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Non-steroidal anti-inflammatory drugs (NSAIDs) have been suggested as the potential new class of preventive or therapeutic antitumor agents. The aim of the present study was to evaluate the antitumor activity of the novel NSAID, CG100649. CG100649 is a novel NSAID dual inhibitor for COX-2 and carbonic anhydrase (CA)-I/-II. In the present study, we investigated the alternative mechanism by which CG100649 mediated suppression of the colon cancer growth and development. The anchorage-dependent and -independent clonogenic assay showed that CG100649 inhibited the clonogenicity of human colon cancer cells. The flow cytometric analysis showed that CG100649 induced the G2/M cell cycle arrest in colon cancer cells. Animal studies showed that CG100649 inhibited the tumor growth in colon cancer xenograft in nude mice. Furthermore, quantitative PCR and FACS analysis demonstrated that CG100649 upregulated the expression of TNF-related apoptosis-inducing ligand (TRAIL) receptors (DR4 and DR5) but decreased the expression of decoy receptors (DcR1 and DcR2) in colon cancer cells. The results showed that CG100649 treatment sensitized TRAIL-mediated growth suppression and apoptotic cell death. The combination treatment resulted in significant repression of the intestinal polyp formation in APCmin/+ mice. Our data clearly demonstrated that CG100649 contains preventive and therapeutic activity for colon cancer. The present study may be useful for identification of the potential benefit of the NSAID CG100649, for the achievement of a better treatment response in colon cancer.


Non-steroidal anti-inflammatory drugs (NSAIDs) have been suggested as the potential new class of preventive or therapeutic antitumor agents. The aim of the present study was to evaluate the antitumor activity of the novel NSAID, CG100649. CG100649 is a novel NSAID dual inhibitor for COX-2 and carbonic anhydrase (CA)-I/-II. In the present study, we investigated the alternative mechanism by which CG100649 mediated suppression of the colon cancer growth and development. The anchoragedependentand-independent clonogenic assay showed that CG100649 inhibited the clonogenicity of human colon cancer cells. The flow cytometric analysis showed that CG100649 induced the G2/M cell cycle arrest in colon cancer cells. Animal studies showed that CG100649 inhibited the tumor growth in colon cancer xenograft in nude mice. Furthermore, quantitative PCR and FACS analysis demonstrated that CG100649 upregulated the expression of TNF-related apoptosis-inducing ligand (TRAIL) receptors (DR4 and DR5) but decreased the expression of decoy receptors (DcR1 and DcR2) in colon cancer cells. The results showed that CG100649 treatment sensitized TRAILmediated growth suppression and apoptotic cell death. The combination treatment resulted in significant repression of the intestinal polyp formation in APCmin/+ mice. Our data clearly demonstrated that CG100649 contains preventive and therapeutic activity for colon cancer. The present study may be useful for identification of the potential benefit of the NSAID CG100649, for the achievement of a better treatment response in colon cancer.


Research and Markets has announced the addition of the "Antibacterial Drug Resistance: Market Landscape, Challenges and Upcoming Opportunities, 2016-2026 " report to their offering. The "Antibacterial Drug Resistance: Market Landscape, Challenges and Upcoming Opportunities, 2016-2026" report provides an extensive study of the current landscape and the growing pipeline of new generation antibiotics targeting drug-resistant bacteria. As indicated earlier, owing to the over-prescription of antibiotics due to improper diagnosis, lack of adherence to proper dosage regimens, their widespread availability as over-the-counter (OTC) drugs, and overuse in agriculture and poultry farming, most antibiotics have been rendered ineffective. Moreover, there currently exists an expanding lag between the pace at which drug resistant bacteria evolve and the time taken for new drugs to reach the market. As a result, antibiotic drug resistance has escalated into a global threat. There are concerns that the lack of effective drugs in this domain may soon trigger the relapse of the pre-antibiotic