Search Results - "Fogliatto, Gianpaolo"
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WaterLOGSY as a method for primary NMR screening: practical aspects and range of applicability
Published in Journal of biomolecular NMR (01-12-2001)“…WaterLOGSY represents a powerful method for primary NMR screening in the identification of compounds interacting with macromolecules, including proteins and…”
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3-Aminopyrazole Inhibitors of CDK2/Cyclin A as Antitumor Agents. 1. Lead Finding
Published in Journal of medicinal chemistry (17-06-2004)“…Abnormal proliferation mediated by disruption of the normal cell cycle mechanisms is a hallmark of virtually all cancer cells. Compounds targeting complexes…”
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Crystal Structures of Anaplastic Lymphoma Kinase in Complex with ATP Competitive Inhibitors
Published in Biochemistry (Easton) (17-08-2010)“…Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase involved in the development of several human cancers and, as a result, is a recognized target…”
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Effective immuno-targeting of the IDH1 mutation R132H in a murine model of intracranial glioma
Published in Acta neuropathologica communications (21-01-2015)“…The R132H mutation of cytosolic isocitrate dehydrogenase (IDH1) is present in the majority of low grade gliomas.Immunotherapy in these tumors has an…”
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Establish an automated flow injection ESI-MS method for the screening of fragment based libraries: Application to Hsp90
Published in European journal of pharmaceutical sciences (30-08-2015)“…[Display omitted] ESI-MS is a well established technique for the study of biopolymers (nucleic acids, proteins) and their non covalent adducts, due to its…”
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Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors
Published in Bioorganic & medicinal chemistry (01-08-2014)“…[Display omitted] In the last decade the heat shock protein 90 (Hsp90) has emerged as a major therapeutic target and many efforts have been dedicated to the…”
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Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases
Published in Bioorganic & medicinal chemistry (01-12-2013)“…A novel series of PIM inhibitors was derived from a combined effort in natural product-inspired library generation and screening. The novel…”
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Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90)
Published in Bioorganic & medicinal chemistry (15-11-2013)“…Fragment based approach and subsequent optimization of the fragment 1 led to the identification of the heat shock protein 90 (Hsp90) inhibitor 18 (NMS-E973),…”
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NMS-E973, a Novel Synthetic Inhibitor of Hsp90 with Activity against Multiple Models of Drug Resistance to Targeted Agents, Including Intracranial Metastases
Published in Clinical cancer research (01-07-2013)“…Recent developments of second generation Hsp90 inhibitors suggested a potential for development of this class of molecules also in tumors that have become…”
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Abstract A213: Potent anticancer activity in vitro and in vivo by NMS-E973, a novel synthetic inhibitor of HSP90
Published in Molecular cancer therapeutics (10-12-2009)“…Abstract The molecular chaperone heat shock protein 90 (HSP90) is essential for the conformational maturation and stability of a variety of proteins, including…”
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3-aminopyrazole inhibitors of CDK/cyclin A as antitumor agents. 1. Lead finding
Published in Journal of medicinal chemistry (2004)Get full text
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CORRECTION OF DYSLIPOPROTEINAEMIA OF CASEIN-FED RABBIT BY FCE 27677, A POTENT NOVEL ACAT INHIBITOR
Published in Pharmacological research (01-03-1996)“…Rabbits fed a wheat starch casein diet develop hypercholesterolaemia characterized by the plasma elevation of low density lipoprotein (LDL) that is caused by…”
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Oxidized lipoproteins induce long-lasting inhibition of nitric oxide synthase from a murine endothelioma cell line (bEnd.4)
Published in Journal of cardiovascular risk (01-04-1995)“…The vascular endothelium produces nitric oxide, which has vasodilatory properties. It has been postulated that some lipoproteins may increase arterial vascular…”
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