Singer Monique, Martin Linda D, Vargaftig B Boris, Park Joungjoa, Gruber Achim D, Li Yuehua, Adler Kenneth B
Unité de Pharmacologie Cellulaire, Institut Pasteur, 28, rue du Dr. Roux, 75724 Paris Cedex 15, France.
Nat Med. 2004 Feb;10(2):193-6. doi: 10.1038/nm983. Epub 2004 Jan 11.
Mucus hypersecretion is a crucial feature of pulmonary diseases such as asthma, chronic bronchitis and cystic fibrosis. Despite much research, there is still no effective therapy for this condition. Recently, we showed that the myristoylated, alanine-rich C-kinase substrate (MARCKS) protein is required for mucus secretion by human bronchial epithelial cells in culture. Having synthesized a peptide corresponding to the N-terminal domain of MARCKS, we now show that the intratracheal instillation of this peptide blocks mucus hypersecretion in a mouse model of asthma. A missense peptide with the same amino acid composition has no effect. Based on quantitative histochemical analysis of the mouse airways, the peptide seems to act by blocking mucus release from goblet cells, possibly by inhibiting the attachment of MARCKS to membranes of intracellular mucin granules. These results support a pivotal role for MARCKS protein, specifically its N-terminal region, in modulating this secretory process in mammalian airways. Intratracheal administration of this MARCKS-related peptide could therapeutically reduce mucus secretion in the airways of human patients with asthma, chronic bronchitis and cystic fibrosis.
黏液高分泌是哮喘、慢性支气管炎和囊性纤维化等肺部疾病的关键特征。尽管进行了大量研究,但针对这种情况仍没有有效的治疗方法。最近,我们发现豆蔻酰化富含丙氨酸的蛋白激酶C底物(MARCKS)蛋白是培养的人支气管上皮细胞分泌黏液所必需的。在合成了一种与MARCKS的N端结构域对应的肽后,我们现在表明,在哮喘小鼠模型中气管内滴注这种肽可阻止黏液高分泌。具有相同氨基酸组成的错义肽则没有效果。基于对小鼠气道的定量组织化学分析,该肽似乎通过阻止杯状细胞释放黏液起作用,可能是通过抑制MARCKS与细胞内黏蛋白颗粒膜的附着。这些结果支持了MARCKS蛋白,特别是其N端区域,在调节哺乳动物气道的这种分泌过程中起关键作用。气管内给予这种与MARCKS相关的肽可在治疗上减少患有哮喘、慢性支气管炎和囊性纤维化的人类患者气道中的黏液分泌。