Abstract:
:A wide range of peptides and polypeptides can be appended to either the N- or C-terminus of G protein-coupled receptors without disrupting substantially ligand binding and signal transduction. Following fusion of fluorescent proteins, reporter gene constructs or G protein alpha subunits to the C-terminal tail of a receptor high content and G protein activation assays can be employed to identify agonist ligands. Further modification of the receptor fusions to introduce enhanced levels of constitutive activity and to physically destabilise the protein allows antagonist/inverse agonists screens to be developed in parallel. Equivalent C-terminal addition of pairs of complementary, non-functional, polypeptide fragments allows the application of enzyme complementation techniques. Introduction of N-terminal tags to receptors has also allowed the introduction of novel assay techniques based on a pH-sensitive cyanine dye. These have the capacity to overcome certain limitations of GPCR-fluorescent protein fusions.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Milligan G,Feng GJ,Ward RJ,Sartania N,Ramsay D,McLean AJ,Carrillo JJdoi
10.2174/1381612043384295subject
Has Abstractpub_date
2004-01-01 00:00:00pages
1989-2001issue
17eissn
1381-6128issn
1873-4286journal_volume
10pub_type
杂志文章,评审abstract::Marine fungi with their successful pharmacological effects were considered to be the treasure of ocean medicines concerning the striking ability of their secondary metabolites. Literature over literature has been published on fungi derived bioactive molecules to probe its therapeutic potential. Marine fungi have an im...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666200728142244
更新日期:2020-07-28 00:00:00
abstract::Repurposing already approved drugs as new anticancer agents is a promising strategy considering the advantages such as low costs, low risks and less time-consumption. Disulfiram (DSF), as the first drug for antialcoholism, was approved by the U.S. Food and Drug Administration (FDA) over 60 years ago. Increasing eviden...
journal_title:Current pharmaceutical design
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doi:10.2174/1381612825666190816233755
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209787846784
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161208799316401
更新日期:2008-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612811319230008
更新日期:2013-01-01 00:00:00
abstract:BACKGROUND:Psoriasis is an autoimmune disease of the skin with lapsing episodes of hyperkeratosis, irritation and inflammation. Numerous methodologies and utilization of different antipsoriatic drugs with various activity methods and routes of administration have been investigated to treat this terrifying sickness. In ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612824666181102151507
更新日期:2018-01-01 00:00:00
abstract:: ...
journal_title:Current pharmaceutical design
pub_type: 社论
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abstract::Clopidogrel, in combination wih aspirin, is currently the drug of choice to prevent thrombosis after coronary stent implantation. Currently, clopidogrel is administered to the vast majority of patients without any assessment of platelet inhibition. Response variability and resistance, however, definitely occur to clop...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2006-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612823666170215144649
更新日期:2017-01-01 00:00:00
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journal_title:Current pharmaceutical design
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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abstract:BACKGROUND AND OBJECTIVES:The 3' repair exonuclease 1 (TREX1) gene is the major DNA-specific 3'-5 'exonuclease of mammalian cells which reduces single- and double-stranded DNA (ssDNA and dsDNA) to prevent undue immune activation mediated by the nucleic acid. TREX1 is also a crucial suppressor of selfrecognition that pr...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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abstract::Since the 1950's, herpes simplex viruses (HSV) have played prominent roles in the development of antivirals. The first efficacious antivirals, as well as the first safe for systemic use, were developed against HSV. It was only in 1995 when the first antiviral against a target not validated first with HSV was approved ...
journal_title:Current pharmaceutical design
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abstract::Ras is a 21 kDa membrane-localized G protein that is coupled to receptor and non-receptor tyrosine kinase activation of downstream cytoplasmic and nuclear events. Mutated ras genes are common, and occur in a wide variety of human malignancies. These activating mutations result in constitutive signaling, thereby stimul...
journal_title:Current pharmaceutical design
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abstract:BACKGROUND:R. Schofield (1978) proposed a hypothesis of hematopoietic stem cells (HSCs) niche (specialized cell microenvironment). An existence of osteoblastic and vascular niches for HSCs has been postulated since 2003. At the same time, the discussion about the existence and functioning of niche for multipotent mesen...
journal_title:Current pharmaceutical design
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abstract::Topiramate is one of the currently most promising compounds in the field of addiction medicine. This paper discusses its potential utility related to a phase model of addiction development, focusing on the assumption that addiction is a continuous process involving different neurobiological pathways, depending on the ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/138161211796150864
更新日期:2011-01-01 00:00:00
abstract::There is a plausible role for cytokines, brain-derived neurotrophic factor (BDNF), and their interaction in major depressive disorder's (MDD) etiology. This review includes (i) briefly defining cytokines, (ii) a discussion of theories for why they may affect brain function, (iii) cross-sectional associations between c...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161212803523680
更新日期:2012-01-01 00:00:00
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journal_title:Current pharmaceutical design
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abstract::G-quadruplexes have found increasing potential in applications such as molecular therapeutics, diagnostics, and sensing. As a consequence, small molecules capable of selectively detecting G-quadruplexes have received significant attention in recent literature. Our review here addresses representative advances in the d...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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journal_title:Current pharmaceutical design
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journal_title:Current pharmaceutical design
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2011-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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journal_title:Current pharmaceutical design
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更新日期:2020-02-12 00:00:00
abstract::A recent meta-analysis showed that the mean age of onset of psychosis among cannabis users was almost three years earlier than that of non-cannabis users. However, because cannabis users usually smoke tobacco, the use of tobacco might independently contribute to the earlier onset of psychosis. We aimed to use meta-ana...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,meta分析
doi:10.2174/138161212802884816
更新日期:2012-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2009-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2018-01-01 00:00:00