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CALP2 是一种钙调蛋白 (CaM) 拮抗剂 (Kd 为 7.9 µM),以亲和力结合 CaM EF-hand/Ca2+ 结合位点。CALP2 抑制 CaM 依赖性磷酸二酯酶 (phosphodiesterase) 活性并增加细胞内 Ca2+ 浓度。CALP2 有效抑制粘附和脱粒。CALP2 还是肺泡巨噬细胞的强激活剂。
CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages[1][2][3][4].
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R Ten Broeke, et al. Calcium sensors as new therapeutic targets for airway hyperresponsiveness and asthma. FASEB J. 2001 Aug;15(10):1831-3. : https://pubmed.ncbi.nlm.nih.gov/11481245
Robert Ten Broeke, et al. Specific modulation of calmodulin activity induces a dramatic production of superoxide by alveolar macrophages. Lab Invest. 2004 Jan;84(1):29-40. : https://pubmed.ncbi.nlm.nih.gov/14631377
M Villain, et al. De novo design of peptides targeted to the EF hands of calmodulin. J Biol Chem. 2000 Jan 28;275(4):2676-85. : https://pubmed.ncbi.nlm.nih.gov/10644729