Generation and characterization of cytochrome P450 3A74 CRISPR/Cas9 knockout bovine foetal hepatocyte cell line (BFH12)
Biochem Pharmacol. 2024 Apr 20:116231. doi: 10.1016/j.bcp.2024.116231. Online ahead of print.ABSTRACTIn human, the cytochrome P450 3A (CYP3A) subfamily of drug-metabolizing enzymes (DMEs) is responsible for a significant number of phase I reactions, with the CYP3A4 isoform superintending the hepatic and intestinal metabolism of diverse endobiotic and xenobiotic compounds. The CYP3A4-dependent bioactivation of chemicals may result in hepatotoxicity and trigger carcinogenesis. In cattle, four CYP3A genes (CYP3A74, CYP3A76, CYP3A28 and CYP3A24) have been identified. Despite cattle being daily exposed to xenobiotics (e.g., myc...
Source: Biochemical Pharmacology - April 22, 2024 Category: Drugs & Pharmacology Authors: Silvia Iori Caterina D'Onofrio Nihay Laham-Karam Isidore Mushimiyimana Lorena Lucatello Ludovica Montanucci Rosa Maria Lopparelli Federico Bonsembiante Francesca Capolongo Marianna Pauletto Mauro Dacasto Mery Giantin Source Type: research
Challenging and target-based shifting strategies for heart failure treatment: An update from the last decades
Biochem Pharmacol. 2024 Apr 20:116232. doi: 10.1016/j.bcp.2024.116232. Online ahead of print.ABSTRACTHeart failure (HF) is a major global health problem afflicting millions worldwide. Despite the significant advances in therapies and prevention, HF still carries very high morbidity and mortality, requiring enormous healthcare-related expenditure, and the search for new weapons goes on. Following initial treatment strategies targeting inotropism and congestion, attention has focused on offsetting the neurohormonal overactivation and three main therapies, including angiotensin-converting enzyme inhibitors or angiotensin II t...
Source: Biochemical Pharmacology - April 22, 2024 Category: Drugs & Pharmacology Authors: Yuichi Hattori Kohshi Hattori Kuniaki Ishii Masanobu Kobayashi Source Type: research
Cancer on motors: How kinesins drive prostate cancer progression?
Biochem Pharmacol. 2024 Apr 19:116229. doi: 10.1016/j.bcp.2024.116229. Online ahead of print.ABSTRACTProstate cancer causes numerous male deaths annually. Although great progress has been made in the diagnosis and treatment of prostate cancer during the past several decades, much about this disease remains unknown, especially its pathobiology. The kinesin superfamily is a pivotal group of motor proteins, that contains a microtubule-based motor domain and features an adenosine triphosphatase activity and motility characteristics. Large-scale sequencing analyses based on clinical samples and animal models have shown that sev...
Source: Biochemical Pharmacology - April 21, 2024 Category: Drugs & Pharmacology Authors: Jia-Ming Wang Feng-Hao Zhang Zi-Xiang Liu Yi-Jie Tang Jiang-Feng Li Li-Ping Xie Source Type: research
6-O-angeloylplenolin inhibits osteoclastogenesis in vitro via suppressing c-Src/NF- κB/NFATc1 pathways and ameliorates bone resorption in collagen-induced arthritis mouse model
In conclusion, 6-OAP has the potential to be further developed for the treatment of RA-related bone erosion.PMID:38643905 | DOI:10.1016/j.bcp.2024.116230 (Source: Biochemical Pharmacology)
Source: Biochemical Pharmacology - April 21, 2024 Category: Drugs & Pharmacology Authors: Zhi-Chao Li Min Li Ling-Xiang Xiao Xi Zheng Rong Li Shi-Jia Dong Yue Wang Hong-Yu Wen Kun-Lin Ruan Ke-Guang Cheng Ming Chen Yan-Hui Tan Source Type: research
Comprehensive review for non-coding RNAs: From mechanisms to therapeutic applications
Biochem Pharmacol. 2024 Apr 19:116218. doi: 10.1016/j.bcp.2024.116218. Online ahead of print.ABSTRACTNon-coding RNAs (ncRNAs) are an assorted collection of transcripts that are not translated into proteins. Since their discovery, ncRNAs have gained prominence as crucial regulators of various biological functions across diverse cell types and tissues, and their abnormal functioning has been implicated in disease. Notably, extensive research has focused on the relationship between microRNAs (miRNAs) and human cancers, although other types of ncRNAs, such as long non-coding RNAs (lncRNAs) and circular RNAs (circRNAs), are als...
