EXCLI Journal最新文献_第10页

Structural and molecular characterization of lopinavir and ivermectin as breast cancer resistance protein (BCRP/ABCG2) inhibitors. 作为乳腺癌抗性蛋白（BCRP/ABCG2）抑制剂的洛匹那韦和依维菌素的结构和分子特征。

IF 4.6 3区生物学

EXCLI Journal Pub Date : 2023-11-14 eCollection Date: 2023-01-01 DOI: 10.17179/excli2023-6427

Julia de Paula Dutra, Gustavo Scheiffer, Thales Kronenberger, Lucas Julian Cruz Gomes, Isadora Zanzarini, Kelly Karoline Dos Santos, Arun K Tonduru, Antti Poso, Fabiane Gomes de Moraes Rego, Geraldo Picheth, Glaucio Valdameri, Vivian Rotuno Moure

{"title":"Structural and molecular characterization of lopinavir and ivermectin as breast cancer resistance protein (BCRP/ABCG2) inhibitors.","authors":"Julia de Paula Dutra, Gustavo Scheiffer, Thales Kronenberger, Lucas Julian Cruz Gomes, Isadora Zanzarini, Kelly Karoline Dos Santos, Arun K Tonduru, Antti Poso, Fabiane Gomes de Moraes Rego, Geraldo Picheth, Glaucio Valdameri, Vivian Rotuno Moure","doi":"10.17179/excli2023-6427","DOIUrl":"10.17179/excli2023-6427","url":null,"abstract":"A current clinical challenge in cancer is multidrug resistance (MDR) mediated by ABC transporters. Breast cancer resistance protein (BCRP) or ABCG2 transporter is one of the most important ABC transporters implicated in MDR and the use of inhibitors is a promising approach to overcome the resistance in cancer. This study aimed to characterize the molecular mechanism of ABCG2 inhibitors identified by a repurposing drug strategy using antiviral, anti-inflammatory and antiparasitic agents. Lopinavir and ivermectin can be considered as pan-inhibitors of ABC transporters, since both compounds inhibited ABCG2, P-glycoprotein and MRP1. They inhibited ABCG2 activity showing IC50 values of 25.5 and 23.4 µM, respectively. These drugs were highly cytotoxic and not transported by ABCG2. Additionally, these drugs increased the 5D3 antibody binding and did not affect the mRNA and protein expression levels. Cell-based analysis of the type of inhibition suggested a non-competitive inhibition, which was further corroborated by in silico approaches of molecular docking and molecular dynamics simulations. These results showed an overlap of the lopinavir and ivermectin binding sites on ABCG2, mainly interacting with E446 residue. However, the substrate mitoxantrone occupies a different site, binding to the F436 region, closer to the L554/L555 plug. In conclusion, these results revealed the mechanistic basis of lopinavir and ivermectin interaction with ABCG2. See also the Graphical abstract(Fig. 1).","PeriodicalId":12247,"journal":{"name":"EXCLI Journal","volume":"22 ","pages":"1155-1172"},"PeriodicalIF":4.6,"publicationDate":"2023-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10776880/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139416736","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Proteomic analysis of hepatic effects of okadaic acid in HepaRG human liver cells. 在 HepaRG 人肝细胞中分析 okadaic 酸对肝脏影响的蛋白质组学。

IF 4.6 3区生物学

EXCLI Journal Pub Date : 2023-10-31 eCollection Date: 2023-01-01 DOI: 10.17179/excli2023-6458

Leonie T D Wuerger, Greta Birkholz, Axel Oberemm, Holger Sieg, Albert Braeuning

引用次数: 0

First case of Lucio's phenomenon in a lepromatous leprosy patient following COVID-19 viral vector vaccine. 首例接种 COVID-19 病毒载体疫苗的麻风病人出现卢西奥现象。

IF 4.6 3区生物学

EXCLI Journal Pub Date : 2023-10-30 eCollection Date: 2023-01-01 DOI: 10.17179/excli2023-6661

Roberto Fernandes Soares-Neto, Geyse Maria Lima da Piedade, Priscila Soares Pereira, Rebeca Yasmin Ribeiro Vieira, Jerocilio Maciel de Oliveira-Júnior, Thalyta Porto Fraga, Martha Débora Lira Tenório, Pedro Dantas Oliveira, Paulo Ricardo Martins-Filho

