keyword
https://read.qxmd.com/read/38536483/cacna2d1-regulates-the-progression-and-influences-the-microenvironment-of-colon-cancer
#1
JOURNAL ARTICLE
Hiroyuki Inoue, Atsushi Shiozaki, Toshiyuki Kosuga, Hiroki Shimizu, Michihiro Kudou, Tomohiro Arita, Hirotaka Konishi, Shuhei Komatsu, Yoshiaki Kuriu, Takeshi Kubota, Hitoshi Fujiwara, Yukiko Morinaga, Eiichi Konishi, Eigo Otsuji
BACKGROUND: Calcium voltage-gated channel auxiliary subunit alpha 2/delta 1 (CACNA2D1), a gene encoding a voltage-gated calcium channel, has been reported as an oncogene in several cancers. However, its role in colon cancer (CC) remains unclear. This study aimed to investigate the function of CACNA2D1 and its effect on the microenvironment in CC. METHODS: Immunohistochemistry (IHC) analysis was performed on samples collected from 200 patients with CC who underwent curative colectomy...
March 27, 2024: Journal of Gastroenterology
https://read.qxmd.com/read/38528462/single-cell-transcriptional-signature-based-drug-repurposing-and-in-vitro-evaluation-in-colorectal-cancer
#2
JOURNAL ARTICLE
Roohallah Mahdi-Esferizi, Zahra Shiasi, Razieh Heidari, Ali Najafi, Issa Mahmoudi, Fatemeh Elahian, Shahram Tahmasebian
BACKGROUND: The need for intelligent and effective treatment of diseases and the increase in drug design costs have raised drug repurposing as one of the effective strategies in biomedicine. There are various computational methods for drug repurposing, one of which is using transcription signatures, especially single-cell RNA sequencing (scRNA-seq) data, which show us a clear and comprehensive view of the inside of the cell to compare the state of disease and health. METHODS: In this study, we used 91,103 scRNA-seq samples from 29 patients with colorectal cancer (GSE144735 and GSE132465)...
March 25, 2024: BMC Cancer
https://read.qxmd.com/read/38521952/enhanced-bacterial-cancer-therapy-delivering-therapeutic-rna-interference-of-c-myc
#3
JOURNAL ARTICLE
Jason S Williams, Adam T Higgins, Katie J Stott, Carly Thomas, Lydia Farrell, Cleo S Bonnet, Severina Peneva, Anna V Derrick, Trevor Hay, Tianqi Wang, Claire Morgan, Sarah Dwyer, Joshua D'Ambrogio, Catherine Hogan, Matthew J Smalley, Lee Parry, Paul Dyson
BACKGROUND: Bacterial cancer therapy was first trialled in patients at the end of the nineteenth century. More recently, tumour-targeting bacteria have been harnessed to deliver plasmid-expressed therapeutic interfering RNA to a range of solid tumours. A major limitation to clinical translation of this is the short-term nature of RNA interference in vivo due to plasmid instability. To overcome this, we sought to develop tumour-targeting attenuated bacteria that stably express shRNA by virtue of integration of an expression cassette within the bacterial chromosome and demonstrate therapeutic efficacy in vitro and in vivo...
March 23, 2024: Cell & Bioscience
https://read.qxmd.com/read/38520870/unveil-the-mechanism-for-ehmt-a-novel-triterpenoid-inhibits-proliferation-and-induces-apoptosis-in-colon-cancer-through-ros-mediated-jnk-signaling-pathway
#4
JOURNAL ARTICLE
Qiushuang Wu, Min Song, Siyuan Luo, Libin Guo, Qingwen Zhang, Hang Fai Kwok
Colon cancer ranks among the most prevalent malignancies worldwide, trailing only lung and breast cancer in incidence. Despite the availability of numerous therapeutic strategies, the burden of new cases and fatalities remains high in countries undergoing socioeconomic transitions. Natural products offer promising avenues for developing more effective and less toxic anticancer agents, expanding the clinical arsenal. In this investigation, we isolated a triterpenoid, (21 S,23 R,24 R)-21,23-epoxy-24-hydroxy-21-methoxytirucalla-7,25-dien-3-one (EHMT), from the fruits of Melia azedarach L...
