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ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology最新文献

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Early-stage Development of anin vitroScreening Assay to Characterize the Activation of Human Adhesion Receptor ADGRE5 人类黏附受体ADGRE5激活的蛋白体外筛选试验的早期发展
ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology Pub Date : 2023-05-18 DOI: 10.1124/jpet.122.149430
A. Mancini, Samy Aouad, Herthana Kandasamy, R. Cerone, S. Schann, L. Sabbagh
{"title":"Early-stage Development of anin vitroScreening Assay to Characterize the Activation of Human Adhesion Receptor ADGRE5","authors":"A. Mancini, Samy Aouad, Herthana Kandasamy, R. Cerone, S. Schann, L. Sabbagh","doi":"10.1124/jpet.122.149430","DOIUrl":"https://doi.org/10.1124/jpet.122.149430","url":null,"abstract":"","PeriodicalId":406842,"journal":{"name":"ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology","volume":"110 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"117211686","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
Structure–Activity Relationships of a Brain-Penetrant D3 Dopamine Receptor Negative Allosteric Modulator and Investigation of its Binding Site 脑渗透D3多巴胺受体负变构调节剂的构效关系及其结合位点的研究
ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology Pub Date : 2023-05-18 DOI: 10.1124/jpet.122.157730
Amy E. Moritz, Nora S. Madaras, Laura R. Inbody, Amber M. Kelley, Disha M. Gandhi, E. Akano, Kuo-Hao Lee, R. Free, Xin Hu, Noel Southall, M. Ferrer, Lei Shi, K. Frankowski, David R. Sibley
{"title":"Structure–Activity Relationships of a Brain-Penetrant D3 Dopamine Receptor Negative Allosteric Modulator and Investigation of its Binding Site","authors":"Amy E. Moritz, Nora S. Madaras, Laura R. Inbody, Amber M. Kelley, Disha M. Gandhi, E. Akano, Kuo-Hao Lee, R. Free, Xin Hu, Noel Southall, M. Ferrer, Lei Shi, K. Frankowski, David R. Sibley","doi":"10.1124/jpet.122.157730","DOIUrl":"https://doi.org/10.1124/jpet.122.157730","url":null,"abstract":",","PeriodicalId":406842,"journal":{"name":"ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology","volume":"41 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"133237344","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
Podocyte injury triggers the formation of intercellular bridges 足细胞损伤触发细胞间桥的形成
ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology Pub Date : 2023-05-18 DOI: 10.1124/jpet.122.264830
Nina Cintron Pregosin, S. Mallipattu
{"title":"Podocyte injury triggers the formation of intercellular bridges","authors":"Nina Cintron Pregosin, S. Mallipattu","doi":"10.1124/jpet.122.264830","DOIUrl":"https://doi.org/10.1124/jpet.122.264830","url":null,"abstract":"Abstract","PeriodicalId":406842,"journal":{"name":"ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology","volume":"44 16","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"113942017","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
Regulation of GPCR Signaling by Sorting Nexins 通过筛选连接蛋白调控GPCR信号传导
ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology Pub Date : 2023-05-18 DOI: 10.1124/jpet.122.276700
Valeria L Robleto, Y. Zhuo, J. Crecelius, A. Marchese
{"title":"Regulation of GPCR Signaling by Sorting Nexins","authors":"Valeria L Robleto, Y. Zhuo, J. Crecelius, A. Marchese","doi":"10.1124/jpet.122.276700","DOIUrl":"https://doi.org/10.1124/jpet.122.276700","url":null,"abstract":"","PeriodicalId":406842,"journal":{"name":"ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology","volume":"229 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"115948168","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
The Adhesion GPCR GPR114/ADGRG5 is Activated by its Tethered-Peptide-Agonist Following Receptor Fragment Dissociation 粘附GPCR GPR114/ADGRG5在受体片段解离后被其栓系肽激动剂激活
ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology Pub Date : 2023-05-18 DOI: 10.1124/jpet.122.173960
Tyler F Bernadyn, Rashmi Adhikari, Alex Vizurraga, Frank E. Kwarcinski, Gregory G. Tall
{"title":"The Adhesion GPCR GPR114/ADGRG5 is Activated by its Tethered-Peptide-Agonist Following Receptor Fragment Dissociation","authors":"Tyler F Bernadyn, Rashmi Adhikari, Alex Vizurraga, Frank E. Kwarcinski, Gregory G. Tall","doi":"10.1124/jpet.122.173960","DOIUrl":"https://doi.org/10.1124/jpet.122.173960","url":null,"abstract":"","PeriodicalId":406842,"journal":{"name":"ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology","volume":"23 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"117099747","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
ACAT-1 Inhibition Limits iNOS in anIn VitroModel of Macrophage Activation ACAT-1抑制在巨噬细胞活化的体外模型中限制iNOS
ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology Pub Date : 2023-05-18 DOI: 10.1124/jpet.122.293390
Sung Jae Lee, E. Stevenson, A. Gow
