Folia Pharmacologica Japonica最新文献_第3页

[The potential of BCL6B as a therapeutic target for chorioretinal vascular lesions]. BCL6B作为绒毛膜视网膜血管病变治疗靶点的潜力。

Folia Pharmacologica Japonica Pub Date : 2025-01-01 DOI: 10.1254/fpj.24064

Shinsuke Nakamura, Hideaki Hara

引用次数: 0

[The 77th Regional Meeting (Seinan Area)]. [第77届区域会议（塞南地区）]。

Folia Pharmacologica Japonica Pub Date : 2025-01-01 DOI: 10.1254/fpj.S24105

引用次数: 0

Folia Pharmacologica Japonica Pub Date : 2025-01-01 DOI: 10.1254/fpj.25003

Shigeo Miyata

引用次数: 0

[Preface]. (前言)。

Folia Pharmacologica Japonica Pub Date : 2025-01-01 DOI: 10.1254/fpj.24079

Youichi Shinozaki, Shinsuke Nakamura

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[Pharmacological properties and clinical trial results of the novel calcium-sensing receptor agonist upacicalcet sodium hydrate (Upacita^® intravenous injection for dialysis)]. 【新型钙敏感受体激动剂upacicalcet sodium hydrate （Upacita®透析静脉注射）的药理学特性及临床试验结果】。

Folia Pharmacologica Japonica Pub Date : 2025-01-01 DOI: 10.1254/fpj.24108

Takeju Otsuki, Seigo Akari, Naomi Kashiwagi, Yoshiyuki Ono

{"title":"[Pharmacological properties and clinical trial results of the novel calcium-sensing receptor agonist upacicalcet sodium hydrate (Upacita® intravenous injection for dialysis)].","authors":"Takeju Otsuki, Seigo Akari, Naomi Kashiwagi, Yoshiyuki Ono","doi":"10.1254/fpj.24108","DOIUrl":"https://doi.org/10.1254/fpj.24108","url":null,"abstract":"Upacicalcet sodium hydrate (upacicalcet) is a novel small-molecule calcium-sensing receptor (CaSR) modulator with an amino acid structure, developed in Japan as a derivative from research into taste enhancement. Upacicalcet specifically targets CaSR and is thought to inhibit parathyroid hormone (PTH) secretion by activating the receptor in the presence of extracellular calcium (Ca). In nonclinical studies, upacicalcet was evaluated for its pharmacological properties, binding characteristics, and effects on ectopic calcification, parathyroid hyperplasia, and bone disorders associated with secondary hyperparathyroidism (SHPT). The results supported its mechanisms of action, binding mode, and efficacy in suppressing disease progression. In clinical trials, upacicalcet demonstrated efficacy and safety in patients with SHPT undergoing hemodialysis, as assessed in domestic Phase I/II trial (AJ1001 trial), Phase II trial (AJ1002 trial), Phase III placebo-controlled trial (AJ1004 trial), and Phase III long-term administration trial (AJ1003 trial). Upacicalcet was approved in June 2021 for the treatment of secondary hyperparathyroidism (SHPT) in patients undergoing hemodialysis and was launched in August of the same year.","PeriodicalId":12208,"journal":{"name":"Folia Pharmacologica Japonica","volume":"160 3","pages":"207-219"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143971595","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

[A remarkable advancement in structural biology aimed at elucidating the ‍mechanism of synovial sarcoma development]. [结构生物学的一个显著进展，旨在阐明‍滑膜肉瘤发展的机制]。

Folia Pharmacologica Japonica Pub Date : 2025-01-01 DOI: 10.1254/fpj.25013

Kenji Iwasaki, Satoshi Takenaka

{"title":"[A remarkable advancement in structural biology aimed at elucidating the ‍mechanism of synovial sarcoma development].","authors":"Kenji Iwasaki, Satoshi Takenaka","doi":"10.1254/fpj.25013","DOIUrl":"https://doi.org/10.1254/fpj.25013","url":null,"abstract":"Synovial sarcoma is a type of soft tissue sarcoma that predominantly occurs near the joints of the extremities in young adults. Its hallmark is a recurrent and pathogenic chromosomal translocation, t(X;18)(p11.2;q11.2), which results in the fusion of the SSX1 or SSX2 gene with SS18. The expressed SS18-SSX fusion protein induces abnormalities in the SWItch/Sucrose Non-Fermentable (SWI/SNF) complex, a chromatin remodeling complex. In this paper, we refer specifically to the human SWI/SNF complex as mSWI/SNF. Since 2020, significant progress has been made in elucidating the molecular mechanisms underlying the initial event in synovial sarcomagenesis, particularly in structural biology, thereby opening new possibilities for structure-based drug design (SBDD). SS18-SSX1 replaces the wild-type SS18, an essential subunit of mSWI/SNF, and in turn ejects SMARCB1, another core subunit of the complex. This aberrant mSWI/SNF complex (ssSWI/SNF) is then relocated to nucleosomes containing H2A K119Ub. H2A is one of the core histone proteins, and its 119th lysine residue is ubiquitinated to form H2A K119Ub. Chromatin domains harboring nucleosomes with this modification typically exhibit suppressed gene expression patterns. Furthermore, this region is occupied by polycomb complexes, but ssSWI/SNF competes with them, leading to gene activation, which constitutes the initial event in synovial sarcomagenesis. Given that SSX1 is normally expressed primarily in the testes, it is plausible that its ectopic expression leads to aberrant function within the chromatin remodeling complex. Ultimately, the C-terminal region of SSX1 was found to bind to the acidic patch within the nucleosome, and its structural details have been elucidated through cryo-electron microscopy.","PeriodicalId":12208,"journal":{"name":"Folia Pharmacologica Japonica","volume":"160 3","pages":"167-171"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143974055","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