March 22, 2024: Biomedicine & Pharmacotherapy
https://read.qxmd.com/read/38519550/three-new-phthalide-derivatives-from-culture-broth-of-dentipellis-fragilis-and-their-cytotoxic-activities
#5
JOURNAL ARTICLE
Dae-Won Ki, Dae-Cheol Choi, Yeong-Seon Won, Seung-Jae Lee, Young-Hee Kim, In-Kyoung Lee, Bong-Sik Yun
Three new phthalide derivatives (1‒3) together with two known compounds, erinaceolactone B (4) and hericerin III (5), were isolated from the culture broth of Dentipellis fragilis. The chemical structures of 1‒5 were determined by analyses of their 1D-, 2D-NMR, and MS. The absolute configuration of 1 was determined by CD analysis. The isolated compounds were assessed for their cytotoxic activities against A549, DU145, HCT116, and HT1080 cancer cell lines. Compounds 1‒5 showed strong cytotoxic activities against DU145, with IC50 values ranging from 14...
March 22, 2024: Journal of Antibiotics
https://read.qxmd.com/read/38518246/copper-ii-complexes-with-2-2-6-2%C3%A2-terpyridine-derivatives-displaying-dimeric-dichloro-%C3%AE-bridged-crystal-structure-biological-activities-from-2d-and-3d-tumor-spheroids-to-in-vivo-models
#6
JOURNAL ARTICLE
Katarzyna Choroba, Barbara Machura, Karol Erfurt, Ana Rita Casimiro, Sandra Cordeiro, Pedro V Baptista, Alexandra R Fernandes
Eight 2,2':6',2″-terpyridines, substituted at the 4'-position with aromatic groups featuring variations in π-conjugation, ring size, heteroatoms, and methoxy groups, were employed to enhance the antiproliferative potential of [Cu2 Cl2 (R-terpy)2 ](PF6 )2 . Assessing the cytotoxicity in A2780 (ovarian carcinoma), HCT116 (colorectal carcinoma), and HCT116DoxR (colorectal carcinoma resistant to doxorubicin) and normal primary fibroblasts revealed that Cu(II) complexes with 4-quinolinyl, 4-methoxy-1-naphthyl, 2-furanyl, and 2-pyridynyl substituents showed superior therapeutic potential in HCT116DoxR cells with significantly reduced cytotoxicity in normal fibroblasts (42-129× lower)...
March 22, 2024: Journal of Medicinal Chemistry
https://read.qxmd.com/read/38517383/cinobufotalin-regulates-the-usp36-c-myc-axis-to-suppress-malignant-phenotypes-of-colon-cancer-cells-in-vitro-and-in-vivo
#7
JOURNAL ARTICLE
Yongjun Hu, Ming Luo
Ubiquitin-specific protease 36 (USP36) has been reported to exhibit oncogenic effects in various malignancies, but the function of USP36 in colon cancer progression remains indefinite. Herein, we aimed to determine the role and mechanism of USP36 in malignant phenotypes of colon cancer cells and explore the potential drug targeting USP36. Bioinformatics analyses indicated that USP36 is highly expressed and significantly related to tumor stages in colon cancer. Besides, USP36 was further up-regulated in oxaliplatin (Oxa)-resistant colon cancer cells...
March 15, 2024: Aging
https://read.qxmd.com/read/38516604/design-synthesis-and-biological-evaluation-of-rhein-piperazine-furanone-hybrids-as-potential-anticancer-agents
#8
JOURNAL ARTICLE
Yu He, Si-Si Zhang, Meng-Xue Wei
Novel rhein-piperazine-furanone hybrids, 5, were designed and synthesized efficiently from rhein. Cytotoxicity of all hybrids 5a-j against A549 human lung cancer cells was superior to the parent rhein and the reference cytarabine (CAR). Hybrid 5e (IC50 = 5.74 μM), the most potent compound, was 46- and 35-fold more toxic against A549 cells than rhein (IC50 = 265.59 μM) and CAR (IC50 = 202.57 μM), respectively. Moreover, hybrid 5e (IC50 = 69.28 μM) was less toxic to normal WI-38 human lung fibroblast cells with good selectivity (WI-38/A549, SI ≈ 12), being much higher than rhein (SI ≈ 1) and CAR (SI ≈ 2)...
