2007
DOI: 10.1002/med.20091
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Allosteric modifiers of neuronal nicotinic acetylcholine receptors: New methods, new opportunities

Abstract: Allosteric, non-competitive inhibitors (NCIs) of neuronal nicotinic acetylcholine receptors (nAChRs) have been shown to produce a wide variety of clinically relevant responses. Many of the observed effects are desired as the nAChR is the therapeutic target, while others are undesired consequences due to off-target binding at the nAChR. Thus, the determination of whether or not a lead drug candidate is an NCI should play an important role in drug discovery programs. However, the current experimental techniques … Show more

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Cited by 40 publications
(46 citation statements)
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References 68 publications
(141 reference statements)
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“…3A. This is consistent with the peak shapes predicted by the theory of non-linear chromatography, which describes the interactions between a ligand and a protein within an affinity chromatography system and which attributes the observed dissymmetry to the relatively slow dissociation of the ligand-protein complex [17]. Although these properties are useful in some experimental setting, they also hinder the direct application CMAC(+) columns in affinity screens.…”
Section: Chromatography Of Fraction 1a On the Cmac(+) And Cmac(−) Colsupporting
confidence: 84%
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“…3A. This is consistent with the peak shapes predicted by the theory of non-linear chromatography, which describes the interactions between a ligand and a protein within an affinity chromatography system and which attributes the observed dissymmetry to the relatively slow dissociation of the ligand-protein complex [17]. Although these properties are useful in some experimental setting, they also hinder the direct application CMAC(+) columns in affinity screens.…”
Section: Chromatography Of Fraction 1a On the Cmac(+) And Cmac(−) Colsupporting
confidence: 84%
“…Using the frontal displacement chromatography of EB [17]. The total specific binding capacity of the columns was shown to average ~0.5 pmoles/mg of stationary phase.…”
Section: Chromatography Of Fraction 1a On the Cmac(+) And Cmac(−) Colmentioning
confidence: 99%
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