Abstract：
:The affinity of a drug candidate for a biological membrane (its lipophilicity) is closely related to the pharmacologically crucial events of absorption, biodistribution, metabolization and excretion. The evolution of knowledge of biological membranes during the past two decades contrasts with the rudimentary parameter most commonly used to assess lipophilicity: P(o/w), the octanol-water partition coefficient. P(o/w) is especially unrealistic when testing molecules that are polar or partially charged. By contrast, lipid vesicle-based methods determine the extent of the actual partition of a drug to a membrane much more accurately, and have the additional advantage of enabling the choice of the lipid composition considered most suitable to answer a specific biological or pharmaceutical question. In addition, some of these methods are appropriate for high throughput screening, thus shifting determinations of membrane partition to a more preliminary stage of drug development. This streamlines research and development, by saving the time and money that would be spent on unpromising leads.
journal_name
Trends Pharmacol Scijournal_title
Trends in pharmacological sciencesauthors
Ribeiro MM,Melo MN,Serrano ID,Santos NC,Castanho MAdoi
10.1016/j.tips.2010.06.007subject
Has Abstractpub_date
2010-10-01 00:00:00pages
449-54issue
10eissn
0165-6147issn
1873-3735pii
S0165-6147(10)00118-5journal_volume
31pub_type
历史文章,杂志文章abstract：:Adenosine, when given by inhalation, initiates the narrowing of airways in subjects with asthma or chronic obstructive pulmonary disease (COPD). The underlying mechanism of this narrowing appears to involve the stimulation of specific mast cell surface adenosine receptors with the subsequent release of mediators and c...
journal_title：Trends in pharmacological sciences
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abstract：:Bioluminescence resonance energy transfer has developed in recent years as a new technique to study protein-protein interactions. Protein partners of interest are tagged with either luciferase or green fluorescent protein (GFP). Non-radiative energy transfer between the excited luciferase and the GFP permits the study...
journal_title：Trends in pharmacological sciences
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abstract：:Hedgehog (Hh) signaling has emerged in recent years as an attractive target for anticancer therapy because its aberrant activation is implicated in several cancers. Major progress has been made in the development of SMOOTHENED (SMO) antagonists, although they have shown several limitations due to downstream SMO pathwa...
journal_title：Trends in pharmacological sciences
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abstract：:The GPR119 receptor is expressed predominantly in pancreatic β cells and in enteroendocrine cells. It is a major target for the development of anti-diabetic drugs that through GPR119 activation may stimulate both insulin and GLP-1 release. GPR119 can be activated by oleoylethanolamide and several other endogenous lipi...
journal_title：Trends in pharmacological sciences
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abstract：:Changes in the structure and function of the small airways (<2mm diameter) are now recognized to play a major role in airflow limitation in both chronic obstructive pulmonary disease (COPD) and severe asthma. Increased thickness of the small airway wall causes lumenal narrowing, which can be further occluded by mucus ...
journal_title：Trends in pharmacological sciences
pub_type： 杂志文章,评审
doi：10.1016/j.tips.2008.04.003
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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更新日期：2007-11-01 00:00:00
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journal_title：Trends in pharmacological sciences
pub_type： 杂志文章,评审
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
pub_type： 杂志文章,评审
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
pub_type： 杂志文章,评审
doi：10.1016/j.tips.2006.10.007
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journal_title：Trends in pharmacological sciences
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pub_type： 杂志文章,评审
doi：10.1016/j.tips.2020.12.004
更新日期：2021-01-23 00:00:00
abstract：:B7x (B7 homolog x, also known as B7-H4, B7S1, and VTCN1) was discovered by ourselves and others in 2003 as the seventh member of the B7 family. It is an inhibitory immune checkpoint of great significance to human disease. Tissue-expressed B7x minimizes autoimmune and inflammatory responses. It is overexpressed in a br...
journal_title：Trends in pharmacological sciences
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abstract：:Pharmacologists have studied receptors for more than a century but a molecular understanding of their properties has emerged only during the past 30-35 years. In this article, I provide a personal retrospective of how developments and discoveries primarily during the 1970s and 1980s led to current concepts about the l...
journal_title：Trends in pharmacological sciences
pub_type： 历史文章,杂志文章
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abstract：:In the past 20 years we have learned a great deal about GABAA receptor (GABAAR) subtypes, and which behaviors are regulated or which drug effects are mediated by each subtype. However, the question of where GABAARs involved in specific drug effects and behaviors are located in the brain remains largely unanswered. We ...
journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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doi：10.1016/j.tips.2011.09.001
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