March 20, 2024: RSC medicinal chemistry
https://read.qxmd.com/read/38513729/synthesis-and-characterisation-of-a-nucleotide-based-pro-drug-formulated-with-a-peptide-into-a-nano-chemotherapy-for-colorectal-cancer
#9
JOURNAL ARTICLE
Jordan J Wilson, Lindsey Bennie, Olga Eguaogie, Ahmed Elkashif, Patrick F Conlon, Lynn Jena, Emma McErlean, Niamh Buckley, Klaudia Englert, Nicholas J Dunne, James H R Tucker, Joseph S Vyle, Helen O McCarthy
Recent studies in colorectal cancer patients (CRC) have shown that increased resistance to thymidylate synthase (TS) inhibitors such as 5-fluorouracil (5-FU), reduce the efficacy of standard of care (SoC) treatment regimens. The nucleotide pool cleanser dUTPase is highly expressed in CRC and is an attractive target for potentiating anticancer activity of chemotherapy. The purpose of the current work was to investigate the activity of P1 , P4 -di(2',5'-dideoxy-5'-selenouridinyl)-tetraphosphate (P4 -SedU2 ), a selenium-modified symmetrically capped dinucleoside with prodrug capabilities that is specifically activated by dUTPase...
March 19, 2024: Journal of Controlled Release
https://read.qxmd.com/read/38508501/accumulation-of-antitumor-polyketides-by-fermentation-of-rubus-delavayi-franch-with-clonostachys-rogersoniana
#10
JOURNAL ARTICLE
Rui-Feng Mei, Jia Su, Guo-Xian Hu, Rui-Dang Yang, Bi-Jian He, Ya-Xian Shi, Le Cai, Zhong-Tao Ding
The aim of this work is to explore the effects of herbal medicine on secondary metabolites of microorganisms during fermentation. Clonostachys rogersoniana was found to metabolize only small amounts of polyketide glycosides rogerson B and C on fresh potatoes, but after replacing the medium to the medicinal plant Rubus delavayi Franch., the type and content of the metabolized polyketones showed significant changes. The sugars and glycosides in R. delavayi are probably responsible for the changes in secondary metabolites...
March 18, 2024: Fitoterapia
https://read.qxmd.com/read/38507104/integrative-approach-using-network-pharmacology-bioinformatics-and-experimental-methods-to-explore-the-mechanism-of-cantharidin-in-treating-colorectal-cancer
#11
JOURNAL ARTICLE
Benchao Hou, Xiaomin Wang, Zhijian He, Haiyun Liu
Cantharidin, a terpenoid produced by blister beetles, has been used in traditional Chinese medicine to treat various ailments and cancers. However, its biological activity, impact, and anticancer mechanisms remain unclear. The Cantharidin chemical gene connections were identified using various databases. The GSE21815 dataset was used to collect the gene expression information. Differential gene analysis and gene ontology analyses were performed. Gene set enrichment analysis was used to assess the activation of disease pathways...
March 20, 2024: Naunyn-Schmiedeberg's Archives of Pharmacology
https://read.qxmd.com/read/38506227/photoactive-imaging-and-therapy-for-colorectal-cancer-using-a-cea-affimer-conjugated-foslip-nanoparticle
#12
JOURNAL ARTICLE
Yazan S Khaled, M Ibrahim Khot, Radhika Aiyappa-Maudsley, Thomas Maisey, Arindam Pramanik, Jim Tiernan, Nicole Lintern, Eiman Al-Enezi, Shazana H Shamsuddin, Darren Tomlinson, Louise Coletta, Paul A Millner, Thomas A Hughes, David G Jayne
Theranostic nanoparticles hold promise for simultaneous imaging and therapy in colorectal cancer. Carcinoembryonic antigen can be used as a target for these nanoparticles because it is overexpressed in most colorectal cancers. Affimer reagents are synthetic proteins capable of binding specific targets, with additional advantages over antibodies for targeting. We fabricated silica nanoparticles using a water-in-oil microemulsion technique, loaded them with the photosensitiser Foslip, and functionalised the surface with anti-CEA Affimers to facilitate fluorescence imaging and photodynamic therapy of colorectal cancer...