era, in which individuals died due to day-to-day bacterial infections. According to certain studies, currently, an estimated 700,000 deaths annually are known to occur due to anti-microbial resistance worldwide. In future, the growing threat of antibiotic resistance is anticipated to prove to be more fatal than cancer. The current scenario depicts an urgent need for new antibiotics with novel mechanisms of action, having the ability to combat antibiotic resistance. The US and EU governments have amended their action plans and conducted many conferences to raise awareness about the situation among both experts in the domain and the general public. Such initiatives are addressed to support R&D strategies of companies engaged in the development of drugs to combat antibiotic resistance. Efforts are underway to assist drug developers in their clinical trial design issues, and even the simplification of regulatory pathways to expedite the time to market for such drugs. In addition, such initiatives endorse public-private partnerships in advancing scientific and clinical efforts in this domain, aid the setting up of surveillance programs to track the widespread use of antibiotics and the development of resistance, and track the growing economic burden due to this phenomenon as well. The new generation antibiotics pipeline comprises of several molecules that target infections caused by deadly pathogens classified under ESKAPE or as urgent threats by the CDC. Several start-ups have entered the market and undertaken various initiatives to develop novel antibiotics with unique mechanisms of action. - An overview of the current state of the market with respect to the key players involved, phase of development of pipeline products (clinical and preclinical/discovery), target classes of pathogens (Gram-negative versus Gram-positive), drug classes and key disease indications. In addition, we have included an insightful representation of the developer landscape, highlighting the geographical presence of key players in the industry. - Detailed profiles of approved drugs, as well as those in phase III of clinical development, highlighting information on clinical trials, their current status of development, recent developments and associated collaborations. - Insights on novel alternative therapies that are being explored/evaluated to target antibiotic resistant pathogenic bacteria; these include teixobactin, anti-microbial peptides, antisense antibacterials, quorum sensing inhibition, nano-metal based therapies and anti-biofilm agents. - Details on the most popular therapeutic areas, namely acute bacterial skin and skin structure infections (ABSSSIs), community-acquired pneumonia (CAP) Clostridium difficile infections (CDIs), complicated intra-abdominal infections (cIAIs), complicated urinary tract infections (cUTIs) and hospital-acquired pneumonia/ventilator-associated pneumonia (HAP/VAP). For each indication, we have provided a brief description of the disease, information on its epidemiology, available treatment plans and active comparator studies of approved drug candidates that are prescribed for the aforementioned indications. - An illustrative grid representation and a bulls-eye analysis of the pipeline molecules, based on their development stage, spectrum of activity and the key indications. - Future commercial potential of the market based on a detailed opportunity analysis, for the period between 2016 and 2026. The research, analysis and insights presented in this report include potential sales of approved antibiotics and those in late stages of development. 1. Preface 2. Executive Summary 3. Introduction 4. Antibiotic Drug Resistance: Development Pipeline and Market Landscape 5. Clinical Development Analysis and Key Comparator Studies 6. New Generation Antibiotics: Marketed Drugs 7. New Generation Antibiotics: Phase III Drugs 8. Emerging Therapies to Combat Antibiotic Resistance 9. Key Therapeutic Areas 10. Market Forecast and Opportunity Analysis 11. Conclusion 12. Interview Transcripts 13. Appendix 1: Tabulated Data 14. Appendix 2: List of Companies and Organization - AAIPharma Services - ABAC Therapeutics - ANTABIO - Abbott Laboratories - Abgentis - Absynth Biologics - Achaogen - Acino Holdings - Actavis - Actelion Pharmaceuticals - Adenium Biotech - Adimab - Aequor - AiCuris - Alaxia Pharma - Albany Molecular Research (AMRI) - Allecra Therapeutics - Allergan - Angelini - Antibio Tx - Antibiotic Adjuvant - Aphios - Appili Therapeutics - Arietis Pharma - Arpida - Arsanis - Assembly Biosciences - AstraZeneca - Austell Laboratories - Aventis Pharma - BKG Pharma - BUGWORKS - Basilea Pharmaceutica - Bayer Pharma - BioVersys - Biocidium Biopharmaceuticals - Biocon - Biosearch Italia - Biovertis - Blueberry Therapeutics - C3 Jian - Calixa Therapeutics - Cantab Anti-infectives - Cardiome Pharma - Cellceutix Corporation - Cempra - Cerexa - Clinigen Group - ContraFect - Crestone - Crystal Genomics - Cubist Pharmaceuticals - CyDex Pharmaceuticals - DSM Sinochem Pharmaceuticals - Da Volterra - Daiichi Sankyo - Debiopharm International - Deinove - Demuris - Discuva - Dong Wha Pharmaceuticals - Dong-A Pharmaceutical - Durata Therapeutics - Eli Lilly - Eligo Bioscience - EnBiotix - Entasis Therapeutics - Eurofarma Laboratórios - Evolva Holding - Evotec - Eydo Pharma - FOB Synthesis - Fedora Pharmaceuticals - Forest Laboratories - Fujisawa Pharmaceuticals - GSK - Galapagos - GangaGen - GeneWEAVE - Hikma Pharmaceuticals - IASO Pharma - iNtRON Biotechnology - Immuron - Indel Therapeutics - Institute of Metagenomics and Microbial Technologies (IMMT) - InterMune - Ionis Pharmaceuticals - Isis Pharmaceuticals - Janssen-Ortho - Japan Radio Company - Johnson & Johnson - Kyorin Pharmaceutical - LegoChem Biosciences - Ligand Pharmaceuticals - Lyndra - MGB Biopharma - Macrolide Pharmaceuticals - MarBiLeads - Matinas BioPharma - MedImmune - Meiji Seika Pharma - Melinta Therapeutics - MerLion Pharmaceuticals - Merck - MethylGene - Microbecide - MicuRx Pharmaceuticals - Mirati Therapeutics - Monash University - MorphoSys - Morphochem - Motif Bio - Mutabilis - Nabriva Therapeutics - Naicon - NanoSafe Coatings - Nanotherapeutics - Navigen Pharmaceuticals - Nemesis Bioscience - Nexgen Biosciences - Nobelex Biotech - Northeastern University - Northern Antibiotics - Nosopharm - NovaBiotics - NovaDigm Therapeutics - Novexel - NovoBiotic Pharmaceuticals - Nuprim - OJ-Bio - Optimer Biotechnology - Optimer Pharmaceuticals - Osel - PENDOPHARM - Pacific Beach BioSciences - Par Pharmaceutical - Paratek Pharmaceuticals - Patheon - Peninsula Pharmaceuticals - Peptilogics - Pfizer - Pherecydes Pharma - Phico Therapeutics - Polyphor - Procarta Biosystems - Pure Actives - R-Pharm - RQx Pharmaceuticals - RaQualia Pharma - Rebiotix - Redx Pharma - Rempex Pharmaceuticals - RexC Pharmaceuticals - Rib-X Pharmaceuticals - Roche - Rx3 Pharmaceuticals - Sanofi-Aventis - SciClone Pharmaceuticals - Sequella - Seres Therapeutics - SetLance - Shionogi - Shire - SinSa Labs - Specialised Therapeutics Australia - Spero Therapeutics - Sumitomo Dainippon Pharma (DSP) - Summit Therapeutics - Synamp Pharmaceuticals - Synthetic Biologics - TAXIS Pharmaceuticals - TaiGen Biotechnology - Takeda Pharmaceutical - Talon Pharmaceuticals - Targanta Therapeutics - TechnoPhage - Techulon - Tetraphase Pharmaceuticals - The Medicines Company - TheraBor Pharmaceuticals - Theravance Biopharma - Treat Systems - Trius Therapeutics - University of Michigan Life Sciences Institute - University of Pittsburgh - Vaxdyn - VenatoRx Pharmaceuticals - Versicor Pharmaceuticals - VibioSphen - Vicuron Pharmaceuticals - ViroPharma - Vitas Pharma - Vyome Biosciences - Wakunaga Pharmaceutical - Warner Chillcott - Wockhardt - Yamanouchi Pharmaceutical - Zavante Therapeutics For more information about this report visit http://www.researchandmarkets.com/research/gqv9bz/antibacterial


Dublin, Dec. 15, 2016 (GLOBE NEWSWIRE) -- Research and Markets has announced the addition of the "Antibacterial Drug Resistance: Market Landscape, Challenges and Upcoming Opportunities, 2016-2026 " report to their offering. The "Antibacterial Drug Resistance: Market Landscape, Challenges and Upcoming Opportunities, 2016-2026" report provides an extensive study of the current landscape and the growing pipeline of new generation antibiotics targeting drug-resistant bacteria. As indicated earlier, owing to the over-prescription of antibiotics due to improper diagnosis, lack of adherence to proper dosage regimens, their widespread availability as over-the-counter (OTC) drugs, and overuse in agriculture and poultry farming, most antibiotics have been rendered ineffective. Moreover, there currently exists an expanding lag between the pace at which drug resistant bacteria evolve and the time taken for new drugs to reach the market. As a result, antibiotic drug resistance has escalated into a global threat. There are concerns that the lack of effective drugs in this domain may soon trigger the relapse of the pre-antibiotic era, in which individuals died due to day-to-day bacterial infections. According to certain studies, currently, an estimated 700,000 deaths annually are known to occur due to anti-microbial resistance worldwide. In future, the growing threat of antibiotic resistance is anticipated to prove to be more fatal than cancer. The current scenario depicts an urgent need for new antibiotics with novel mechanisms of action, having the ability to combat antibiotic resistance. The US and EU governments have amended their action plans and conducted many conferences to raise awareness about the situation among both experts in the domain and the general public. Such initiatives are addressed to support R&D strategies of companies engaged in the development of drugs to combat antibiotic resistance. Efforts are underway to assist drug developers in their clinical trial design issues, and even the simplification of regulatory pathways to expedite the time to market for such drugs. In addition, such initiatives endorse public-private partnerships in advancing scientific and clinical efforts in this domain, aid the setting up of surveillance programs to track the widespread use of antibiotics and the development of resistance, and track the growing economic burden due to this phenomenon as well. The new generation antibiotics pipeline comprises of several molecules that target infections caused by deadly pathogens classified under ESKAPE or as urgent threats by the CDC. Several start-ups have entered the market and undertaken various initiatives to develop novel antibiotics with unique mechanisms of action. The report features: - An overview of the current state of the market with respect to the key players involved, phase of development of pipeline products (clinical and preclinical/discovery), target classes of pathogens (Gram-negative versus Gram-positive), drug classes and key disease indications. In addition, we have included an insightful representation of the developer landscape, highlighting the geographical presence of key players in the industry. - Detailed profiles of approved drugs, as well as those in phase III of clinical development, highlighting information on clinical trials, their current status of development, recent developments and associated collaborations. - Insights on novel alternative therapies that are being explored/evaluated to target antibiotic resistant pathogenic bacteria; these include teixobactin, anti-microbial peptides, antisense antibacterials, quorum sensing inhibition, nano-metal based therapies and anti-biofilm agents. - Details on the most popular therapeutic areas, namely acute bacterial skin and skin structure infections (ABSSSIs), community-acquired pneumonia (CAP) Clostridium difficile infections (CDIs), complicated intra-abdominal infections (cIAIs), complicated urinary tract infections (cUTIs) and hospital-acquired pneumonia/ventilator-associated pneumonia (HAP/VAP). For each indication, we have provided a brief description of the disease, information on its epidemiology, available treatment plans and active comparator studies of approved drug candidates that are prescribed for the aforementioned indications. - An illustrative grid representation and a bulls-eye analysis of the pipeline molecules, based on their development stage, spectrum of activity and the key indications. - Future commercial potential of the market based on a detailed opportunity analysis, for the period between 2016 and 2026. The research, analysis and insights presented in this report include potential sales of approved antibiotics and those in late stages of development. Key Topics Covered: 1. Preface 2. Executive Summary 3. Introduction 4. Antibiotic Drug Resistance: Development Pipeline and Market Landscape 5. Clinical Development Analysis and Key Comparator Studies 6. New