journal
https://read.qxmd.com/read/38461904/the-role-of-g-protein-coupled-receptor-kinases-in-glp-1r-%C3%AE-arrestin-recruitment-and-internalisation
#41
JOURNAL ARTICLE
Samantha M McNeill, Jessica Lu, Carlo Marion C Carino, Asuka Inoue, Peishen Zhao, Patrick M Sexton, Denise Wootten
The glucagon-like peptide 1 receptor (GLP-1R) is a validated clinical target for the treatment of type 2 diabetes and obesity. Unlike most G protein-coupled receptors (GPCRs), the GLP-1R undergoes an atypical mode of internalisation that does not require β-arrestins. While differences in GLP-1R trafficking and β-arrestin recruitment have been observed between clinically used GLP-1R agonists, the role of G protein-coupled receptor kinases (GRKs) in affecting these pathways has not been comprehensively assessed...
March 8, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38461903/unraveling-the-immune-landscape-and-therapeutic-biomarker-pmepa1-for-oxaliplatin-resistance-in-colorectal-cancer-a-comprehensive-approach
#42
JOURNAL ARTICLE
Zhengguang Zhang, Tianming Lu, Zhe Zhang, Zixian Liu, Ruoning Qian, Ruogu Qi, Fuqiong Zhou, Min Li
Oxaliplatin (OXA) is a platinum-based chemotherapeutic agent with promising applications in the treatment of various malignancies, particularly colorectal cancer (CRC). However, the management of OXA resistance remains an ongoing obstacle in CRC therapy. This study aims to comprehensively investigate the immune landscape, targeted therapeutic biomarkers, and mechanisms that influence OXA resistance in CRC. Our results demonstrated that our OXA resistance-based CRC prognostic model not only provides risk assessment for patients but also reflects the immune landscape of patients...
March 8, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38460909/the-pathophysiology-of-visceral-adipose-tissues-in-cardiometabolic-diseases
#43
REVIEW
Mi-Jeong Lee, Jeehoon Kim
Central pattern of fat distribution, especially fat accumulation within the intraabdominal cavity increases risks for cardiometabolic diseases. Portal hypothesis combined with a pathological remodeling in visceral fat is considered the major etiological factor explaining the independent contribution of visceral obesity to cardiometabolic diseases. Excessive remodeling in visceral fat during development of obesity leads to dysfunctions in the depot, characterized by hypertrophy and death of adipocytes, hypoxia, inflammation, and fibrosis...
March 8, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38460910/potential-role-of-modulating-autophagy-levels-in-sensorineural-hearing-loss
#44
REVIEW
Ting Zou, Renwei Xie, Sihan Huang, Dingkun Lu, Jun Liu
In recent years, extensive research has been conducted on the pathogenesis of sensorineural hearing loss (SNHL). Apoptosis and necrosis have been identified to play important roles in hearing loss, but they cannot account for all hearing loss. Autophagy, a cellular process responsible for cell self-degradation and reutilization, has emerged as a significant factor contributing to hearing loss, particularly in cases of autophagy deficiency. Autophagy plays a crucial role in maintaining cell health by exerting cytoprotective and metabolically homeostatic effects in organisms...
March 7, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38460908/corynoxine-triggers-cell-death-via-activating-pp2a-and-regulating-akt-mtor-gsk3%C3%AE-axes-in-nsclc
#45
JOURNAL ARTICLE
Guoqing Hou, Weihua Hu, Yazhou Sang, Xiaocai Gan, Hui Xu, Qiongying Hu, Xuan Cao
This study investigates the anticancer activity and pharmacological mechanisms of Corynoxine (Cory) in non-small cell lung cancer (NSCLC). Cory, a natural product derived from the Chinese herbal medicine Uncaria rhynchophylla, demonstrates promising pharmacological activity. Cell proliferation and viability were evaluated via MTT and colony formation assays. Flow cytometry was employed to analyze cell apoptosis, cycle distribution, and mitochondrial membrane potential. Autophagy was detected using fluorescence microscopy and electron microscopy...
