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Wnt pharmaceutics

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https://www.readbyqxmd.com/read/27567978/wnt-%C3%AE-catenin-signaling-inhibitor-icg-001-enhances-pigmentation-of-cultured-melanoma-cells
#1
Kyung-Il Kim, Do-Sun Jeong, Eui Chang Jung, Jeung-Hoon Lee, Chang Deok Kim, Tae-Jin Yoon
BACKGROUND: Wnt/β-catenin signaling is important in development and differentiation of melanocytes. OBJECTIVE: The object of this study was to evaluate the effects of several Wnt/β-catenin signaling inhibitors on pigmentation using melanoma cells. METHODS: Melanoma cells were treated with Wnt/β-catenin signaling inhibitors, and then melanin content and tyrosinase activity were checked. RESULTS: Although some inhibitors showed slight inhibition of pigmentation, we failed to observe potential inhibitory effect of those chemicals on pigmentation of HM3KO melanoma cells...
August 20, 2016: Journal of Dermatological Science
https://www.readbyqxmd.com/read/27500408/large-scale-production-of-cardiomyocytes-from-human-pluripotent-stem-cells-using-a-highly-reproducible-small-molecule-based-differentiation-protocol
#2
Hananeh Fonoudi, Hassan Ansari, Saeed Abbasalizadeh, Gillian M Blue, Nasser Aghdami, David S Winlaw, Richard P Harvey, Alexis Bosman, Hossein Baharvand
Maximizing the benefit of human pluripotent stem cells (hPSCs) for research, disease modeling, pharmaceutical and clinical applications requires robust methods for the large-scale production of functional cell types, including cardiomyocytes. Here we demonstrate that the temporal manipulation of WNT, TGF-β, and SHH signaling pathways leads to highly efficient cardiomyocyte differentiation of single-cell passaged hPSC lines in both static suspension and stirred suspension bioreactor systems. Employing this strategy resulted in ~ 100% beating spheroids, consistently containing > 80% cardiac troponin T-positive cells after 15 days of culture, validated in multiple hPSC lines...
2016: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/27397144/astragaloside-i-stimulates-osteoblast-differentiation-through-the-wnt-%C3%AE-catenin-signaling-pathway
#3
Xun Cheng, Biaofang Wei, Lijuan Sun, Xiaofang Hu, Jichao Liang, Yong Chen
Astragaloside I (As-I), one of the main active ingredients in Astragalus membranaceus, is believed to have osteogenic properties, but this hypothesis has not been investigated in detail. In the present work, the As-I-induced osteogenic effects and its underlying mechanism were studied in MC3T3-E1 cells. The results indicated that the cellular levels of ALP and extracellular matrix calcium increased in a dose-dependent manner by As-I. To clarify the mechanisms involved in this process, the effect of As-I on the key osteogenic-related genes was investigated...
July 10, 2016: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/27351373/pentoxifylline-inhibits-wnt-signalling-in-%C3%AE-cateninhigh-patient-derived-melanoma-cell-populations
#4
Beata Talar, Anna Gajos-Michniewicz, Marcin Talar, Salem Chouaib, Malgorzata Czyz
BACKGROUND: The heterogeneity of melanoma needs to be addressed and combination therapies seem to be necessary to overcome intrinsic and acquired resistance to newly developed immunotherapies and targeted therapies. Although the role of WNT/β-catenin pathway in melanoma was early demonstrated, its contribution to the lack of the melanoma patient response to treatment was only recently recognized. Using patient-derived melanoma cell populations, we investigated the influence of pentoxifylline on melanoma cells with either high or low expression of β-catenin...
2016: PloS One
https://www.readbyqxmd.com/read/27294914/protective-effect-of-ginsenoside-rg1-on-hematopoietic-stem-progenitor-cells-through-attenuating-oxidative-stress-and-the-wnt-%C3%AE-catenin-signaling-pathway-in-a-mouse-model-of-d-galactose-induced-aging
#5
Jing Li, Dachuan Cai, Xin Yao, Yanyan Zhang, Linbo Chen, Pengwei Jing, Lu Wang, Yaping Wang
Stem cell senescence is an important and current hypothesis accounting for organismal aging, especially the hematopoietic stem cell (HSC). Ginsenoside Rg1 is the main active pharmaceutical ingredient of ginseng, which is a traditional Chinese medicine. This study explored the protective effect of ginsenoside Rg1 on Sca-1⁺ hematopoietic stem/progenitor cells (HSC/HPCs) in a mouse model of d-galactose-induced aging. The mimetic aging mouse model was induced by continuous injection of d-gal for 42 days, and the C57BL/6 mice were respectively treated with ginsenoside Rg1, Vitamin E or normal saline after 7 days of d-gal injection...
