lkb1

TMPA 是一种核受体 Nur77 和 LKB1 相互作用的拮抗剂。

Pim1 AKK1-IN-1 (LKB1 AAK1 dual inhibitor) 是多种酶抑制剂，能够作用于Pim1、AKK1、MST2 和 LKB1，Kd 值分别为 35、53、75 和 380 nM，还抑制 MPSK1 和 TNIK。

Kallikrein 5-IN-2 是一种选择性 KallikreinKLK5抑制剂 (pIC50=7.1)。KLK5 抑制可以使表皮脱落正常化并减少相关的炎症和瘙痒。

Phillyrin (Forsythin) 是从连翘中分离出来的一种天然产物，具有抗甲型流感病毒的活性，以及抗菌和消炎作用。

H3B-616是一种强效异位剂的抑制剂，针对Carbamoyl phosphate synthetase 1 (CPS1)，其IC50为66 nM。CPS1被认为是LKB1缺乏的非小细胞肺癌中的潜在合成致死靶标。在这些癌细胞中，CPS1的过表达促进了嘧啶的合成。

Panduratin A(泛影素 A)是一种天然的查尔酮衍生物，在人口腔表皮样癌KB细胞中对MMP-9具有抑制活性；对DENV-2的NS3蛋白酶具有抑制活性（Ki=25 μM）；对人雄激素非依赖性前列腺癌细胞PC-3和DU-145有明显的细胞毒性；还能够激活LKB1-AMPK-PPARα δ信号通路，增强肌细胞线粒体的氧化能力。

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg ml) and Gram-negative bacteria (MICs = 136-200 µg ml), as well as yeasts (MICs = 10-20 µg ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16 BL6 mouse model of melanoma when administered at a dose of 25 mg kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg kg.3Ajoene (25 mg kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16 BL6 melanoma cells in C57BL 6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)

Gomisin J 是在五味子中发现的小分子量木脂素，具有血管舒张活性，在非酒精性脂肪性肝病方面有研究潜力。 它通过激活 AMPK、LKB1 和 Ca2+ 钙调蛋白依赖性蛋白激酶 II 以及抑制 HepG2 细胞中的胎球蛋白 A 来调节脂肪生成酶和脂肪分解酶以及炎症分子的表达，从而抑制脂质积累。