March 7, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38460907/daurisoline-suppress-glioma-progression-by-inhibiting-autophagy-through-pi3k-akt-mtor-pathway-and-increases-tmz-sensitivity
#46
JOURNAL ARTICLE
Hai-Tang Yin, Hui-Lu, Ji-Hong Yang, Qin Li, Ming Li, Qing-Qing Zhao, Zhi-Peng Wen
Glioma is one of the most common primary malignant tumors of the central nervous system. Temozolomide (TMZ) is the only effective chemotherapeutic agent, but it easily develops resistance and has unsatisfactory efficacy. Consequently, there is an urgent need to develop safe and effective compounds for glioma treatment. The cytotoxicity of 30 candidate compounds to glioma cells was detected by the CCK-8 assay. Daurisoline (DAS) was selected for further investigation due to its potent anti-glioma effects. Our study revealed that DAS induced glioma cell apoptosis through increasing caspase-3/6/9 activity...
March 7, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38458331/columbianadin-suppresses-glioblastoma-progression-by-inhibiting-the-pi3k-akt-signaling-pathway
#47
JOURNAL ARTICLE
Wei Zhang, Jianhong Dong, Jiayun Xu, Yiming Qian, Danni Chen, Ziwei Fan, Hao Yang, Jianglei Xiang, Xiumin Xue, Xuan Luo, Yuanyuan Jiang, Yongjie Wang, Zhihui Huang
Glioblastoma (GBM) is the most common malignant glioma among brain tumors with low survival rate and high recurrence rate. Columbianadin (CBN) has pharmacological properties such as anti-inflammatory, analgesic, thrombogenesis-inhibiting and anti-tumor effects. However, it remains unknown that the effect of CBN on GBM cells and its underlying molecular mechanisms. In the present study, we found that CBN inhibited the growth and proliferation of GBM cells in a dose-dependent manner. Subsequently, we found that CBN arrested the cell cycle in G0/G1 phase and induced the apoptosis of GBM cells...
March 6, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38458330/the-role-of-telomerase-reverse-transcriptase-in-the-mitochondrial-protective-functions-of-angiotensin-1-7-in-diabetic-cd34-cells
#48
JOURNAL ARTICLE
Jesmin Jahan, Shrinidh Joshi, Ildamaris Montes de Oca, Andrew Toelle, Christine Lopez-Yang, Carmen V Chacon, Andreas W Beyer, Charles A Garcia, Yagna Pr Jarajapu
Angiotensin (Ang)-(1-7) stimulates vasoprotective functions of diabetic (DB) CD34+ hematopoietic stem/progenitor cells partly by decreasing reactive oxygen species (ROS), increasing nitric oxide (NO) levels and decreasing TGFβ1 secretion. Telomerase reverse transcriptase (TERT) translocates to mitochondria and regulates ROS generation. Alternative splicing of TERT results in variants α-, β- and α-β-TERT, which may oppose functions of full-length (FL) TERT. This study tested if the protective functions of Ang-(1-7) or TGFβ1-silencing are mediated by mitoTERT and that diabetes decreases FL-TERT expression by inducing splicing...
March 6, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38458329/srt1720-inhibits-bladder-cancer-cell-progression-by-impairing-autophagic-flux
#49
JOURNAL ARTICLE
Lanlan Li, Shengjun Fu, Jianliang Wang, Jianzhong Lu, Yan Tao, Liangtao Zhao, Beitang Fu, Lanpeng Lu, Caifei Xiang, Xince Sun, Shanhui Liu, Degui Wang, Zhiping Wang
Bladder cancer (BC) is the most common cancer of the urinary tract, with poor survival, high recurrence rates, and lacking of targeted drugs. In this study, we constructed a library to screen compounds inhibiting bladder cancer cells growth. Among them, SRT1720 was identified to inhibit bladder cancer cell proliferation in vitro and in vivo. SRT1720 treatment also suppressed bladder cancer cells migration, invasion and induced apoptosis. Mechanism studies shown that SRT1720 promoted autophagosomes accumulation by inducing early-stage autophagy but disturbed the late-stage of autophagy by blocking fusion of autophagosomes and lysosomes...
