對具有ELR-CXC趨化素高度親合力的受體蛋白細胞所引發疾病之拮抗治療劑ANTAGONISTS FOR DISEASES INDUCED BY CELLS WITH HIGH-AFFINITY ELR-CXC CHEMOKINE RECEPTOR PROTEINS

專利類型

發明

專利國別 (專利申請國家)

美國

專利申請案號

13/494,587

專利證號

US 8,536,116 B2

專利獲證名稱

對具有ELR-CXC趨化素高度親合力的受體蛋白細胞所引發疾病之拮抗治療劑ANTAGONISTS FOR DISEASES INDUCED BY CELLS WITH HIGH-AFFINITY ELR-CXC CHEMOKINE RECEPTOR PROTEINS

專利所屬機關 (申請機關)

國立清華大學

獲證日期

2013/09/17

技術說明

本發明提供一種拮抗治療劑，其包括以一胺基酸序列表示的胜肽鏈，該胺基酸序列由N端起算第3個胱胺酸再往該N端具有以X1X2X3X4X5表示之一序列，其中X1為芳香性、疏水性或長鏈之胺基酸，X2為麩醯胺，X3為絲胺酸，X4為丙胺酸，且X5為脯胺酸。在一實施例中，X1為苯丙胺酸。本發明可用於抑制、治療透過表現CXCR1或/及CXCR2受體而使細胞產生的活化而造成的相關疾病，如白血球中表現CXCR1或/及CXCR2受體的嗜中性球所引發的急性發炎反應或慢性發炎反應及抑制腫瘤成長所伴隨之血管新生作用。 Enclosed is an antagonist, which includes a peptide chain represented by an amino acid sequence. The amino acid sequence has a short sequence, C-X1X2X3X4X5-N, which is situated before and neighbored to the third cysteine (Cys, C) of the N terminal, wherein X1 is an amino acid with aromatic ring, hydrophobic property or long chain, and X2, X3, X4 and X5 are glutamine (G), serine (S), alanine (A) and proline (P) resepectively. In one embodiment, X1 is phenylalanine (F). The present antagonists can be used to inhibit or treat with the diseases caused by the activated cells expressing CXCR1 and/or CXCR2 receptor, for example, the acute or chronic inflammatory reaction induced with polymorphonuclear neutrophils (PMNs) expressing CXCR1 and/or CXCR2 receptor, and angiogenesis accompanied by tumor growth inhibition.

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