Source: Biochemical Pharmacology - April 21, 2024 Category: Drugs & Pharmacology Authors: YanJun Zhang Lijuan Zhan Xue Jiang Xiaozhu Tang Source Type: research
Marein, a novel natural product for restoring chemo-sensitivity to cancer cells through competitive inhibition of ABCG2 function
This study reveals a novel role and mechanism of marein in modulating drug resistance, and may have important implications in treatment of cancers that are resistant to chemotherapeutic drugs that belong to the substrates of ABCG2 transporters.PMID:38643907 | DOI:10.1016/j.bcp.2024.116219 (Source: Biochemical Pharmacology)
Source: Biochemical Pharmacology - April 21, 2024 Category: Drugs & Pharmacology Authors: Yixuan Li Fanfan Guo Wenjing Wang FangLin Lv Lu Zhang Mingxian Zhu Shumin Yang Shunli Dong Mingxuan Zhou Zhenyun Li Zengyan Zhu Jin-Ming Yang Yi Zhang Source Type: research
Increased uterine arterial tone, stiffness and remodeling with augmented matrix metalloproteinase-1 and -7 in uteroplacental ischemia-induced hypertensive pregnancy
Biochem Pharmacol. 2024 Apr 19:116227. doi: 10.1016/j.bcp.2024.116227. Online ahead of print.ABSTRACTPreeclampsia is a pregnancy-related disorder manifested as hypertensive pregnancy (HTN-Preg) and often fetal growth restriction (FGR), but the mechanisms involved are unclear. We have reported enhanced reactivity of systemic vessels in HTN-Preg rats, but the critical changes in the uterine circulation are less clear. We tested whether HTN-Preg involves localized aberrations in uterine arterial tone, stiffness and remodeling by matrix metalloproteinases (MMPs). Blood pressure (BP) and litter size were recorded in normal preg...
Source: Biochemical Pharmacology - April 21, 2024 Category: Drugs & Pharmacology Authors: Chen Lin Marc Q Mazzuca Raouf A Khalil Source Type: research
Comparison of the function of two novel human dopamine D2 receptor variants identifies a likely mechanism for their pathogenicity
Biochem Pharmacol. 2024 Apr 19:116228. doi: 10.1016/j.bcp.2024.116228. Online ahead of print.ABSTRACTTwo recently discovered DRD2 mutations, c.634A > T, p.Ile212Phe and c.1121 T > G, p.Met374Arg, cause hyperkinetic movement disorders that have overlapping features but apparently differ in severity. The two known carriers of the Met374Arg variant had early childhood disease onset and more severe motor, cognitive, and neuropsychiatric deficits than any known carriers of the Ile212Phe variant, whose symptoms were first apparent in adolescence. Here, we evaluated if differences in the function of the two variants in cult...
Source: Biochemical Pharmacology - April 21, 2024 Category: Drugs & Pharmacology Authors: Dayana Rodriguez-Contreras Javier Garc ía-Nafría Amy E Chan Ujwal Shinde Kim A Neve Source Type: research
Identification of a new class of activators of the Hippo pathway with antitumor activity in vitro and in vivo
Biochem Pharmacol. 2024 Apr 17:116217. doi: 10.1016/j.bcp.2024.116217. Online ahead of print.ABSTRACTThe Hippo pathway is a key regulator of tissue growth, organ size, and tumorigenesis. Activating the Hippo pathway by gene editing or pharmaceutical intervention has been proven to be a new therapeutic strategy for treatment of the Hippo pathway-dependent cancers. To now, a number of compounds that directly target the downstream effector proteins of Hippo pathway, including YAP and TEADs, have been disclosed, but very few Hippo pathway activators are reported. Here, we discovered a new class of Hippo pathway activator, YL-6...
Source: Biochemical Pharmacology - April 19, 2024 Category: Drugs & Pharmacology Authors: Guifeng Lin Anjie Xia Jingxin Qiao Hailin Zhang Pei Chen Pei Zhou Qian Hu Zhiyu Xiang Shiyu Zhang Linli Li Shengyong Yang Source Type: research
Doxorubicin-based ENO1 targeted drug delivery strategy enhances therapeutic efficacy against colorectal cancer
Biochem Pharmacol. 2024 Apr 17;224:116220. doi: 10.1016/j.bcp.2024.116220. Online ahead of print.ABSTRACTAlpha-enolase (ENO1), a multifunctional protein with carcinogenic properties, has emerged as a promising cancer biomarker because of its differential expression in cancer and normal cells. On the basis of this characteristic, we designed a cell-targeting peptide that specifically targets ENO1 and connected it with the drug doxorubicin (DOX) by aldehyde-amine condensation. A surface plasmon resonance (SPR) assay showed that the affinity for ENO1 was stronger (KD = 2.5 µM) for the resulting cell-targeting drug, DOX-P, th...