March 6, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38442793/her2-targeted-therapy-in-colorectal-cancer-current-landscape-and-future-directions
#50
REVIEW
Na Chen, Ling He, Qiang Zou, Hongxin Deng
Colorectal cancer (CRC) is one of the most common causes of tumor-related deaths globally. Despite recent improvements in the comprehensive therapy of malignancy, metastatic CRC continues to have a poor prognosis. Human epidermal growth factor receptor 2 (HER2) is an established oncogenic driver, which is successfully targeted for breast and gastric cancers. Approximately 5% of CRC patients carry somatic HER2 mutations or gene amplification. In 2019, the U.S. Food and Drug Administration have approved trastuzumab and pertuzumab in combination with chemotherapy for the treatment of HER2-positive metastatic CRC...
March 3, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38442792/therapeutic-potential-of-lipin-inhibitors-for-the-treatment-of-cancer
#51
REVIEW
Elizabeth G Slane, Samantha J Tambrini, Brian S Cummings
Lipins are phosphatidic acid phosphatases (PAP) that catalyze the conversion of phosphatidic acid (PA) to diacylglycerol (DAG). Three lipin isoforms have been identified: lipin-1, -2 and -3. In addition to their PAP activity, lipin-1 and -2 act as transcriptional coactivators and corepressors. Lipins have been intensely studied for their role in regulation of lipid metabolism and adipogenesis; however, lipins are hypothesized to mediate several pathologies, such as those involving metabolic diseases, neuropathy and even cognitive impairment...
March 3, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38438053/adipose-tissue-derived-stem-cells-in-vivo-and-in-vitro-models-for-metabolic-diseases
#52
REVIEW
Jaime Navarro-Perez, Stefania Carobbio
The primary role of adipose tissue stem cells (ADSCs) is to support the function and homeostasis of adipose tissue in physiological and pathophysiological conditions. However, when ADSCs become dysfunctional in diseases such as obesity and cancer, they become impaired, undergo signalling changes, and their epigenome is altered, which can have a dramatic effect on human health. In more recent years, the therapeutic potential of ADSCs in regenerative medicine, wound healing, and for treating conditions such as cancer and metabolic diseases has been extensively investigated with very promising results...
March 2, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38438052/toll-like-receptor-signalling-as-a-cannabinoid-target
#53
REVIEW
Melody Cui Sun, Almudena Otálora-Alcaraz, Jack A Prenderville, Eric J Downer
Toll-like receptors (TLRs) have become a focus in biomedicine and biomedical research given the roles of this unique family of innate immune proteins in immune activation, infection, and autoimmunity. It is evident that TLR dysregulation, and subsequent alterations in TLR-mediated inflammatory signalling, can contribute to disease pathogenesis, and TLR targeted therapies are in development. This review highlights evidence that cannabinoids are key regulators of TLR signalling. Cannabinoids include component of the plant Cannabis sativa L...
March 2, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38438051/from-molecular-pathogenesis-to-therapy-unraveling-non-coding-rnas-dnmt3a-axis-in-human-cancers
#54
REVIEW
Chunjie Huang, Seyed Mohsen Aghaei-Zarch
Cancer is a comprehensive classification encompassing more than 100 forms of malignancies that manifest in diverse tissues within the human body. Recent studies have provided evidence that aberrant epigenetic modifications are pivotal indicators of cancer. Epigenetics encapsulates DNA methyltransferases as a crucial class of modifiers. DNMTs, including DNMT3A, assume central roles in DNA methylation processes that orchestrate normal biological functions, such as gene transcription, predominantly in mammals...
March 2, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38432053/corrigendum-to-therapeutic-potential-of-dinitrobenzene-sulfonic-acid-dnbs-induced-colitis-in-mice-by-targeting-il-1%C3%AE-and-il-18-biochem-pharmacol-155-2018-150-161
#55
Daniela Impellizzeri, Rosalba Siracusa, Marika Cordaro, Alessio Filippo Peritore, Enrico Gugliandolo, Giuseppe Mancuso, Angelina Midiri, Rosanna Di Paola, Salvatore Cuzzocrea
No abstract text is available yet for this article.
