Serine/threonin kinase
Serine/threonine protein kinases (STK) are interesting pharmacological targets for mCRPC being involved, inter alia, in resistance to therapy and local invasion or metastases. These protein family can be grouped in receptor STK and non-receptor STK. Receptor belonging this class bind TGFβ/activin/nodal and BMP/GDF (growth/differentiation factor)/MIS (Müllerian inhibiting substance) and are involved in bone metastases. Bone marrow stromal cells, indeed, secreted TGF-β isoforms modulating apoptosis and malignant cells selection. This receptor activates a complex enzymatic cascade responsible for the promotion of Epithelial/Mesenchymal Transition (EMT) as well as to generation of cancer stem cells. Non receptor STKs include inter alia: (i) kinases of PI3K/Akt/mTOR pathway; (ii) Ras-RafMEK-ERK pathway pathway, (iii) Rho GTPases including p21 activated family members (PAK) including PAK proteins RhoA and C and Rho associated kinasaes (ROCKs). PI3K/AKT/mTOR and Ras-Raf-MEK-ERK signals are dysregulated in PCa. Hyperactive status of diverse signal-transduction pathways, such as the PI3K–AKT and MAPK pathways, or from alterations in the general nuclear import/export machinery may result in aberrant nucleocytoplasmic shuttling of proteins involved in cell proliferation and survival.
References
1.Festuccia C. Expert Opin Investig Drugs. 2017;26(1):25–34.
References
1.Festuccia C. Expert Opin Investig Drugs. 2017;26(1):25–34.
Apoptosis
Serine/threonin kinase
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TAO Kinase inhibitor 2
产品货号 : M36917
cas no: 850467-77-5
TAO Kinase inhibitor 2 (Example 49) 是 TAO 激酶 抑制剂 (IC50=50-500 nM)。TAO Kinase inhibitor 2 还抑制 KIAA1361 和 JIK,IC50s 为 50-500 nM。 -
Chymotrypsin
产品货号 : M36555
cas no: 9004-07-3
Chymotrypsin (Chymotrypsin A) 是一种由胰腺产生的丝氨酸蛋白酶(serine protease)。Chymotrypsin 在芳香氨基酸的羧基侧切割蛋白质链。 -
PCSK9-IN-10
产品货号 : M36396
cas no: 368434-98-4
PCSK9-IN-10 是一种有效的,具有口服活性的 PCSK9 抑制剂,IC50 值为 6.4 μM。PCSK9-IN-10 增加 LDLR 蛋白的表达并降低 PCSK9 的表达。PCSK9-IN-10 可减缓动脉粥样硬化进展。PCSK9-IN-10 具有研究高脂血症的潜力。 -
N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine
产品货号 : M28592
cas no: 1071135-06-2
N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine 是一种新型 2,6-naphthyridine,经高通量筛选 (HTS) 鉴定为双蛋白激酶C/D (PKC/PKD) 抑制剂。 -
HA-1004
产品货号 : M27881
cas no: 91742-10-8
HA-1004 是 PKG、PKA、PKC 和 MLC 的抑制剂。