引用次数: 0

Virtual ergonomics of PPE systems - a standardization perspective. 个人防护设备系统的虚拟人体工程学--标准化视角。

IF 4.6 3区生物学

EXCLI Journal Pub Date : 2023-10-27 eCollection Date: 2023-01-01 DOI: 10.17179/excli2023-6727

Peter Bröde, Edith Classen, Jean Léonard, Ronald Heus, Kalev Kuklane

引用次数: 0

Is polio making a comeback? The cost of vaccine hesitancy and the disparity in vaccine coverage. 小儿麻痹症是否卷土重来？疫苗犹豫不决的代价和疫苗覆盖率的差异。

IF 4.6 3区生物学

EXCLI Journal Pub Date : 2023-10-26 eCollection Date: 2023-01-01 DOI: 10.17179/excli2023-6594

Thalles Guilarducci Costa, Rizia Rocha Silva, João Victor Rosa de Freitas, Rodrigo Luiz Vancini, Marilia Santos Andrade, Claudio Andre Barbosa de Lira

引用次数: 0

Anti-inflammatory and anti-fibrotic effects of berberine-loaded liquid crystalline nanoparticles. 负载小檗碱的液晶纳米粒子的抗炎和抗纤维化作用

IF 4.6 3区生物学

EXCLI Journal Pub Date : 2023-10-26 eCollection Date: 2023-01-01 DOI: 10.17179/excli2023-6467

Amlan Chakraborty, Keshav Raj Paudel, Chao Wang, Gabriele De Rubis, Dinesh Kumar Chellappan, Philip Michael Hansbro, Chrishan S Samuel, Kamal Dua

引用次数: 0

How different viruses perturb host cellular machinery via short linear motifs. 不同病毒如何通过短线性图案扰乱宿主细胞机制

IF 4.6 3区生物学

EXCLI Journal Pub Date : 2023-10-26 eCollection Date: 2023-01-01 DOI: 10.17179/excli2023-6328

Sobia Idrees, Keshav Raj Paudel, Tayyaba Sadaf, Philip M Hansbro

引用次数: 0

Potential and challenges of high-speed (4D) body scanning for mobility analysis of firefighter clothing: a methodical case study. 高速 (4D) 人体扫描用于消防员服装流动性分析的潜力和挑战：方法案例研究。

IF 4.6 3区生物学

EXCLI Journal Pub Date : 2023-10-19 eCollection Date: 2023-01-01 DOI: 10.17179/excli2023-6101

Dominik Muenks, Yordan Kyosev, Felix Kunzelmann

{"title":"Potential and challenges of high-speed (4D) body scanning for mobility analysis of firefighter clothing: a methodical case study.","authors":"Dominik Muenks, Yordan Kyosev, Felix Kunzelmann","doi":"10.17179/excli2023-6101","DOIUrl":"10.17179/excli2023-6101","url":null,"abstract":"In this study, protective clothing for firefighters is analyzed using 4D body scanning and 3D hand scanning, with a focus on the experimental analysis of ergonomic comfort. In particular, German firefighting clothing is examined to discuss the possibilities and limitations of current scanning technologies for capturing firefighting clothing. For this purpose, various movements are recorded in the 4D scanner. In addition, a method for determining position changes of protective clothing at identified limits is presented. The initial results illustrated that the analysis of protective clothing for firefighters using 4D scanning is problematic due to specific materials, reflections, and surface properties. Improvements in the scanning process and optimization of algorithms are required to achieve more detailed and precise results. Concerning the ergonomic comfort related to the mobility under firefighting clothing use conditions, this methodical case study highlights the limits of current approaches, with a focus on the limitations of 4D scanning and potential improvements.","PeriodicalId":12247,"journal":{"name":"EXCLI Journal","volume":"22 ","pages":"1092-1103"},"PeriodicalIF":4.6,"publicationDate":"2023-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10694343/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138487052","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Exploring mito-nuclear genetic factors in Leber's hereditary optic neuropathy: insights from comprehensive profiling of unique cases. 探索 Leber 遗传性视神经病变的有丝分裂核遗传因素：对独特病例进行全面分析的启示。

IF 4.6 3区生物学

EXCLI Journal Pub Date : 2023-10-09 eCollection Date: 2023-01-01 DOI: 10.17179/excli2023-6297