March 2, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38430671/corrigendum-to-reversal-of-the-deleterious-effects-of-chronic-dietary-hfcs-55-intake-by-ppar-%C3%AE-agonism-correlates-with-impaired-nlrp3-inflammasome-activation-biochem-pharmacol-85-2-2013-257-264
#56
Massimo Collino, Elisa Benetti, Mara Rogazzo, Raffaella Mastrocola, Muhammed M Yaqoob, Manuela Aragno, Christroph Theimermann, Roberto Fantozzi
No abstract text is available yet for this article.
March 1, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38431231/lactic-acid-in-macrophage-polarization-a-factor-in-carcinogenesis-and-a-promising-target-for-cancer-therapy
#57
REVIEW
Mobarakeh Ajam-Hosseini, Romina Heydari, Milad Rasouli, Fatemeh Akhoondi, Niloofar Asadi Hanjani, Sander Bekeschus, Mohammad Doroudian
Cancer remains a formidable challenge, continually revealing its intricate nature and demanding novel treatment approaches. Within this intricate landscape, the tumor microenvironment and its dynamic components have gained prominence, particularly macrophages that can adopt diverse polarization states, exerting a profound influence on cancer progression. Recent revelations have spotlighted lactic acid as a pivotal player in this complex interplay. This review systematically explores lactic acid's multifaceted role in macrophage polarization, focusing on its implications in carcinogenesis...
February 29, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38428824/expression-and-function-of-vista-on-myeloid-cells
#58
REVIEW
Siyu Li, Geng Wang, Yan Ren, Xinyue Liu, Yixuan Wang, Jianing Li, Hua Liu, Jiaqiang Yang, Jingjun Xing, Yanru Zhang, Canxia He, Suling Xu, Xin Hou, Na Li
V-domain containing Ig Suppressor of T cell Activation (VISTA) is predominantly expressed on myeloid cells and functions as a ligand/receptor/soluble molecule. In inflammatory responses and immune responses, VISTA regulates multiple functions of myeloid cells, such as chemotaxis, phagocytosis, T cell activation. Since inflammation and immune responses are critical in many diseases, VISTA is a promising therapeutic target. In this review, we will describe the expression and function of VISTA on different myeloid cells, including neutrophils, monocytes, macrophages, dendritic cells (DCs), myeloid-derived suppressor cells (MDSCs)...
February 29, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38428828/sting-deficiency-alleviates-ferroptosis-through-fpn1-stabilization-in-diabetic-kidney-disease
#59
JOURNAL ARTICLE
Qin-Xiao Zhao, Sen-Bo Yan, Fen Wang, Xiao-Xing Li, Guo-Kai Shang, Zi-Jie Zheng, Jie Xiao, Zong-Wei Lin, Chuan-Bao Li, Xiao-Ping Ji
Ferroptosis, a form of cell death driven by iron-dependent lipid peroxidation, has known as one of the most significant pathological processes involved in diabetic kidney disease (DKD). Stimulator of interferon genes (STING) has been demonstrated its potential in regulating ferroptosis, but the regulatory role in DKD mice and underlying mechanisms haven't been illustrated. To elucidate whether and how STING regulates ferroptosis in DKD, we detected the influence of STING on diabetic-related ferroptosis in a diabetic model and in erastin-induced renal tubular epithelial cells (RTECs)...
February 28, 2024: Biochemical Pharmacology
https://read.qxmd.com/read/38428827/proliferation-and-migration-of-pc-3-prostate-cancer-cells-is-counteracted-by-ppar%C3%AE-cladosporol-binding-mediated-apoptosis-and-a-decreased-lipid-biosynthesis-and-accumulation
#60
JOURNAL ARTICLE
Roberta Rapuano, Alessio Riccio, Antonella Mercuri, Jessica Raffaella Madera, Sabrina Dallavalle, Salvatore Moricca, Angelo Lupo
OBJECTIVES: Chemoprevention, consisting of the administration of natural and/or synthetic compounds, appears to be an alternative way to common therapeutical approaches to preventing the occurrence of various cancers. Cladosporols, secondary metabolites from Cladosporium tenuissimum, showed a powerful ability in controlling human colon cancer cell proliferation through a peroxisome proliferator-activated receptor gamma (PPARγ)-mediated modulation of gene expression. Hence, we carried out experiments to verify the anticancer properties of cladosporols in human prostate cancer cells...
February 28, 2024: Biochemical Pharmacology
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