March 20, 2024: Nanoscale
https://read.qxmd.com/read/38505918/increased-pkn2-and-m2-polarized-macrophages-promote-hct116-cell-invasion
#13
JOURNAL ARTICLE
Cheng He, Yimei Lin, Feng Qiu, Qingxin Zeng
Colorectal cancer is the third most common malignant tumor, with highly invasive and metastatic potential in the later stage. This study investigated the role of PKN2 overexpression and M2-polarized macrophages in dictating the malignant phenotype of colorectal cancer cells. HCT116 colorectal cancer cell line with PKN2 overexpression was generated to investigate the functional role of PKN2. THP-1 cells were polarized into M2-like macrophages, and the co-culture system of THP-1/M2 cells and HCT116 cells was established to examine the impacts of M2-polairzed macrophages on the malignant phenotype of colorectal cancer cells...
2024: Critical Reviews in Immunology
https://read.qxmd.com/read/38504172/art1-knockdown-decreases-the-il-6-induced-proliferation-of-colorectal-cancer-cells
#14
JOURNAL ARTICLE
Ting Lin, Shuxian Zhang, Yi Tang, Ming Xiao, Ming Li, Hanjuan Gong, Hailun Xie, Yalan Wang
Colorectal cancer (CRC) is a worldwide health concern. Chronic inflammation is a risk factor for CRC, and interleukin-6 (IL-6) plays a pivotal role in this process. Arginine-specific mono-ADP-ribosyltransferase-1 (ART1) positively regulates inflammatory cytokines. ART1 knockdown reduces the level of glycoprotein 130 (gp130), a key transducer in the IL-6 signalling pathway. However, the relationship between ART1 and IL-6 and the resulting effects on IL-6-induced proliferation in CRC cells remain unclear. The aims of this study were to investigate the effects of ART1 knockdown on IL-6-induced cell proliferation in vitro and use an in vivo murine model to observe the growth of transplanted tumours...
March 19, 2024: BMC Cancer
https://read.qxmd.com/read/38502532/exploiting-co-iii-cyclopentadienyl-complexes-to-develop-anticancer-agents
#15
JOURNAL ARTICLE
João Franco Machado, Sandra Cordeiro, Joana N Duarte, Paulo J Costa, Paulo J Mendes, Maria Helena Garcia, Pedro V Baptista, Alexandra R Fernandes, Tânia S Morais
In recent years, organometallic complexes have attracted much attention as anticancer therapeutics aiming at overcoming the limitations of platinum drugs that are currently marketed. Still, the development of half-sandwich organometallic cobalt complexes remains scarcely explored. Four new cobalt(III)-cyclopentadienyl complexes containing N,N-heteroaromatic bidentate, and phosphane ligands were synthesized and fully characterized by elemental analysis, spectroscopic techniques, and DFT methods. The cytotoxicity of all complexes was determined in vitro by the MTS assay in colorectal (HCT116), ovarian (A2780), and breast (MDA-MB-231 and MCF-7) human cancer cell lines and in a healthy human cell line (fibroblasts)...
March 19, 2024: Inorganic Chemistry
https://read.qxmd.com/read/38498382/effect-of-cu-ii-compound-containing-dipicolinic-acid-on-dna-damage-a-study-of-antiproliferative-activity-and-dna-interaction-properties-by-spectroscopic-molecular-docking-and-molecular-dynamics-approaches
#16
JOURNAL ARTICLE
Ameneh Heidari, Effat Dehghanian, Zohreh Razmara, Somaye Shahraki, Hojat Samareh Delarami, Mostafa Heidari Majd
A polymeric compound formulized as [Cu(µ-dipic)2 {Na2 (µ-H2 O)4 ]n .2nH2 O ( I ), where dipic is 2,6-pyridine dicarboxylic acid (dipicolinic acid, H2 dipic), was synthesized by sonochemical irradiation. The initial in-vitro cytotoxic activity of this complex compared with renowned anticancer drugs like cisplatin, versus HCT116 colon cell lines, shows promising results. This study investigated the interaction mode between compound ( I ) and calf-thymus DNA utilizing a range of analytical techniques including spectrophotometry, fluorimetry, partition coefficient analysis, viscometry, gel electrophoresis and molecular docking technique...