2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27143851/baicalein-suppresses-metastasis-of-breast-cancer-cells-by-inhibiting-emt-via-downregulation-of-satb1-and-wnt-%C3%AE-catenin-pathway
#6
Xingcong Ma, Wanjun Yan, Zhijun Dai, Xiaoyan Gao, Yinan Ma, Quntao Xu, Jiantao Jiang, Shuqun Zhang
BACKGROUND: The flavonoid baicalein, a historically used Chinese herbal medicine, shows a wide range of biological and pharmaceutical effects, among which its potent antitumor activity has raised great interest in recent years. However, the molecular mechanism involved in the antimetastatic effect of baicalein remains poorly understood. This study aimed to verify the inhibitory effects of baicalein on metastasis of MDA-MB-231 human breast cancer cells both in vitro and in vivo, as well as to investigate the related mechanisms...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27142748/effects-of-quercetin-a-natural-phenolic-compound-in-the-differentiation-of-human-mesenchymal-stem-cells-msc-into-adipocytes-and-osteoblasts
#7
Antonio Casado-Díaz, Jaouad Anter, Gabriel Dorado, José Manuel Quesada-Gómez
Natural phenols may have beneficial properties against oxidative stress, which is associated with aging and major chronic aging-related diseases, such as loss of bone mineral mass (osteoporosis) and diabetes. The main aim of this study was to analyze the effect of quercetin, a major nutraceutical compound present in the "Mediterranean diet", on mesenchymal stem-cell (MSC) differentiation. Such cells were induced to differentiate into osteoblasts or adipocytes in the presence of two quercetin concentrations (0...
June 2016: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/26626076/the-role-of-wnt-regulation-in-heart-development-cardiac-repair-and-disease-a-tissue-engineering-perspective
#8
REVIEW
Aric Pahnke, Genna Conant, Locke Davenport Huyer, Yimu Zhao, Nicole Feric, Milica Radisic
Wingless-related integration site (Wnt) signaling has proven to be a fundamental mechanism in cardiovascular development as well as disease. Understanding its particular role in heart formation has helped to develop pluripotent stem cell differentiation protocols that produce relatively pure cardiomyocyte populations. The resultant cardiomyocytes have been used to generate heart tissue for pharmaceutical testing, and to study physiological and disease states. Such protocols in combination with induced pluripotent stem cell technology have yielded patient-derived cardiomyocytes that exhibit some of the hallmarks of cardiovascular disease and are therefore being used to model disease states...
May 6, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/26613980/2-amino-4-3-4-methylenedioxy-benzylamino-6-3-methoxyphenyl-pyrimidine-is-an-anti-inflammatory-tlr-2-4-and-5-response-mediator-in-human-monocytes
#9
Huizhi Wang, Mark W Graves, Huaxin Zhou, Zhen Gu, Richard J Lamont, David A Scott
OBJECTIVE AND DESIGN: To elucidate the influence of 2-amino-4-(3,4-(methylenedioxy)benzylamino)-6-(3-methoxyphenyl)pyrimidine (AMBMP), a canonical Wnt/β-catenin pathway activator, on the inflammatory response of TLR-engaged innate cells in vitro. MATERIAL OR SUBJECT: Primary human monocytes. TREATMENT: AMPMB (0-10 μM), LPS (0-1.0 μg/ml), Pam3CSK4, FSL-1, or S. typhimurium flagellin (0-0.25 μg/ml). METHODS: TLR-induced cytokine release (TNF, IL-6, IL-12 p40) was monitored by ELISA while Wnt-related signals (GSK3β, p65, IκB, β-catenin) were assessed by Western blot, pharmaceutical inhibition and gene silencing...
January 2016: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
https://www.readbyqxmd.com/read/26554834/missense-mutations-in-lrp5-associated-with-high-bone-mass-protect-the-mouse-skeleton-from-disuse-and-ovariectomy-induced-osteopenia
#10
Paul J Niziolek, Whitney Bullock, Matthew L Warman, Alexander G Robling
The low density lipoprotein receptor-related protein-5 (LRP5), a co-receptor in the Wnt signaling pathway, modulates bone mass in humans and in mice. Lrp5 knock-out mice have severely impaired responsiveness to mechanical stimulation whereas Lrp5 gain-of-function knock-in and transgenic mice have enhanced responsiveness to mechanical stimulation. Those observations highlight the importance of Lrp5 protein in bone cell mechanotransduction. It is unclear if and how high bone mass-causing (HBM) point mutations in Lrp5 alter the bone-wasting effects of mechanical disuse...