Generation Antibiotics: Marketed Drugs 7. New Generation Antibiotics: Phase III Drugs 8. Emerging Therapies to Combat Antibiotic Resistance 9. Key Therapeutic Areas 10. Market Forecast and Opportunity Analysis 11. Conclusion 12. Interview Transcripts 13. Appendix 1: Tabulated Data 14. Appendix 2: List of Companies and Organization - AAIPharma Services - ABAC Therapeutics - ANTABIO - Abbott Laboratories - Abgentis - Absynth Biologics - Achaogen - Acino Holdings - Actavis - Actelion Pharmaceuticals - Adenium Biotech - Adimab - Aequor - AiCuris - Alaxia Pharma - Albany Molecular Research (AMRI) - Allecra Therapeutics - Allergan - Angelini - Antibio Tx - Antibiotic Adjuvant - Aphios - Appili Therapeutics - Arietis Pharma - Arpida - Arsanis - Assembly Biosciences - AstraZeneca - Austell Laboratories - Aventis Pharma - BKG Pharma - BUGWORKS - Basilea Pharmaceutica - Bayer Pharma - BioVersys - Biocidium Biopharmaceuticals - Biocon - Biosearch Italia - Biovertis - Blueberry Therapeutics - C3 Jian - Calixa Therapeutics - Cantab Anti-infectives - Cardiome Pharma - Cellceutix Corporation - Cempra - Cerexa - Clinigen Group - ContraFect - Crestone - Crystal Genomics - Cubist Pharmaceuticals - CyDex Pharmaceuticals - DSM Sinochem Pharmaceuticals - Da Volterra - Daiichi Sankyo - Debiopharm International - Deinove - Demuris - Discuva - Dong Wha Pharmaceuticals - Dong-A Pharmaceutical - Durata Therapeutics - Eli Lilly - Eligo Bioscience - EnBiotix - Entasis Therapeutics - Eurofarma Laboratórios - Evolva Holding - Evotec - Eydo Pharma - FOB Synthesis - Fedora Pharmaceuticals - Forest Laboratories - Fujisawa Pharmaceuticals - GSK - Galapagos - GangaGen - GeneWEAVE - Hikma Pharmaceuticals - IASO Pharma - iNtRON Biotechnology - Immuron - Indel Therapeutics - Institute of Metagenomics and Microbial Technologies (IMMT) - InterMune - Ionis Pharmaceuticals - Isis Pharmaceuticals - Janssen-Ortho - Japan Radio Company - Johnson & Johnson - Kyorin Pharmaceutical - LegoChem Biosciences - Ligand Pharmaceuticals - Lyndra - MGB Biopharma - Macrolide Pharmaceuticals - MarBiLeads - Matinas BioPharma - MedImmune - Meiji Seika Pharma - Melinta Therapeutics - MerLion Pharmaceuticals - Merck - MethylGene - Microbecide - MicuRx Pharmaceuticals - Mirati Therapeutics - Monash University - MorphoSys - Morphochem - Motif Bio - Mutabilis - Nabriva Therapeutics - Naicon - NanoSafe Coatings - Nanotherapeutics - Navigen Pharmaceuticals - Nemesis Bioscience - Nexgen Biosciences - Nobelex Biotech - Northeastern University - Northern Antibiotics - Nosopharm - NovaBiotics - NovaDigm Therapeutics - Novexel - NovoBiotic Pharmaceuticals - Nuprim - OJ-Bio - Optimer Biotechnology - Optimer Pharmaceuticals - Osel - PENDOPHARM - Pacific Beach BioSciences - Par Pharmaceutical - Paratek Pharmaceuticals - Patheon - Peninsula Pharmaceuticals - Peptilogics - Pfizer - Pherecydes Pharma - Phico Therapeutics - Polyphor - Procarta Biosystems - Pure Actives - R-Pharm - RQx Pharmaceuticals - RaQualia Pharma - Rebiotix - Redx Pharma - Rempex Pharmaceuticals - RexC Pharmaceuticals - Rib-X Pharmaceuticals - Roche - Rx3 Pharmaceuticals - Sanofi-Aventis - SciClone Pharmaceuticals - Sequella - Seres Therapeutics - SetLance - Shionogi - Shire - SinSa Labs - Specialised Therapeutics Australia - Spero Therapeutics - Sumitomo Dainippon Pharma (DSP) - Summit Therapeutics - Synamp Pharmaceuticals - Synthetic Biologics - TAXIS Pharmaceuticals - TaiGen Biotechnology - Takeda Pharmaceutical - Talon Pharmaceuticals - Targanta Therapeutics - TechnoPhage - Techulon - Tetraphase Pharmaceuticals - The Medicines Company - TheraBor Pharmaceuticals - Theravance Biopharma - Treat Systems - Trius Therapeutics - University of Michigan Life Sciences Institute - University of Pittsburgh - Vaxdyn - VenatoRx Pharmaceuticals - Versicor Pharmaceuticals - VibioSphen - Vicuron Pharmaceuticals - ViroPharma - Vitas Pharma - Vyome Biosciences - Wakunaga Pharmaceutical - Warner Chillcott - Wockhardt - Yamanouchi Pharmaceutical - Zavante Therapeutics For more information about this report visit http://www.researchandmarkets.com/research/gtt9s3/antibacterial


Jeong H.W.,Seoul National University | Lee J.-W.,Seoul National University | Kim W.S.,Seoul National University | Choe S.S.,Seoul National University | And 15 more authors.
