Abstract:
:Kit is a growth factor receptor of the type III tyrosine kinase family, whose gain-of-function mutations have been identified as driving causes of different kinds of tumours. It thus represents a viable drug target, and the development of Kit inhibitors has been shown to be a promising therapeutic concept. This review will focus on structural and signalling properties of both wild-type and mutant Kit, as well as its role in the development of human cancers. Special attention will be dedicated to gastrointestinal stromal tumours, GISTs. Progress in research on the aetiopathogenesis of GISTs and their therapeutic approaches will be fully discussed, focusing on the latest tendencies for the treatment of these kinds of tumours.
journal_name
Curr Med Chemjournal_title
Current medicinal chemistryauthors
Sartini S,Dario B,Morelli M,Da Settimo F,La Motta Cdoi
10.2174/092986711796150504subject
Has Abstractpub_date
2011-01-01 00:00:00pages
2893-903issue
19eissn
0929-8673issn
1875-533Xpii
BSP/CMC/E-Pub/2011/ 212journal_volume
18pub_type
杂志文章,评审abstract::Serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists. Among 5-HTRs, the 5-HT(1A) subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind...
journal_title:Current medicinal chemistry
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journal_title:Current medicinal chemistry
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journal_title:Current medicinal chemistry
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更新日期:2012-01-01 00:00:00
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journal_title:Current medicinal chemistry
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journal_title:Current medicinal chemistry
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journal_title:Current medicinal chemistry
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更新日期:2014-01-01 00:00:00
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journal_title:Current medicinal chemistry
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更新日期:2015-05-04 00:00:00
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journal_title:Current medicinal chemistry
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更新日期:2009-01-01 00:00:00
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journal_title:Current medicinal chemistry
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更新日期:2007-01-01 00:00:00
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journal_title:Current medicinal chemistry
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更新日期:2005-01-01 00:00:00
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journal_title:Current medicinal chemistry
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abstract::Since the discovery of penicillin, natural and synthetic β-lactams have aroused great interest not only as sources of effective antibacterial agents but also as specific inhibitors of proteases responsible for various non-bacterial pathological processes. This interest was reflected in our review published in Current ...
journal_title:Current medicinal chemistry
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abstract::β-Aryl-β-amino acids constitute very useful scaffolds able to lead, via various intra-molecular cyclisation reactions, to a great diversity of cyclic derivatives with numerous biological and therapeutic properties. The present article aims at reporting an exhaustive overview of these ring-closure sequences and their a...
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更新日期:2010-01-01 00:00:00
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journal_title:Current medicinal chemistry
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更新日期:2004-07-01 00:00:00
abstract::COX-2, a key enzyme that catalyzed the rate-limiting steps in the conversion of arachidonic acid to prostaglandins, played a pivotal role in inflammatory process. Different from other family members, COX-2 was barely detectable in normal physiological conditions and highly inducible during acute inflammatory response ...
journal_title:Current medicinal chemistry
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更新日期:2020-09-17 00:00:00
abstract::With the increasing production of engineered nanomaterials (ENMs) exploited in many consumer products, a wider number of people is expected to be exposed to such materials in the near future, both in occupational and environmental settings. This has raised concerns about the possible implications on public health. In ...
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更新日期:2012-01-01 00:00:00
abstract:: ...
journal_title:Current medicinal chemistry
pub_type: 社论
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abstract::Protein-ligand docking is currently an important tool in drug discovery efforts and an active area of research that has been the subject of important developments over the last decade. These are well portrayed in the rising number of available protein-ligand docking software programs, increasing level of sophisticatio...
journal_title:Current medicinal chemistry
pub_type: 历史文章,杂志文章,评审
doi:10.2174/0929867311320180002
更新日期:2013-01-01 00:00:00
abstract::Radical induced oxidative damage is extremely harmful to tissues and organs due to molecular modifications brought to polyunsaturated membrane lipids, proteins and nucleic acids. Oxidative stress is believed to be one of the pathophysiological mechanisms that operate in neurodegenerative disorders such as cerebral isc...
journal_title:Current medicinal chemistry
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abstract:BACKGROUND:Research on Chromogranin A (CGA) and its derived fragments convincingly demonstrated the multifunctional activity of the 21 amino acid peptide named Catestatin (CST: human CGA352-372, bovine CGA344-364, rat CGA367-387). This review aims to provide a synopsis of the current information concerning the biologic...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2017-01-01 00:00:00
abstract::In recent years there has been a growing interest in computer-based screening. One of the driving forces has been the increased efficiency of protein crystallography leading to the real possibility of using structure-based design as a significant contributor to the discovery of novel ligands. In 1957 after 22 years of...
journal_title:Current medicinal chemistry
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更新日期:2003-05-01 00:00:00