Source: Biochemical Pharmacology - April 19, 2024 Category: Drugs & Pharmacology Authors: Jun Liu Xiaoyu Hu Guanghao Yu Qingrong Wang Liwei Gu Jianying Shen Qinghe Zhao Hao Sun Shi Wang Zhongyuan Guo Yu Zhao Hai Ma Source Type: research
Celecoxib and sulindac sulfide elicit anticancer effects on PIK3CA-mutated head and neck cancer cells through endoplasmic reticulum stress, reactive oxygen species, and mitochondrial dysfunction
Biochem Pharmacol. 2024 Apr 18;224:116221. doi: 10.1016/j.bcp.2024.116221. Online ahead of print.ABSTRACTGain-of-function mutation in the phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha gene (PIK3CA) is a significant factor in head and neck cancer (HNC). Patients with HNC harboring PIK3CA mutations receive therapeutic benefits from the use of non-steroidal anti-inflammatory drugs (NSAIDs). However, the molecular mechanisms underlying these effects remain unknown. Here, we examined the Detroit562 and FaDu cell lines as HNC models with and without a hyperactive PIK3CA mutation (H1047R), respecti...
Source: Biochemical Pharmacology - April 19, 2024 Category: Drugs & Pharmacology Authors: Nga Thi Thanh Nguyen Sang Yoon Lee Source Type: research
HOXB9 promotes osteosarcoma cell survival and malignancy under glucose starvation via upregulating SPP1 expression
In this study, we found that HOXB9 was increased upon glucose starvation. Elevated HOXB9 suppressed osteosarcoma cell death and supported cell growth and migration under glucose starvation. Further mechanistic studies demonstrated that HOXB9 directly bound to the promoter of secreted phosphoprotein 1 (SPP1) and transcriptionally upregulated SPP1 expression which then led cell death decrease and cell growth increase under glucose deprivation environment. Clinically, HOXB9 was significantly upregulated in osteosarcoma compared with normal tissues and increase of HOXB9 expression was positively associated with the elevation o...
Source: Biochemical Pharmacology - April 15, 2024 Category: Drugs & Pharmacology Authors: Jian Han Renchen Ji Shuo Zheng Xin Xia Wenxiao Du Hongtao He Chuanchun Han Wenzhi Zhao Xiaojie Li Yuan Wang Lu Zhang Source Type: research
A model of alcoholic liver disease based on different hepatotoxics leading to liver cancer
In conclusion, we provide a useful model for exploring the chronological ALD-associated alterations and stages, and addressing therapeutic approaches.PMID:38621424 | DOI:10.1016/j.bcp.2024.116209 (Source: Biochemical Pharmacology)
Source: Biochemical Pharmacology - April 15, 2024 Category: Drugs & Pharmacology Authors: Brisa Rodope Alarc ón-Sánchez Osiris Germ án Idelfonso-García Dafne Guerrero-Escalera Carolina Pi ña-Vázquez Guillermo de Anda-J áuregui Jos é Luis Pérez-Hernández Mireya de la Garza Francisco Garc ía-Sierra Yesennia S ánchez-Pérez Rafael Bal Source Type: research
Tanshinone IIA acts as a regulator of lipogenesis to overcome osimertinib acquired resistance in lung cancer
Biochem Pharmacol. 2024 Apr 13:116207. doi: 10.1016/j.bcp.2024.116207. Online ahead of print.ABSTRACTOsimertinib is a novel epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI), acting as the first-line medicine for advanced EGFR-mutated NSCLC. Recently, the acquired resistance to osimertinib brings great challenges to the advanced treatment. Therefore, it is in urgent need to find effective strategy to overcome osimertinib acquired resistance. Here, we demonstrated that SREBP pathway-driven lipogenesis was a key mediator to promote osimertinib acquired resistance, and firstly found Tanshinone IIA (Tan IIA...
Source: Biochemical Pharmacology - April 15, 2024 Category: Drugs & Pharmacology Authors: Lin Cao Zhiyan Qin Ting Yu Xupeng Bai Shiqin Jiang Daifei Wang Fangqing Ning Min Huang Jing Jin Source Type: research
HOXB9 promotes osteosarcoma cell survival and malignancy under glucose starvation via upregulating SPP1 expression
In this study, we found that HOXB9 was increased upon glucose starvation. Elevated HOXB9 suppressed osteosarcoma cell death and supported cell growth and migration under glucose starvation. Further mechanistic studies demonstrated that HOXB9 directly bound to the promoter of secreted phosphoprotein 1 (SPP1) and transcriptionally upregulated SPP1 expression which then led cell death decrease and cell growth increase under glucose deprivation environment. Clinically, HOXB9 was significantly upregulated in osteosarcoma compared with normal tissues and increase of HOXB9 expression was positively associated with the elevation o...
Source: Biochemical Pharmacology - April 15, 2024 Category: Drugs & Pharmacology Authors: Jian Han Renchen Ji Shuo Zheng Xin Xia Wenxiao Du Hongtao He Chuanchun Han Wenzhi Zhao Xiaojie Li Yuan Wang Lu Zhang Source Type: research