Molecular Pharmacology | Year: 2010

Activation of peroxisome proliferator-activated receptors (PPARs) have been implicated in the treatment of metabolic disorders with different mechanisms; PPARα agonists promote fatty acid oxidation and reduce hyperlipidemia, whereas PPARγ agonists regulate lipid redistribution from visceral fat to subcutaneous fat and enhance insulin sensitivity. To achieve combined benefits from activated PPARs on lipid metabolism and insulin sensitivity, a number of PPARα/γ dual agonists have been developed. However, several adverse effects such as weight gain and organ failure of PPARα/γ dual agonists have been reported. By use of virtual ligand screening, we identified and characterized a novel PPARα/γ dual agonist, (R)-1-(4-(2-(5- methyl-2-p-tolyloxazol-4-yl)ethoxy)benzyl)piperidine-2-carboxylic acid (CG301360), exhibiting the improvement in insulin sensitivity and lipid metabolism. CG301360 selectively stimulated transcriptional activities of PPARα and PPARγ and induced expression of their target genes in a PPARα- and PPARγ-dependent manner. In cultured cells, CG301360 enhanced fatty acid oxidation and glucose uptake and it reduced pro-inflammatory gene expression. In db/db mice, CG301360 also restored insulin sensitivity and lipid homeostasis. Collectively, these data suggest that CG301360 would be a novel PPARα/γagonist, which might be a potential lead compound to develop against insulin resistance and hyperlipidemia. Copyright © 2010 The American Society for Pharmacology and Experimental Therapeutics.


Jeong H.W.,Seoul National University | Lee J.-W.,Seoul National University | Kim W.S.,Seoul National University | Choe S.S.,Seoul National University | And 15 more authors.
Diabetes | Year: 2011

OBJECTIVE - Peroxisome proliferator-activated receptor (PPAR)-α/ γ dual agonists have been developed to alleviate metabolic disorders. However, several PPARα/γ dual agonists are accompanied with unwanted side effects, including body weight gain, edema, and tissue failure. This study investigated the effects of a novel PPARα/γ dual agonist, CG301269, on metabolic disorders both in vitro and in vivo. RESEARCH DESIGN AND METHODS - Function of CG301269 as a PPARα/γ dual agonist was assessed in vitro by luciferase reporter assay, mammalian one-hybrid assay, and analyses of PPAR target genes. In vitro profiles on fatty acid oxidation and inflammatory responses were acquired by fatty acid oxidation assay and quantitative (q)RT-PCR of proinflammatory genes. In vivo effect of CG301269 was examined in db/db mice. Total body weight and various tissue weights were measured, and hepatic lipid profiles were analyzed. Systemic glucose and insulin tolerance were measured, and the in vivo effect of CG301269 on metabolic genes and proinflammatory genes was examined by qRT-PCR. RESULTS - CG301269 selectively stimulated the transcriptional activities of PPARα and PPARγ. CG301269 enhanced fatty acid oxidation in vitro and ameliorated insulin resistance and hyperlipidemia in vivo. In db/db mice, CG301269 reduced inflammatory responses and fatty liver, without body weight gain. CONCLUSIONS - We demonstrate that CG301269 exhibits beneficial effects on glucose and lipid metabolism by simultaneous activation of both PPARα and PPARγ. Our data suggest that CG301269 would be a potential lead compound against obesity and related metabolic disorders. © 2011 by the American Diabetes Association.

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