Listing 1 - 10 of 539 | << page >> |
Sort by
|
Choose an application
Lipogenesis (de novo fatty acid synthesis) is one of the metabolic changes needed for tumor evolution. This occurs in the major part à cancer cells. In those cells, some of the lipogenic enzyme are overexpressed. In this work, we focus on FAS: fatty acid synthase. FAS (multifunctional enzyme) is an oncogene, catalyzing fatty acid biosynthesis in the cytoplasm. When FAS is overexpressed, cancer prognostic is poor. It was observed for example for breast or prostatic cancer. That’s why inhibition (by pharmacological agents or genetic) appears as a new target therapy for establishment of antitmoral therapy. Consequently, apoptosis in cancer cells in induced and can be observed in vitro and in vivo. As far as we know, pharmalogical inhibitors of FAS have all that they could stop tumoral cell proliferation, cause their death (by apoptosis) and avoid tumoral growth. Normal cells, don’t suffer of the FAS inhibitors effects, because FAS isn’t’ overexpressed there. Among the know inhibitors of FAS, we can notice: cerulenin (poorly specific of lipogenesis), C75 (a derived compound from cerulenin, more specific, but inducing a loss of weight) and orlistat (medicine used for obesity treatment, that seems to be more specific). They are different by their inhibition mechanism and by their binding site. All of them proved their antitumoral potential despite their differences. Further researchers should be helpful which catalytic domain may be the most promising target for drug development based on FAS inhibition (chemotherapy as welle as chemoprevention). L’augmentation de la lipogenèse (ou synthèse d’acides gras de novo) fait partie des adaptations métaboliques indispensables à la croissance et à la survie tumorale. Ce renforcement de la lipogenèse est une caractéristique commune à de nombreuses cellules cancéreuses, mis en évidence par une augmentation élevée de l’expression des enzymes lipogéniques telles que le fatty acid synthase (FAS). Cette enzyme multifonctionnelle, constituant un oncogène, catalyse la biosynthèse des acides gras à longue chaîne dans le cytoplasme. Surexprimée dans la majorité des cancers et à un stade précoce pour certains d’entre eux ; elle annonce un mauvais pronostic notamment dans les cancers du sein et de la prostate. Ainsi, FAS apparaît comme une nouvelle cible de choix pour le développement de traitements antitumoraux. L’inhibition de FAS par des agents pharmacologiques ou par des moyens génétiques représente donc un réel intérêt. La synthèse d’acides gras de novo est essentielle à la progression tumorale, c’est pourquoi l’inhibition de la lipogenèse ciblant FAS entraîne l’apoptose sélective des cellules cancéreuses aussi bien in vitro qu’in vivo. Les inhibiteurs pharmacologiques de FAS identifiés jusqu’à maintenant, ont montré qu’ils pouvaient bloquer la prolifération des cellules tumorales, susciter leur mort et empêcher la croissance de la tumeur. Cet effet est minimisé chez les cellules saines puisque FAS n’y est pas surexprimée. Parmi les inhibiteurs de FAS connus, on réactive de la cérulénine (inhibiteur peu spécifique de la lipogenèse), C75 (forme moins réactive de la céruléline, plu spécifique, mais qui provoque une perte de poids) et l’orlistat (médicament utilisé dans le traitement de l’obésité, qui inhibe le domaine thioestérase de FAS et semble plus spécifique). Ils différent d’une part leur mécanisme d’inhibition, et d’autre part par le domaine catalytique qu’ils ciblent. Tous ont prouvé leur efficacité à induire des effets antitumoraux malgré ces différences. La poursuite des recherches devrait permettre de déterminer quel domaine catalytique de FAS constitue al cible la plus prometteuse pour le développement d’un médicament de chimioprévention anticancéreuse qui inhibe FAS.
Fatty Acid Synthetase Complex --- Lipogenesis --- Neoplasms --- Pharmacologic Actions
Choose an application
Drugs --- Drugs --- Drug Design --- Pharmacologic Actions --- Design --- Structure-activity relationships
Choose an application
Pharmacology. Therapy --- Pharmacologic Actions --- Drug Therapy --- Pharmacology. --- Physiology, Pathological. --- Chemotherapy --- Pharmacologie --- Physiopathologie --- Chimiothérapie --- Chimiothérapie --- Pharmacologic Actions. --- Drug Therapy.
Choose an application
Geneesmiddelen --- Médicaments --- Drug Therapy. --- farmacologie --- geneesmiddelen --- toxicologie --- Therapy, Drug --- Chemotherapy --- Pharmacotherapy --- Chemotherapies --- Drug Therapies --- Pharmacotherapies --- Therapies, Drug --- Disease --- Pharmaceutical Preparations --- Pharmacologic Actions --- drug therapy --- therapeutic use --- Drug Therapy
Choose an application
Drug therapy --- Drug Therapy. --- Therapy, Drug --- Chemotherapy --- Pharmacotherapy --- Chemotherapies --- Drug Therapies --- Pharmacotherapies --- Therapies, Drug --- Disease --- Pharmaceutical Preparations --- Pharmacologic Actions --- drug therapy --- therapeutic use --- Drug therapy. --- Drug Therapy
Choose an application
Drug Therapy. --- Therapy, Drug --- Chemotherapy --- Pharmacotherapy --- Chemotherapies --- Drug Therapies --- Pharmacotherapies --- Therapies, Drug --- Disease --- Pharmaceutical Preparations --- Pharmacologic Actions --- drug therapy --- therapeutic use --- Drug Therapy
Choose an application
Chemotherapy --- Drug Therapy. --- Chemotherapy. --- Drug therapy --- Pharmacotherapy --- Therapeutics --- Drugs --- Pharmacology --- Therapy, Drug --- Chemotherapies --- Drug Therapies --- Pharmacotherapies --- Therapies, Drug --- Disease --- Pharmaceutical Preparations --- Pharmacologic Actions --- drug therapy --- therapeutic use
Choose an application
Pharmacology, Clinical --- Drug Therapy --- Therapy, Drug --- Chemotherapy --- Pharmacotherapy --- Chemotherapies --- Drug Therapies --- Pharmacotherapies --- Therapies, Drug --- Disease --- Pharmaceutical Preparations --- Pharmacologic Actions --- Clinical Pharmacology --- drug therapy --- therapeutic use
Choose an application
Drug Therapy. --- Therapy, Drug --- Chemotherapy --- Pharmacotherapy --- Chemotherapies --- Drug Therapies --- Pharmacotherapies --- Therapies, Drug --- Disease --- Pharmaceutical Preparations --- Pharmacologic Actions --- drug therapy --- therapeutic use --- Periodicals --- Drug Therapy
Choose an application
Articles that further knowledge and advance the science and application of antimicrobial chemotherapy with antibiotics and antifungal, antiviral and antiprotozoal agents primarily in human medicine.
Chemotherapy --- Drug Therapy. --- Chemotherapy. --- Drug therapy --- Pharmacotherapy --- Therapy, Drug --- Chemotherapies --- Drug Therapies --- Pharmacotherapies --- Therapies, Drug --- Disease --- Pharmaceutical Preparations --- drug therapy --- therapeutic use --- Therapeutics --- Drugs --- Pharmacology --- Pharmacologic Actions
Listing 1 - 10 of 539 | << page >> |
Sort by
|