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}
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
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{"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}
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}
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}
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
{"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}
{"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}
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}
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}
{"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}
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