cyclo(RLsKDK) (TFA) (BK-1361 (TFA)) is a specific inhibitor of metalloproteinase Reduced cell invasion with dose-dependent manner.
cyclo(RLsKDK) (TFA) (10 µg/g;腹腔注射;一周一次持续 4 周) 显著降低了植入 Panc1_ctrl 或 Panc1_A8 细胞的小鼠中的肿瘤量。cyclo(RLsKDK) (TFA) 提高了胰腺导管腺癌 (PDAC) 小鼠存活率,降低了可溶性 ADAM8 (sADAM8) 含量、pERK1/2 活化、PDAC 在 PDAC 小鼠肝脏和肺部中的转移[2]。
[1]. Yim V, et al. Synthesis and biological evaluation of analogues of the potent ADAM8 inhibitor cyclo(RLsKDK) for the treatment of inflammatory diseases and cancer metastasis. Bioorg Med Chem. 2016 Sep 15;24(18):4032-4037.
[2]. Schlomann U, et al. ADAM8 as a drug target in pancreatic cancer. Nat Commun. 2015 Jan 28;6:6175.
