2015: PloS One
https://www.readbyqxmd.com/read/26522946/the-use-of-porcupine-inhibitors-to-target-wnt-driven-cancers
#11
REVIEW
Soo Yei Ho, Thomas H Keller
Over the past decade, academic groups and pharmaceutical companies have uncovered several components and targets for intervention in the Wnt pathway. One approach is to block Wnt signalling through the use of orally bioavailable small molecules that prevent Wnt ligand secretion. In recent years, the membrane bound O-acyl transferase (MBOAT) porcupine (PORCN) has emerged as a molecular target of interest in the search for clinical options to treat Wnt-driven cancers. This review shall provide an overview of the reported small molecule inhibitors for PORCN and discuss the progress made in identifying human disease models that are responsive to PORCN inhibitors...
December 1, 2015: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/26511653/a-universal-and-robust-integrated-platform-for-the-scalable-production-of-human-cardiomyocytes-from-pluripotent-stem-cells
#12
Hananeh Fonoudi, Hassan Ansari, Saeed Abbasalizadeh, Mehran Rezaei Larijani, Sahar Kiani, Shiva Hashemizadeh, Ali Sharifi Zarchi, Alexis Bosman, Gillian M Blue, Sara Pahlavan, Matthew Perry, Yishay Orr, Yaroslav Mayorchak, Jamie Vandenberg, Mahmood Talkhabi, David S Winlaw, Richard P Harvey, Nasser Aghdami, Hossein Baharvand
UNLABELLED: Recent advances in the generation of cardiomyocytes (CMs) from human pluripotent stem cells (hPSCs), in conjunction with the promising outcomes from preclinical and clinical studies, have raised new hopes for cardiac cell therapy. We report the development of a scalable, robust, and integrated differentiation platform for large-scale production of hPSC-CM aggregates in a stirred suspension bioreactor as a single-unit operation. Precise modulation of the differentiation process by small molecule activation of WNT signaling, followed by inactivation of transforming growth factor-β and WNT signaling and activation of sonic hedgehog signaling in hPSCs as size-controlled aggregates led to the generation of approximately 100% beating CM spheroids containing virtually pure (∼90%) CMs in 10 days...
December 2015: Stem Cells Translational Medicine
https://www.readbyqxmd.com/read/26478571/berberine-promotes-bone-marrow-derived-mesenchymal-stem-cells-osteogenic-differentiation-via-canonical-wnt-%C3%AE-catenin-signaling-pathway
#13
Ke Tao, Deming Xiao, Jian Weng, Ao Xiong, Bin Kang, Hui Zeng
Berberine (BBR) has recently been reported to be extensively used for musculoskeletal disorders such as osteoporosis through enhancing osteogenic differentiation, inhibiting osteoclastogenesis and bone resorption and repressing adipogenesis. Although canonical Wnt signaling plays a crucial role in suppressing bone marrow-derived mesenchymal stem cells (MSCs) commitment to the chondrogenic and adipogenic lineage and enhancing osteogenic differentiation, no previous reports have shown an association between BBR-induced osteogenesis and Wnt/β-catenin signaling pathway...
January 5, 2016: Toxicology Letters
https://www.readbyqxmd.com/read/26439805/targeting-the-wnt-signaling-pathway-in-colorectal-cancer
#14
REVIEW
Masaaki Sawa, Mari Masuda, Tesshi Yamada
INTRODUCTION: The treatment of patients with advanced colorectal cancer still remains challenging, and identification of new target molecules and therapeutic avenues remains a priority. The great majority of colorectal cancers have mutations in one of two genes involved in the Wnt signaling pathway: the adenomatous polyposis coli (APC) and β-catenin (CTNNB1) genes. Up to now, however, no therapeutics for targeting this pathway have been established. AREAS COVERED: This review article begins with a brief summary of Wnt signaling from the viewpoints of genetics, cancer stem cell biology, and drug development...
2016: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/26275858/pharmaceutical-inhibition-of-glycogen-synthetase-kinase-3-beta-suppresses-wear-debris-induced-osteolysis
#15
Dechun Geng, Jian Wu, Hongguo Shao, Shijun Zhu, Yijun Wang, Wen Zhang, Zichuan Ping, Xuanyang Hu, Xuesong Zhu, Yaozeng Xu, Huilin Yang
Aseptic loosening is associated with the development of wear debris-induced peri-implant osteolytic bone disease caused by an increased osteoclastic bone resorption and decreased osteoblastic bone formation. However, no effective measures for the prevention and treatment of peri-implant osteolysis currently exist. The aim of this study was to determine whether lithium chloride (LiCl), a selective inhibitor of glycogen synthetase kinase 3 beta (GSK-3β), mitigates wear debris-induced osteolysis in a murine calvarial model of osteolysis...