Prakash Chermakani, Poigaialwar Gowri, Shanmugam Mahesh Kumar, Periasamy Sundaresan

{"title":"Exploring mito-nuclear genetic factors in Leber's hereditary optic neuropathy: insights from comprehensive profiling of unique cases.","authors":"Prakash Chermakani, Poigaialwar Gowri, Shanmugam Mahesh Kumar, Periasamy Sundaresan","doi":"10.17179/excli2023-6297","DOIUrl":"10.17179/excli2023-6297","url":null,"abstract":"Leber's hereditary optic neuropathy (LHON) is a mitochondrial complex I disorder and causes inexorable painless vision loss. Recent studies from India reported that a significant proportion of LHON patients lack primary mitochondrial DNA mutations, suggesting that alternative genetic factors contribute to disease development. Therefore, this study investigated the genetic profile of LHON-affected individuals in order to understand the role of mito-nuclear genetic factors in LHON. A total of thirty probands displaying symptoms consistent with LHON have undergone whole mitochondrial and whole exome sequencing. Interestingly, whole mtDNA sequencing revealed primary mtDNA mutations in 30 % of the probands (n=9), secondary mtDNA mutations in 40 % of the probands (n=12) and no mitochondrial changes in 30 % of individuals (n=9). Further, WES analysis determined pathogenic mutations in 11 different nuclear genes, especially in cases with secondary mtDNA mutations (n=6) or no mtDNA mutations (n=6). These findings provide valuable insight into LHON genetic predisposition, particularly in cases lacking primary mtDNA mutations. See also Figure 1(Fig. 1).","PeriodicalId":12247,"journal":{"name":"EXCLI Journal","volume":"22 ","pages":"1077-1091"},"PeriodicalIF":4.6,"publicationDate":"2023-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10694345/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138487050","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A facile method to generate cerebral organoids from human pluripotent stem cells. 一种从人类多能干细胞产生大脑类器官的简单方法。

IF 4.6 3区生物学

EXCLI Journal Pub Date : 2023-10-05 eCollection Date: 2023-01-01 DOI: 10.17179/excli2023-6299

Susan Simorgh, Seyed Ahmad Mousavi, San Kit To, Vincent Pasque, Keimpe Wierda, Tim Vervliet, Meghdad Yeganeh, Paria Pooyan, Yoke Chin Chai, Catherine Verfaillie, Hossein Baharvand

{"title":"A facile method to generate cerebral organoids from human pluripotent stem cells.","authors":"Susan Simorgh, Seyed Ahmad Mousavi, San Kit To, Vincent Pasque, Keimpe Wierda, Tim Vervliet, Meghdad Yeganeh, Paria Pooyan, Yoke Chin Chai, Catherine Verfaillie, Hossein Baharvand","doi":"10.17179/excli2023-6299","DOIUrl":"https://doi.org/10.17179/excli2023-6299","url":null,"abstract":"Human cerebral organoids (COs) are self-organizing three-dimensional (3D) neural structures that provide a human-specific platform to study the cellular and molecular processes that underlie different neurological events. The first step of CO generation from human pluripotent stem cells (hPSCs) is neural induction, which is an in vitro simulation of neural ectoderm development. Several signaling pathways cooperate during neural ectoderm development and in vitro differentiation of hPSCs toward neural cell lineages is also affected by them. In this study, we considered some of the known sources of these variable signaling cues arising from cell culture media components and sought to modulate their effects by applying a comprehensive combination of small molecules and growth factors for CO generation. Histological analysis demonstrated that these COs recapitulate the neural progenitor zone and early cortical layer organization, containing different types of neuronal and glial cells which was in accordance with single-nucleus transcriptome profiling results. Moreover, patch clamp and intracellular Ca2+ dynamic studies demonstrated that the COs behave as a functional neural network. Thus, this method serves as a facile protocol for generating hPSC-derived COs that faithfully mimic the features of their in vivo counterparts in the developing human brain. See also Figure 1(Fig. 1).","PeriodicalId":12247,"journal":{"name":"EXCLI Journal","volume":"22 ","pages":"1055-1076"},"PeriodicalIF":4.6,"publicationDate":"2023-10-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10620858/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71479929","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0