Abstract：
:The concept of drug-target residence time has been in focus in recent drug discovery literature. However, few studies consider the combined effect of pharmacokinetics (PK) and binding kinetics (BK) on the duration of effect of a drug. Using a simple model that takes both PK and BK into account, we found that prolongation of binding owing to a long drug-target residence time can only occur when the binding dissociation is slower than the PK elimination. Data for several drugs and/or drug candidates in the literature indicate that the opposite is observed, that is, they have a slower elimination compared with dissociation. These observations greatly reduce the usability of drug-target residence times for estimating the duration of effect of a drug in vivo.
journal_name
Drug Discov Todayjournal_title
Drug discovery todayauthors
Dahl G,Akerud Tdoi
10.1016/j.drudis.2013.02.010subject
Has Abstractpub_date
2013-08-01 00:00:00pages
697-707issue
15-16eissn
1359-6446issn
1878-5832pii
S1359-6446(13)00068-8journal_volume
18pub_type
杂志文章,评审abstract：:The increasing incidence of cutaneous malignancies signifies the need for multiple treatment options. Several available reviews have emphasized the potential role of various botanical extracts and naturally occurring compounds as anti-skin-cancer agents. Few studies relate to the role of chemoprevention and therapeuti...
journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
pub_type： 杂志文章,评审
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journal_title：Drug discovery today
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journal_title：Drug discovery today
pub_type： 杂志文章,评审
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journal_title：Drug discovery today
pub_type： 杂志文章,评审
doi：10.1016/j.drudis.2012.02.013
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
pub_type： 杂志文章,评审
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journal_title：Drug discovery today
pub_type： 杂志文章,评审
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journal_title：Drug discovery today
pub_type： 杂志文章,评审
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journal_title：Drug discovery today
pub_type： 杂志文章,评审
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journal_title：Drug discovery today
pub_type： 杂志文章,评审
doi：10.1016/j.drudis.2011.02.005
更新日期：2012-05-01 00:00:00
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journal_title：Drug discovery today
pub_type： 杂志文章,评审
doi：10.1016/j.drudis.2014.09.018
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
pub_type： 杂志文章
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journal_title：Drug discovery today
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