel.
Abstract translation:本发明提供鉴定调节蛋白质活性的试剂的方法,其中所述蛋白质由SEQ ID NO:1的氨基酸序列表示或与SEQ ID NO:1具有至少90%的氨基酸序列同一性 并将氯离子转移穿过细胞膜,包括:(a)将表达蛋白质的细胞暴露于所述试剂; 和(b)测量暴露的细胞中氯离子转运的程度,其中与表达蛋白质但不暴露于试剂的对照细胞相比,氯离子转移程度的变化指示能够调节 蛋白质的活性。 通过该方法鉴定的药剂可用于预防或治疗由钙活化氯化物通道功能障碍引起的各种疾病。
Abstract:
The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions comprising such analogues, and their uses as vanilloid receptor agonists and potent analgesics. The present invention provides a pharmaceutical composition for treating acute, chronic, inflammatory or neuropathic pains or for treating bladder hypersensitivity.
Abstract:
The present invention relates to a method for producing a recombinant, spider toxin peptide and analgesic compositions containing said peptide. More specifically, the present invention relates to a method in which the gene for GsMTx4 is subcloned into a vector, so that it is linked to a secretion signal sequence of the alpha factor and under the control of methanol-inducible alcohol oxidase (AOX) promoter to construct a recombinant yeast expression plasmid. Yeast cells are transformed with this plasmid to produce the GsMTx4 peptide and analgesic compositions containing said peptide. The recombinant yeast expression system of the present invention affords a more stable method for producing GsMTx4 than its natural route. Thus the GsMTx4 peptide and its derivatives produced by the method of this invention can be used in the cure of related diseases such as heart failure as the peptide specifically inhibits mechanosensitive ion channels.
Abstract:
The present invention relates to a method for producing a recombinant, spider toxin peptide and analgesic compositions containing said peptide. More specifically, the present invention relates to a method in which the gene for GsMTx4 is subcloned into a vector, so that it is linked to a secretion signal sequence of the alpha factor and under the control of methanol-inducible alcohol oxidase (AOX) promoter to construct a recombinant yeast expression plasmid. Yeast cells are transformed with this plasmid to produce the GsMTx4 peptide and analgesic compositions containing said peptide. The recombinant yeast expression system of the present invention affords a more stable method for producing GsMTx4 than its natural route. Thus the GsMTx4 peptide and its derivatives produced by the method of this invention can be used in the cure of related diseases such as heart failure as the peptide specifically inhibits mechanosensitive ion channels.
Abstract:
Disclosed is the use of metabolites produced from arachiconic acid by the catalytic action of lipoxygenase as capsaicin-channel or- receptor agonists. The lipoxygenase metavolites of arachidonic acid and their derivatives can activate the capsaicin channel to excite pain nerves, causing serious pain. In contrast, the capsaicin channel activation of the pain nerves, so that an analgesic effects are brought about. The lipoxygenase metabolites of arachidonic acid can be used as an analgesic and in searching for and developing analgesics.