Folia Pharmacologica Japonica最新文献_第10页

[The plasma protein HRG is an important factor for preventing sepsis and maintaining homeostatic response]. [血浆蛋白 HRG 是预防败血症和维持平衡反应的重要因素】。］

Folia Pharmacologica Japonica Pub Date : 2024-01-01 DOI: 10.1254/fpj.23027

Masahiro Nishibori, Hidenori Wake, Masakiyo Sakaguchi

{"title":"[The plasma protein HRG is an important factor for preventing sepsis and maintaining homeostatic response].","authors":"Masahiro Nishibori, Hidenori Wake, Masakiyo Sakaguchi","doi":"10.1254/fpj.23027","DOIUrl":"10.1254/fpj.23027","url":null,"abstract":"Acute phase proteins such as CRP, amyloid protein A, and α1-antitrypsin are produced in the liver and their plasma levels are increased during the acute inflammatory response. In contrast, there are plasma proteins whose dynamics are opposite to acute phase proteins. This group includes histidine-rich glycoprotein (HRG), inter-α-inhibitor proteins, albumin, and transthyretin. HRG binds to a variety of factors and regulates the fundamental processes; the blood coagulation, the clearance of apoptotic cells, and tumor growth. In the present review, we focus on the anti-septic effects of HRG in mice model, the actions of HRG on human blood cells/vascular endothelial cells, and the identification of a novel receptor CLEC1A for HRG, based on our recent findings. HRG appears to maintain the quiescence of neutrophils; a round shape, the low levels of spontaneous release of ROS, the ease passage through artificial microcapillaries, and prevention of adhesion to vascular endothelial cells. HRG also inhibited activation of vascular endothelial cells; the suppression of adhesion molecules and the inhibition of HMGB1 mobilization and cytokine secretion. It was shown that plasma HRG level was an excellent biomarker of septic patients in ICU for the evaluation of severity and prognosis. So far little attention has been paid to HRG in terms of a functional role in sepsis and ARDS, however, it is strongly suggested that HRG may be an important plasma factor that prevents a progress in the septic cascade and maintains the homeostasis of blood cells and vascular endothelial cells.","PeriodicalId":12208,"journal":{"name":"Folia Pharmacologica Japonica","volume":"159 2","pages":"107-111"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140021333","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

[Preface]. [序言]。

Folia Pharmacologica Japonica Pub Date : 2024-01-01 DOI: 10.1254/fpj.23099

Ichiro Kawahata, Masahiro Nagai

引用次数: 0

[Recent advances in understanding of basophil function and differentiation]. [了解嗜碱性粒细胞功能和分化的最新进展]。

Folia Pharmacologica Japonica Pub Date : 2024-01-01 DOI: 10.1254/fpj.23084

Kensuke Miyake, Junya Ito, Hajime Karasuyama

引用次数: 0

[Strategy for the development of small-molecule antidepressant targeting PAC1 receptor]. [以 PAC1 受体为靶点的小分子抗抑郁药的开发策略]。

Folia Pharmacologica Japonica Pub Date : 2024-01-01 DOI: 10.1254/fpj.24008

Ichiro Takasaki, Atsuko Hayata-Takano, Yusuke Shintani, Takashi Kurihara, Hitoshi Hashimoto

{"title":"[Strategy for the development of small-molecule antidepressant targeting PAC1 receptor].","authors":"Ichiro Takasaki, Atsuko Hayata-Takano, Yusuke Shintani, Takashi Kurihara, Hitoshi Hashimoto","doi":"10.1254/fpj.24008","DOIUrl":"10.1254/fpj.24008","url":null,"abstract":"Major depressive disorder (MDD) is a psychiatric disorder that affects more than 300 million people worldwide and has a serious impact on society. Conventional antidepressants targeting monoamines in the brain based on the monoamine hypothesis are known to take a prolonged time to be effective or less effective in 30% of MDD patients. Hence, there is a need to develop antidepressants that are effective against treatment-resistant depression and have a new mechanism different from the monoamine hypothesis. An increasing number of research groups including us have been establishing that pituitary adenylate cyclase-activating polypeptide (PACAP) and one of its receptors, PAC1 receptor, are closely related to the etiology of stress-related diseases such as MDD. Therefore, it is strongly suggested that the PAC1 receptor is a promising target in the treatment of psychiatric disorders. We developed a novel, non-peptidic, small-molecule, high-affinity PAC1 receptor antagonists and conducted behavioral pharmacology experiments in mice to characterize a novel PAC1 receptor antagonist as a new option for MDD therapy. The results show that our novel PAC1 receptor antagonist has the potential to be a new antidepressant with a high safety profile. In this review, we would like to present the background of developing our novel PAC1 receptor antagonist and its effects on mouse models of acute stress.","PeriodicalId":12208,"journal":{"name":"Folia Pharmacologica Japonica","volume":"159 4","pages":"219-224"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141467237","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 : 2024-01-01 DOI: 10.1254/fpj.24067