November 2015: Biomaterials
https://www.readbyqxmd.com/read/26273492/a-comprehensive-overview-of-skeletal-phenotypes-associated-with-alterations-in-wnt-%C3%AE-catenin-signaling-in-humans-and-mice
#16
REVIEW
Kevin A Maupin, Casey J Droscha, Bart O Williams
The Wnt signaling pathway plays key roles in differentiation and development and alterations in this signaling pathway are causally associated with numerous human diseases. While several laboratories were examining roles for Wnt signaling in skeletal development during the 1990s, interest in the pathway rose exponentially when three key papers were published in 2001-2002. One report found that loss of the Wnt co-receptor, Low-density lipoprotein related protein-5 (LRP5), was the underlying genetic cause of the syndrome Osteoporosis pseudoglioma (OPPG)...
March 2013: Bone Research
https://www.readbyqxmd.com/read/26259537/is-mir-34a-a-well-equipped-swordsman-to-conquer-temple-of-molecular-oncology
#17
REVIEW
Ammad Ahmad Farooqi, Sundas Fayyaz, Iryna Shatynska-Mytsyk, Zeeshan Javed, Saima Jabeen, Ilhan Yaylim, Maria Luisa Gasparri, Pierluigi Benedetti Panici
Overwhelmingly increasing advancements in miRNA biology have opened new avenues for pharmaceutical companies to initiate studies on designing effective, safe, and therapeutically active candidates using miRNA mimetics and miRNA inhibitors. In accordance with this approach, development of miravirsen and SPC3649, an LNA-based (locked nucleic acid) antisense molecule against miR-122, to treat hepatitis C has sparked interest in identifying most efficient microRNAs for journey from bench-top toward pharmaceutical industry and breakthroughs in delivery technology will pave the way to 'final frontier'...
March 2016: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/26210995/novel-small-molecule-inhibitors-of-cancer-stem-cell-signaling-pathways
#18
Danysh Abetov, Zhanar Mustapova, Timur Saliev, Denis Bulanin, Kanat Batyrbekov, Charles P Gilman
The main aim of oncologists worldwide is to understand and then intervene in the primary tumor initiation and propagation mechanisms. This is essential to allow targeted elimination of cancer cells without altering normal mitotic cells. Currently, there are two main rival theories describing the process of tumorigenesis. According to the Stochastic Model, potentially any cell, once defunct, is capable of initiating carcinogenesis. Alternatively the Cancer Stem Cell (CSC) Model posits that only a small fraction of undifferentiated tumor cells are capable of triggering carcinogenesis...
December 2015: Stem Cell Reviews
https://www.readbyqxmd.com/read/26177200/novel-phenotypic-outcomes-identified-for-a-public-collection-of-approved-drugs-from-a-publicly-accessible-panel-of-assays
#19
Jonathan A Lee, Paul Shinn, Susan Jaken, Sarah Oliver, Francis S Willard, Steven Heidler, Robert B Peery, Jennifer Oler, Shaoyou Chu, Noel Southall, Thomas S Dexheimer, Jeffrey Smallwood, Ruili Huang, Rajarshi Guha, Ajit Jadhav, Karen Cox, Christopher P Austin, Anton Simeonov, G Sitta Sittampalam, Saba Husain, Natalie Franklin, David J Wild, Jeremy J Yang, Jeffrey J Sutherland, Craig J Thomas
Phenotypic assays have a proven track record for generating leads that become first-in-class therapies. Whole cell assays that inform on a phenotype or mechanism also possess great potential in drug repositioning studies by illuminating new activities for the existing pharmacopeia. The National Center for Advancing Translational Sciences (NCATS) pharmaceutical collection (NPC) is the largest reported collection of approved small molecule therapeutics that is available for screening in a high-throughput setting...
2015: PloS One
https://www.readbyqxmd.com/read/26087309/doxycycline-down-regulates-dna-pk-and-radiosensitizes-tumor-initiating-cells-implications-for-more-effective-radiation-therapy
#20
Rebecca Lamb, Marco Fiorillo, Amy Chadwick, Bela Ozsvari, Kimberly J Reeves, Duncan L Smith, Robert B Clarke, Sacha J Howell, Anna Rita Cappello, Ubaldo E Martinez-Outschoorn, Maria Peiris-Pagès, Federica Sotgia, Michael P Lisanti
DNA-PK is an enzyme that is required for proper DNA-repair and is thought to confer radio-resistance in cancer cells. As a consequence, it is a high-profile validated target for new pharmaceutical development. However, no FDA-approved DNA-PK inhibitors have emerged, despite many years of drug discovery and lead optimization. This is largely because existing DNA-PK inhibitors suffer from poor pharmacokinetics. They are not well absorbed and/or are unstable, with a short plasma half-life. Here, we identified the first FDA-approved DNA-PK inhibitor by "chemical proteomics"...
June 10, 2015: Oncotarget
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