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p21-activated kinase 1 is allostericallyInhibited by naphthoquinone (NQ) derivatives
오상원,이기인,최중권,김경아,김응국,신은영 충북대학교 동물의학연구소 2017 Journal of Biomedical and Translational Research Vol.18 No.2
The p21-activated kinases (PAKs) are a family of serine/threonine protein kinases and activated by binding with activated Rho GTPases such as Rac or Cdc42. PAKs regulate actin cytoskeletal remodeling, cell motility, cell survival, and apoptosis. Also, PAKs are involved in several diseases such as cancer, virus infectious diseases, mental retardation, Alzheimer and Parkinson's diseases. Therefore, the substances that are able to inhibit PAK activation can be used as powerful tools and medicines for PAK relative diseases or specific inhibitors for study of PAK signaling pathway. In this study, we investigated and characterized the 5 compounds of 4-benzene-1, 2-naphthoquinone (NQ) family as candidate substances to inhibit the PAK1 activation in vitro and in cells. Binding between p21-binding domain (PBD) of PAK1 and Cdc42 was blocked by 5 NQ-compounds in ELISA assay. Myelin basic protein (MBP) phosphorylation was dramatically reduced by treatment of these compounds in vitro kinase assay for Cdc42-induced or constitutive active PAK1 mutant. Also, phosphorylation at Thr 423 of transfected PAK1 was inhibited by treatment of 5 NQ-compounds in 293T cells, respectively. Finally, NQ-5 inhibited strongly the PAK1 activation by PDGF stimulation and cell motility in PDGF-induced wound migration assay in NIH 3T3 cells. Therefore, these NQ compounds will be good candidates as target molecules to regulate PAK1-related diseases or inhibitors to study PAK1 signaling pathway.
Identification of Osteogenic Purmorphamine Derivatives
이성진,이학교,조성윤,최중권,신혜경,곽은정,조미란,김혜련,김승렬,김용민,박경진,최중국 한국분자세포생물학회 2008 Molecules and cells Vol.26 No.4
During embryonic and cancer development, the Hedgehog family of proteins, including Sonic Hedgehog, play an important role by relieving the inhibition of Smo by Ptc, thus activating the Smo signaling cascade. Recently, a purine compound, purmorphamine, has been reported to target the Hedgehog signaling pathway by interacting with Smo. Interestingly, both Sonic Hedgehog and purmorphamine were found to promote the osteogenic differentiation of mouse chondroprogenitor cells. However, there is insufficient information as to how the activation of this seemingly unrelated signaling pathway, either by Sonic Hedgehog or purmorphamine, contributes to osteogenesis. Using alkaline phosphatase assays, we screened 125 purmorphamine derivatives from the Korea Chemical Bank for effects on the differentiation of preosteoblast C2C12 cells. Here, we report that two purine derivatives modulate ALP activity as well as the expression of genes whose expression is known or suggested to be involved in osteogenesis.
박노상(No Sang Park),김현숙(Hyun Sook Kim),민창희(Chang Hee Min),최중권(Joong Kwon Choi) 대한약학회 1990 약학회지 Vol.34 No.2
3-Substituted 5-aminoisoxazole-4-carboxylates were prepared by the reaction of corresponding bormoaldoximes with cyanoacetate. The 3-trifluoromethylisoxazole derivatives were acylated to amides with various aminopyridine derivatives to afford diamides. The ester group was hydrolyzed and decarboxylated easily to give 3-trifluoromethyl-5-aminoisoxazole. The aminoisoxazole was also converted to amides. 5-Amino-3-trifluoromethylisoxazole-5-one-4-carboxylate was prepared by the reaction of trifluoroacetoaldoximoyl bromide and malonate. 5-Amino-3-methylisoxazole-5-one-4-acetate was prepared by the reaction of hydroxylamine and acetylmalonate. The synthesized compounds were tested for antiinflammatory activities.
Benzotriazepin 유도체의 암세포에 대한 다약제내성 억제효과
김미혜(Mi Hye Kim),최상운(Sang Un Choi),최은정(Eun Jung Choi),김성수(Sung Soo Kim),최중권(Jung Kwon Choi),안진희(Jin Hee Ahn),이정옥(Chong Ock Lee),권광일(Kwang ll Kwon) 대한약학회 2005 약학회지 Vol.49 No.1
The occurrence of resistance to chemotherapeutic drugs is a major problem for successful cancer treatment. This resistant phenotype of cancer cell frequently reveals a broad spectrum to structurally and/or functionally unrelated anti-cancer drugs, termed multidrug resistance (MDR). Overexpression of P-glycoprotein (P-gp), a transmembrane drug efflux pump, is a major mechanism of MDR. Accordingly, considerable effort has been directed towards to development of compounds that inhibit P-gp, reverse the MDR phenotype and sensitize cancer cells to conventional chemotherapy without undesired toxicological effects. In an effort to search for novel MDR reversal agent, we tested the cytotoxicity of paclitaxel, a well-known substrate of P-gp, against P-gp-expressing HCT15 and HCT15/CL02 human colorectal cancer cells in the presence or absence of benzotriazepin analogues, as well as against P-gp-negative A549 human non-small cell lung and SK-OV-3 human ovarian cancer cells in vitro. Among the compounds tested, the agents that have phenyl amide moiety at 3 position remarkably increased the cytotoxicity of paclitaxel against P-gp-expressing cancer cells, but not against P-gp-negative cancer cells. BTZ-15 and BTZ-16 at 4μM revealed similar MDR reversal activity to 10μM verapamil, a well-known MDR reversal agent.