Hideki Ono

引用次数: 0

[The quick screening of binding compounds and proteins for drug discovery and pharmacological research]. [用于药物发现和药理学研究的结合化合物和蛋白质快速筛选]。

Folia Pharmacologica Japonica Pub Date : 2024-01-01 DOI: 10.1254/fpj.24057

Naoki Tarui

{"title":"[The quick screening of binding compounds and proteins for drug discovery and pharmacological research].","authors":"Naoki Tarui","doi":"10.1254/fpj.24057","DOIUrl":"10.1254/fpj.24057","url":null,"abstract":"In drug discovery and pharmacological research, early identification of target molecules for compounds with pharmacological effects is crucial. However, this process often requires significant effort and can be rate-limiting, thereby slowing down research progress. This paper introduces a simplified and rapid method for quick screening of binding compounds or proteins. Utilizing Affinity Selection Mass Spectrometry (ASMS), this technique efficiently detects compound-target binding through size-exclusion chromatography and mass spectrometry. ASMS offers high sensitivity and specificity, making it ideal for accurate identification of binding interactions. We have further enhanced ASMS to handle membrane proteins without solubilization, creating Binder Selection Technology (BST). BST allows screening against both soluble and challenging membrane proteins such as GPCRs and SLC transporters. By using cell membrane fractions or organelle fractions with high target molecule expression, BST efficiently identifies potential binding compounds. This innovative method constructs a comprehensive database of binding compounds for various targets, facilitating rapid hypothesis testing and pharmacological evaluation. Additionally, BST screens 17,000 proteins, including membrane proteins, using wheat germ cell-free and animal cell expression systems. This approach allows exploration of binding interactions without labeling compounds or immobilizing proteins, preserving their native state. BST is powerful for identifying targets of compounds with known pharmacological effects but unknown targets in animal or cell-based assays. By utilizing BST, researchers can overcome bottlenecks in early drug discovery, significantly enhancing research speed and success rates. This method represents a major advancement, providing an efficient and effective way to identify and validate target molecules in drug discovery.","PeriodicalId":12208,"journal":{"name":"Folia Pharmacologica Japonica","volume":"159 6","pages":"407-412"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142575631","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

[Preface]. [序言]。

Folia Pharmacologica Japonica Pub Date : 2024-01-01 DOI: 10.1254/fpj.24042

Shigeo Miyata, Sayaka Takemoto-Kimura

引用次数: 0

[Possibility of short synthetic peptides with activities of suppressing amyloid β aggregation and resolving its aggregated form as therapeutic drugs for Alzheimer's disease]. [具有抑制淀粉样蛋白 β 聚集和分解其聚集形式活性的短合成肽作为阿尔茨海默病治疗药物的可能性]。

Folia Pharmacologica Japonica Pub Date : 2024-01-01 DOI: 10.1254/fpj.24077

Youichirou Higashi

{"title":"[Possibility of short synthetic peptides with activities of suppressing amyloid β aggregation and resolving its aggregated form as therapeutic drugs for Alzheimer's disease].","authors":"Youichirou Higashi","doi":"10.1254/fpj.24077","DOIUrl":"https://doi.org/10.1254/fpj.24077","url":null,"abstract":"Lecanemab is a new anti-amyloid antibody being developed as a treatment for Alzheimer's disease. It is expected to delay the progression of the disease by reducing the accumulation of amyloid beta (Aβ) in the brain. However, no drug has been developed that can completely eliminate Aβ and improve symptoms. A representative Catalytide, JAL-TA9 (YKGSGFRMI), cleaves Aβ42 and improves symptoms in an Alzheimer's disease mouse model, suggesting that JAL-TA9 is a promising candidate for treating Alzheimer's disease by effectively eliminating Aβ. The catalytic center of JAL-TA9 is GSGFR. To identify better Catalytides for Alzheimer's treatment, we analyzed the structure-activity relationship of 21 point-mutated GSGFR derivatives. In this process, we discovered two peptides, GSGFK and GSGNR, that not only inhibit Aβ25-35 aggregation but also dissolve aggregated Aβ25-35. Intracerebroventricular administration of GSGFK protected mice against Aβ25-35-induced short-term memory deficits and promoted microglial phagocytic activity. Like Lecanemab, GSGFK targets Aβ, but it has advantages such as safety, administration method, and cost. In this talk, we will discuss the potential of GSGFK as a therapeutic candidate for Alzheimer's disease.","PeriodicalId":12208,"journal":{"name":"Folia Pharmacologica Japonica","volume":"159 6","pages":"402-406"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142575619","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

[Preface]. [序言]。

Folia Pharmacologica Japonica Pub Date : 2024-01-01 DOI: 10.1254/fpj.24031

Kazuhiro Tamura, Fuminori Taniguchi

引用次数: 0

[Preface]. [序言]。

Folia Pharmacologica Japonica Pub Date : 2024-01-01 DOI: 10.1254/fpj.24078

Shogo Tokuyama

引用次数: 0