March 18, 2024: Journal of Biomolecular Structure & Dynamics
https://read.qxmd.com/read/38494866/targeted-inhibition-of-colorectal-cancer-proliferation-the%C3%A2-dual-modulatory-role-of-2-4-dtbp-on-anti-apoptotic-bcl-2-and-survivin-proteins
#17
JOURNAL ARTICLE
Partha Saha, Mangala Hegde, Kanak Chakraborty, Achinta Singha, Nobendu Mukerjee, Deepshikha Ghosh, Ajaikumar B Kunnumakkara, Mohd Shahnawaz Khan, Md Irshad Ahmad, Arabinda Ghosh, Ajoy Kumer, Samir Kumar Sil
The anti-apoptotic proteins, Bcl-2 and Survivin, are consistently overexpressed in numerous human malignancies, notably in colorectal cancer. 2,4-Di-tert-butylphenol (2,4-DTBP) is a naturally occurring phenolic compound known for its diverse biological activities, including anti-cancer properties. The mechanism behind 2,4-DTBP-induced inhibition of cell proliferation and apoptosis in human colorectal cancer cells, specifically regarding Bcl-2 and Survivin, remains to be elucidated. In this study, we employed both in silico and in vitro methodologies to underpin this interaction at the molecular level...
April 2024: Journal of Cellular and Molecular Medicine
https://read.qxmd.com/read/38492819/cafestol-inhibits-colon-cancer-cell-proliferation-and-tumor-growth-in-xenograft-mice-by-activating-lkb1-ampk-ulk1-dependent-autophagy
#18
JOURNAL ARTICLE
Yuemei Feng, JiZhuo Yang, Yihan Wang, Xue Wang, Qian Ma, Yalin Li, Xuehui Zhang, Songmei Wang, Qiao Zhang, Fei Mi, Yanjiao Wang, Dubo Zhong, Jianzhong Yin
Chemotherapy failure in colorectal cancer patients is the major cause of recurrence and poor prognosis. As a result, there is an urgent need to develop drugs that have a good chemotherapy effect while also being extremely safe. In this study, we found cafestol inhibited colon cancer growth and HCT116 proliferation in vivo and in vitro, and improved the composition of intestinal flora. Further metabolomic data showed that autophagy and AMPK pathways were involved in the process of cafestol's anti-colon cancer effects...
March 14, 2024: Journal of Nutritional Biochemistry
https://read.qxmd.com/read/38491042/bionanofactory-for-green-synthesis-of-collagen-nanoparticles-characterization-optimization-in-vitro-and-in-vivo-anticancer-activities
#19
JOURNAL ARTICLE
Asmaa A El-Sawah, Noura El-Ahmady El-Naggar, Heba E Eldegla, Hoda M Soliman
Collagen nanoparticles (collagen-NPs) are promising biological polymer nanoparticles due to their exceptional biodegradability and biocompatibility. Collagen-NPs were bio-fabricated from pure marine collagen using the cell-free supernatant of a newly isolated strain, Streptomyces sp. strain NEAA-3. Streptomyces sp. strain NEAA-3 was identified as Streptomyces plicatus strain NEAA-3 based on its cultural, morphological, physiological properties and 16S rRNA sequence analysis. The sequence data has been deposited under accession number OR501412...
March 15, 2024: Scientific Reports
https://read.qxmd.com/read/38488882/identification-of-a-novel-selective-cdk9-inhibitor-for-the-treatment-of-crc-design-synthesis-and-biological-activity-evaluation
#20
JOURNAL ARTICLE
Ye Zhong, Jing Xu, Ruochen Zhou, Li Tang, Shaoyue Ding, Zhaohui Ren, Ning Song, Baichun Hu, Huali Yang, Yili Sun, Maosheng Cheng, Jia Li, Yang Liu
Cyclin-dependent kinase 9 (CDK9) is a member of the transcription CDK subfamily. In this work, we preliminarily demonstrated the feasibility of CDK9 as a potent target of treatment for colorectal cancer, and a series of novel CDK9 inhibitors were rationally designed and synthesized based on the structure of AZD5438 (a pan CDKs inhibitor reported by AstraZeneca). A novel selective CDK9 inhibitor named CLZX-205, which possessed significant CDK9 inhibitory activity (IC50 = 2.9 nM) with acceptable pharmacokinetic properties and antitumor efficacy in vitro and in vivo, was developed...
March 15, 2024: Journal of Medicinal Chemistry
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