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961.
Sul OJ Kim JC Kyung TW Kim HJ Kim YY Kim SH Kim JS Choi HS 《Bioscience, biotechnology, and biochemistry》2010,74(11):2209-2213
Gold nanoparticles inhibited osteoclast (OC) formation induced by the receptor activator of nuclear factor-κB ligand (RANKL) in bone marrow-derived macrophages (BMMs). This was accompanied by a decreased level of tartrate-resistant alkaline phosphatase (TRAP) and less activation of nuclear factor (NF)-κB. The nanoparticles also reduced the production of reactive oxygen species (ROS) in response to RANKL and upregulated RANKL-induced glutathione peroxidase-1 (Gpx-1), suggesting a role as an antioxidant in the BMM. The inhibitory effects on OC formation might have been due to elevated defense against oxidative stress. 相似文献
962.
A novel approach CE-Ploc is proposed for predicting protein subcellular locations by exploiting diversity both in feature and decision spaces. The
diversity in a sequence of feature spaces is exploited using hydrophobicity and hydrophilicity of amphiphilic pseudo amino
acid composition and a specific learning mechanism. Diversity in learning mechanisms is exploited by fusion of classifiers
that are based on different learning mechanisms. Significant improvement in prediction performance is observed using jackknife
and independent dataset tests. 相似文献
963.
964.
965.
Young Ae Yoon Chan Sun Park Myung Hun Cha Hyunho Choi Jae Young Sim Jae Gyu Kim 《Bioorganic & medicinal chemistry letters》2010,20(19):5735-5738
A series of pyrimidine derivatives as acid pump antagonists (APAs) was synthesized and the inhibitory activities against H+/K+ ATPase isolated from hog gastric mucosa were determined. After elaborating on substituents at C2 and C4 position of the pyrimidine scaffold, we have observed that the compound 7h is a potent APA with H+/K+ ATPase, IC50 = 52 nM. 相似文献
966.
Jehun Choi Sung Jin Bae Young Mi Ha Jae Kyung No Eun Kyeong Lee Jun Sik Lee Suhee Song Hyojin Lee Hongsuk Suh Byung Pal Yu Hae Young Chung 《Bioorganic & medicinal chemistry letters》2010,20(16):4882-4884
In searching for new agents with a depigmenting effect, we synthesized a derivative of resveratrol, 5-(6-hydroxy-2-naphthyl)-1,2,3-benzenetriol (5HNB) with a potent tyrosinase inhibitory activity. 5HNB inhibited mushroom tyrosinase with an IC50 value of 2.95 μM, which is more potent than the well-known anti-tyrosinase activity of kojic acid (IC50 = 38.24). The results of the enzymatic inhibition kinetics by Lineweaver–Burk analysis indicated 5HNB inhibits tyrosinase non-competitively when l-tyrosine was used as the substrate. Based on the strong inhibitory action of 5HNB, it is expected that 5HNB can suppress melanin production in which tyrosinase plays the essential role. Our expectation was confirmed by the experimentations with B16 melanoma cells in which 5HNB inhibited melanin production. We propose that 5HNB might have skin-whitening effects as well as therapeutic potential for treating skin pigmentation disorders. 相似文献
967.
Hee Jin Kim Myung-Ho Jung Hwan Kim Mohammed I. El-Gamal Tae Bo Sim So Ha Lee Jun Hee Hong Jung-Mi Hah Jung-Hyuck Cho Jung Hoon Choi Kyung Ho Yoo Chang-Hyun Oh 《Bioorganic & medicinal chemistry letters》2010,20(1):413-417
Synthesis of a new series of diarylureas and amides having pyrrolo[3,2-b]pyridine scaffold is described. Their in vitro antiproliferative activity against human melanoma cell line A375 and HS 27 human fibroblast cell line was tested and the effect of substituents on the pyrrolo[3,2-b]pyridine was investigated. The newly synthesized compounds, except meta-substituted derivatives (Ij–k and Iv–w), generally showed superior or similar activity against A375 to Sorafenib. Among all of these derivatives, compounds Ir and It having 5-benzylamide substituted 4′-amide moieties showed the most potent antiproliferative activity against A375. 相似文献
968.
Chul Min Park So Young Kim Woo Kyu Park Jung Hwan Choi Churl Min Seong 《Bioorganic & medicinal chemistry letters》2010,20(17):5221-5224
(Piperazin-1-yl-phenyl)-arylsulfonamides were synthesized and identified to show high affinities for both 5-HT2C and 5-HT6 receptors. Among them, naphthalene-2-sulfonic acid isopropyl-[3-(4-methyl-piperazin-1-yl)-phenyl]-amide (6b) exhibits the highest affinity towards both 5-HT2C (IC50 = 4 nM) and 5-HT6 receptors (IC50 = 3 nM) with good selectivity over other serotonin (5-HT1A, 5-HT2A, and 5-HT7) and dopamine (D2–D4) receptor subtypes. In 5-HT2C and 5-HT6 receptor functional assays, this compound showed considerable antagonistic activity for both receptors. 相似文献
969.
Thommey P. Thomas Seok Ki Choi Ming-Hsin Li Alina Kotlyar James R. Baker 《Bioorganic & medicinal chemistry letters》2010,20(17):5191-5194
This communication describes the synthesis and in vitro biological evaluation of novel generation 5 PAMAM dendrimers conjugated with riboflavin as a targeting ligand. Cell-based experiments demonstrated that a dendrimer conjugated with riboflavin is able to undergo cellular binding and uptake in KB cells, and when the dendrimer is also conjugated with methotrexate, the riboflavin dendrimer conjugate can potently inhibit cell growth. 相似文献
970.