[Nationwide survey of practice after COVID-19 pandemic conducted in medical schools]. [新冠肺炎大流行后全国医学院实践情况调查]。

Folia Pharmacologica Japonica Pub Date : 2025-01-01 DOI: 10.1254/fpj.25010

Masaki Mogi, Shung Liu

引用次数: 0

[Physiologically-based pharmacokinetic model analysis of antipsychotic risperidone and its active metabolite paliperidone in perinatal period]. [抗精神病药物利培酮及其活性代谢物帕利哌酮在围产期的生理药代动力学模型分析]。

Folia Pharmacologica Japonica Pub Date : 2025-01-01 DOI: 10.1254/fpj.24065

Ikuko Yano

{"title":"[Physiologically-based pharmacokinetic model analysis of antipsychotic risperidone and its active metabolite paliperidone in perinatal period].","authors":"Ikuko Yano","doi":"10.1254/fpj.24065","DOIUrl":"10.1254/fpj.24065","url":null,"abstract":"Pregnancy can affect the absorption, distribution, metabolism, and excretion of several drugs due to pregnancy-induced physiological changes. Risperidone, a second-generation antipsychotic, is prescribed to pregnant women when the benefits outweigh the risks to the fetus. Serum concentrations of risperidone and its active metabolite paliperidone in a pregnant woman as well as her newborn were measured, and physiologically-based pharmacokinetic (PBPK) models of both drugs were developed. The effects of pregnancy on pharmacokinetic parameters of both drugs were quantitively assessed by the developed PBPK model. As a result, serum concentrations of risperidone and paliperidone decrease in the pregnant status and abruptly recover to the non-pregnant level after delivery mainly due to cytochrome P450 (CYP) 2D6 activity changes, and therefore, close and careful monitoring of clinical symptoms should be considered during pregnancy and after delivery. In the 10 different models for estimating the renal function of children, the Flanders metadata equation showed the lowest absolute bias and the greatest precision in predicting paliperidone serum concentration in the neonate. PBPK model-informed approach could help with the precision dosing in special populations, such as pregnant women and neonates.","PeriodicalId":12208,"journal":{"name":"Folia Pharmacologica Japonica","volume":"160 2","pages":"103-107"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143537006","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Folia Pharmacologica Japonica Pub Date : 2025-01-01 DOI: 10.1254/fpj.24087

Eiichi Taira

引用次数: 0

[Drug discovery using iPS cells and in silico model]. [利用iPS细胞和计算机模型发现药物]。

Folia Pharmacologica Japonica Pub Date : 2025-01-01 DOI: 10.1254/fpj.24046

Yuya Fujiwara, Yoshinori Yoshida

{"title":"[Drug discovery using iPS cells and in silico model].","authors":"Yuya Fujiwara, Yoshinori Yoshida","doi":"10.1254/fpj.24046","DOIUrl":"https://doi.org/10.1254/fpj.24046","url":null,"abstract":"Human induced pluripotent stem cells derived cardiomyocytes (hiPSC-CMs) can recapitulate the properties of human cardiomyocyte and exhibit disease phenotypes in vitro, attributable to their healthy- or patient-specific genetic backgrounds. Therefore, hiPSC-CMs are a crucial tool for developing therapeutic agents for cardiovascular diseases, and regenerative medicine using hiPSC-CMs is expected to be an alternative therapy to heart transplantation. Moreover, the development of organoid models has been advanced to replicate the complex structure of heart tissue in vitro, thereby effectively facilitating drug discovery. On the other hand, current methods for advancing drug discovery using hiPSC-CMs face limitations, including the difficulty of quantifying characteristics such as cell structure and predicting the risk and efficacy of candidate drug in clinical practice. In the field of regenerative medicine, challenges include quality control and the verification of safety of transplanted cells in human. In silico model, including artificial intelligence (AI) and simulation, have been developed in the field of drug discovery using hiPSC-CMs. These advancements encompass phenotype scoring via AI and risk prediction through simulations. This review outlines the current status and challenges of drug discovery using hiPSC-CMs and in silico model, based on the published reports.","PeriodicalId":12208,"journal":{"name":"Folia Pharmacologica Japonica","volume":"160 1","pages":"13-17"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142931070","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0