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排序方式: 共有298条查询结果,搜索用时 15 毫秒
61.
Ohta H Sato K Murata N Damirin A Malchinkhuu E Kon J Kimura T Tobo M Yamazaki Y Watanabe T Yagi M Sato M Suzuki R Murooka H Sakai T Nishitoba T Im DS Nochi H Tamoto K Tomura H Okajima F 《Molecular pharmacology》2003,64(4):994-1005
Lysophosphatidic acid (LPA) exerts a variety of biological responses through specific receptors: three subtypes of the EDG-family receptors, LPA1, LPA2, and LPA3 (formerly known as EDG-2, EDG-4, and EDG-7, respectively), and LPA4/GPR23, structurally distinct from the EDG-family receptors, have so far been identified. In the present study, we characterized the action mechanisms of 3-(4-[4-([1-(2-chlorophenyl)ethoxy]carbonyl amino)-3-methyl-5-isoxazolyl] benzylsulfanyl) propanoic acid (Ki16425) on the EDG-family LPA receptors. Ki16425 inhibited several responses specific to LPA, depending on the cell types, without any appreciable effect on the responses to other related lipid receptor agonists, including sphingosine 1-phosphate. With the cells overexpressing LPA1, LPA2, or LPA3, we examined the selectivity and mode of inhibition by Ki16425 against the LPA-induced actions and compared them with those of dioctyl glycerol pyrophosphate (DGPP 8:0), a recently identified antagonist for LPA receptors. Ki16425 inhibited the LPA-induced response in the decreasing order of LPA1 >/= LPA3 > LPA2, whereas DGPP 8:0 preferentially inhibited the LPA3-induced actions. Ki16425 inhibited LPA-induced guanosine 5'-O-(3-thio)triphosphate binding as well as LPA receptor binding to membrane fractions with a same pharmacological specificity as in intact cells. The difference in the inhibition profile of Ki16425 and DGPP 8:0 was exploited for the evaluation of receptor subtypes involved in responses to LPA in A431 cells. Finally, Ki16425 also inhibited LPA-induced long-term responses, including DNA synthesis and cell migration. In conclusion, Ki16425 selectively inhibits LPA receptor-mediated actions, especially through LPA1 and LPA3; therefore, it may be useful in evaluating the role of LPA and its receptor subtypes involved in biological actions. 相似文献
62.
Sasaki Yoshiyuki Hokuto Daisuke Inoue Takashi Nomi Takeo Yoshikawa Takahiro Matsuo Yasuko Koyama Fumikazu Sho Masayuki 《Annals of surgical oncology》2019,26(12):3982-3989
Annals of Surgical Oncology - Herpesvirus entry mediator (HVEM) has been suggested to play various roles in cancer biology. The authors report that HVEM expression in tumor cells is associated with... 相似文献
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We evaluated the safety and efficacy of ethyl loflazepate in children with epilepsy. The study group comprised 21 outpatients (4 by generalized, 17 by localization-related) aged between 9 months and 17 years. Ethyl loflazepate was administered at a dose of 0.015 mg/kg/day twice daily. The final mean dose was 1.35 mg/day. The mean number of prior antiepileptic drugs was 5.7. The entire treatment period was more than 24 months after ethyl loflazepate administration. Six children (28.6%) became seizure-free for the entire study 6 months after administration, 11 (52.4%) had a seizure reduction of more than 50% for over entire 24 months. The mean number of co-medications was 2.4. Adverse events occurred in only 1 patient. Responders, defined as reduction of ≥50% in seizure frequency, included 2/2 of patients with West syndrome and 15/17 (88.2%) with localization-related epilepsy. Ethyl loflazepate represents an important addition to the treatments available for refractory epilepsies in children. 相似文献
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Komachi M Sato K Tobo M Mogi C Yamada T Ohta H Tomura H Kimura T Im DS Yanagida K Ishii S Takeyoshi I Okajima F 《Cancer science》2012,103(6):1099-1104
Pancreatic cancer is highly metastatic and has a poor prognosis. However, there is no established treatment for pancreatic cancer. Lysophosphatidic acid (LPA) has been shown to be present in effluents of cancers and involved in migration and proliferation in a variety of cancer cells, including pancreatic cancer cells, in vitro. In the current study, we examined whether an orally active LPA antagonist is effective for pancreatic cancer tumorigenesis and metastasis in vivo. Oral administration of Ki16198, which is effective for LPA(1) and LPA(3), into YAPC-PD pancreatic cancer cell-inoculated nude mice significantly inhibited tumor weight and remarkably attenuated invasion and metastasis to lung, liver, and brain, in association with inhibition of matrix metalloproteinase (MMP) accumulation in ascites in vivo. Ki16198 inhibited LPA-induced migration and invasion in several pancreatic cancer cells in vitro, which was associated with the inhibition of LPA-induced MMP production. In conclusion, Ki16198 is a promising orally active LPA antagonist for inhibiting the invasion and metastasis of pancreatic cancer cells. The inhibitory effects of the antagonist on invasion and metastasis in vivo may be partially explained by the inhibition of motility activity and MMP production in cancer cells. 相似文献
69.
Fumiko Kimura Tatsuo Umezawa Tomonari Asano Ruri Chihara Naoko Nishi Shigeyoshi Nishimura Fumikazu Sakai 《Japanese journal of radiology》2010,28(6):437-445
Purpose
We compared stair-step artifacts and radiation dose between prospective electrocardiography (ECG)-gated coronary computed tomography angiography (prospective CCTA) and retrospective CCTA using 64-detector CT and determined the optimal padding time (PT) for prospective CCTA. 相似文献70.
Takashi Inoue Hisao Fujii Fumikazu Koyama Shinji Nakamura Takeshi Ueda Naoto Nishigori Keijiro Kawasaki Shinsaku Obara Takayuki Nakamoto Kazuaki Uchimoto Kohei Morita Takeshi Nishikawa Chiho Ohbayashi Yoshiyuki Nakajima 《Surgical endoscopy》2016,30(7):2773-2778