{"title":"ACAT-1 Inhibition Limits iNOS in anIn VitroModel of Macrophage Activation","authors":"Sung Jae Lee, E. Stevenson, A. Gow","doi":"10.1124/jpet.122.293390","DOIUrl":"https://doi.org/10.1124/jpet.122.293390","url":null,"abstract":"Each year in the United States, there are 190,600 cases of acute lung injury (ALI), associated with a mortality rate of over 74,000 deaths. Data shows acyl ‐ coenzyme A acetyltransferase ‐ 1 (ACAT ‐ 1) inhibition improves pulmonary inflammation in an in vivo murine model of ALI. We hypothesize that ACAT ‐ 1 inhibition has anti ‐ inflammatory effects beyond its intended use to reduce cholesterol esterification. The purpose of this study is to establish an in vitro bone marrow ‐ derived macrophage (BMDM) model to investigate the effect of ACAT ‐ 1 inhibition in macrophage activation by inducing an inflammatory response through lipopolysaccharide (LPS), and selectively inhibiting ACAT ‐ 1 with K ‐ 604. This model will provide insight on target cell metabolism, reduce interference from whole ‐ body effects, and minimize animal use. Monocytes were harvested from the bone marrow of 6 ‐ 8 week old wild ‐ type mice C57BL/6J (Jackson Laboratory) and stimulated with M ‐ CSF on d0, 3, and 7 to induce macrophage differentiation. To examine if ACAT ‐ 1 inhibition limits macrophage activation, K ‐ 604 was co ‐ administered with M ‐ CSF. Then, the cells were treated with LPS on d7 and harvested after 24h. Nitrite, NOS2 expression, and iNOS protein were determined through nitrite colorimetric measurement, RT ‐ qPCR, and western blot, respectively. Nitrite was measured as a proxy for nitric oxide (NO) production and was observed to decrease in LPS ‐ stimulated cells chronically treated with K ‐ 604. NOS2 was also reduced in LPS and K ‐ 604 conjunctive treatment. Compared to LPS, iNOS was reduced with chronic K ‐ 604 as measured by iNOS protein. LPS ‐ induced macrophage activation was suppressed and NO production was hindered due to lack of the iNOS protein. This aligns with the in vivo model, where K ‐ 604","PeriodicalId":406842,"journal":{"name":"ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"115502415","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
Structure-activity relationship of G protein-coupled receptor kinase 5 (GRK5) and its mutants G蛋白偶联受体激酶5 (GRK5)及其突变体的构效关系
ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology Pub Date : 2023-05-18 DOI: 10.1124/jpet.122.147510
Priyanka Naik, Qiuyan Chen, John J. G. Tesmer
{"title":"Structure-activity relationship of G protein-coupled receptor kinase 5 (GRK5) and its mutants","authors":"Priyanka Naik, Qiuyan Chen, John J. G. Tesmer","doi":"10.1124/jpet.122.147510","DOIUrl":"https://doi.org/10.1124/jpet.122.147510","url":null,"abstract":"","PeriodicalId":406842,"journal":{"name":"ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology","volume":"40 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114526847","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
HIV-1 gp120- and Morphine-Induced Endolysosome Iron Release Triggers Disruption of the Reactive Species Interactome and Cell Death HIV-1 gp120-和吗啡诱导的内溶酶体铁释放触发反应性物种相互作用组的破坏和细胞死亡
ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology Pub Date : 2023-05-18 DOI: 10.1124/jpet.122.251230
Nirmal Kumar, P. Halcrow, D. Quansah, Braelyn Liang, J. Geiger
{"title":"HIV-1 gp120- and Morphine-Induced Endolysosome Iron Release Triggers Disruption of the Reactive Species Interactome and Cell Death","authors":"Nirmal Kumar, P. Halcrow, D. Quansah, Braelyn Liang, J. Geiger","doi":"10.1124/jpet.122.251230","DOIUrl":"https://doi.org/10.1124/jpet.122.251230","url":null,"abstract":"","PeriodicalId":406842,"journal":{"name":"ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology","volume":"27 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"121905552","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
Calcium-dependent regulation of G protein-coupled receptor kinases G蛋白偶联受体激酶的钙依赖性调控
ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology Pub Date : 2023-05-18 DOI: 10.1124/jpet.122.242570
K. Komolov, D. Laurinavichyute, A. Bhardwaj, J. Benovic
{"title":"Calcium-dependent regulation of G protein-coupled receptor kinases","authors":"K. Komolov, D. Laurinavichyute, A. Bhardwaj, J. Benovic","doi":"10.1124/jpet.122.242570","DOIUrl":"https://doi.org/10.1124/jpet.122.242570","url":null,"abstract":"","PeriodicalId":406842,"journal":{"name":"ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology","volume":"453 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"123288144","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
Revisiting Pirin: Evidence for a Role in Translation but not in Transcriptional Control 再访皮林:在翻译中扮演角色的证据，而不是在转录控制中
ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology Pub Date : 2023-05-18 DOI: 10.1124/jpet.122.551800
Anna Denaly Cab Gomez, R. Neubig, E. Lisabeth
{"title":"Revisiting Pirin: Evidence for a Role in Translation but not in Transcriptional Control","authors":"Anna Denaly Cab Gomez, R. Neubig, E. Lisabeth","doi":"10.1124/jpet.122.551800","DOIUrl":"https://doi.org/10.1124/jpet.122.551800","url":null,"abstract":"","PeriodicalId":406842,"journal":{"name":"ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology","volume":"23 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128333838","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
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