CALP2TFA是一种钙调蛋白(CaM)拮抗剂(Kd为7.9µM)，以亲和力结合CaMEF-hand/Ca2+结合位点。CALP2TFA抑制CaM依赖性磷酸二酯酶(phosphodiesterase)活性并增加细胞内Ca2+浓度。CALP2TFA有效抑制粘附和脱粒。CALP2TFA还是肺泡巨噬细胞的强激活剂。
CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages[1][2][3][4].
[1]. R Houtman, et al. Attenuation of very late antigen-5-mediated adhesion of bone marrow-derived mast cells to fibronectin by peptides with inverted hydropathy to EF-hands. J Immunol. 2001 Jan 15;166(2):861-7. [2]. R Ten Broeke, et al. Calcium sensors as new therapeutic targets for airway hyperresponsiveness and asthma. FASEB J. 2001 Aug;15(10):1831-3. [3]. 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. [4]. 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.
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