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Golovanov, I. B.; Tsygankova, I. G.

doi:10.1023/a:1015374102560

Cited by 4 publications

(7 citation statements)

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“…The log P values of peptides and metallocene peptides in this study span a wide range. A log P value of around −1.2 for [Leu 5 ]‐enkephalin 1 is consistent with the literature 56. All of the studied modifications of enkephalin lead to an increase in log P .…”

Section: Discussionsupporting

confidence: 90%

Modification with Organometallic Compounds Improves Crossing of the Blood–Brain Barrier of [Leu⁵]‐Enkephalin Derivatives in an In Vitro Model System

et al. 2009

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Enkephalin peptides are thought to be suitable vectors for the passage of the blood-brain barrier (BBB). Modifications that do not alter the amino acid sequence are often used to improve the permeation through living membrane systems. As a new type of modification we introduce organometallic compounds, in particular ferrocene carboxylic acid. Derivatives of [Leu5]enkephalin were synthesised and labelled with organometallic compounds by using solid-phase synthesis techniques. All new metal-peptide bioconjugates were comprehensively characterised by HPLC, NMR spectroscopy and mass spectrometry and found to be at least 95% pure. For the first time, permeation coefficients in a BBB model for organometal-peptide derivatives were determined in this work. The uptake and localisation of fluorescein-labelled enkephalins was monitored by fluorescence microscopy on three cancer cell lines. Octanol/H2O partition coefficients of the compounds were measured by HPLC. The introduction of the organometallic moiety enhances the uptake into cells and the permeation coefficient of [Leu5]-enkephalin. This could be due to an increase in lipophilicity caused by the organometallic label. The metal-peptide conjugates were found to be nontoxic up to mM concentrations. The low cytotoxicity encourages further experiments that could take advantage of the selectivity of enkephalin derivatives for opioid receptors.

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Section: Discussionsupporting

confidence: 90%

Modification with Organometallic Compounds Improves Crossing of the Blood–Brain Barrier of [Leu⁵]‐Enkephalin Derivatives in an In Vitro Model System

et al. 2009

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“…It can be estimated as described in [9]. The term E AB disp can be approximately determined by London formula:…”

Section: Methodsmentioning

confidence: 99%

“…For this class of compounds several ways of consideration are also possible: 1) Using (9) with the addition of one more parameter for cycle formation: P n 1 a n 2 b (a) Calculations have been performed according to equation: T boil n 1 a n 2 b n 3 g n 4 d 1 n 5 d 2 Á Á Á n c d c n X d X n * d * .…”

Section: Estimations For Cyclic Moleculesmentioning

confidence: 99%

Estimation of Physicochemical Properties from the Structure-Property Relationship: A New Approach

Golovanov

Tsygankova²

2000

Quant. Struct.-Act. Relat.

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An approach is proposed for estimating the physicochemical properties of the organic molecules of different classes from a simple structure-property correlation equation. The necessity of consideration of molecular conformations is analyzed. The method is applied for estimating the boiling temperatures of saturated hydrocarbons. Possible applications for other properties are discussed. Some modi®cations of SPCE for the cases with the shortage of experimental data are described.

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“…And when used in aircraft construction, the disruption of the moving environment can lead to a peak and crash of the aircraft. In works [1,2,3] various variants of surface portions are considered, but none of them provides a linear law of curvature change.…”

Section: Modeling and Computer Implementation Of A Surface Portion On...mentioning

confidence: 99%

“…Recent research and publication analysis. In articles [1,2,3], various variants of portions of surfaces are described, but none of them provides the setting of a linear law of change in curvature over the surface.…”

Section: Statement Of Problemmentioning

confidence: 99%

Modeling and Computer Implementation of a Surface Portion on the Basis of “Clothoid” Curves

2022

mpom23

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Cited by 4 publications

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Modification with Organometallic Compounds Improves Crossing of the Blood–Brain Barrier of [Leu⁵]‐Enkephalin Derivatives in an In Vitro Model System

Modification with Organometallic Compounds Improves Crossing of the Blood–Brain Barrier of [Leu⁵]‐Enkephalin Derivatives in an In Vitro Model System

Estimation of Physicochemical Properties from the Structure-Property Relationship: A New Approach

Modeling and Computer Implementation of a Surface Portion on the Basis of “Clothoid” Curves

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Untitled

Cited by 4 publications

References 1 publication

Modification with Organometallic Compounds Improves Crossing of the Blood–Brain Barrier of [Leu5]‐Enkephalin Derivatives in an In Vitro Model System

Modification with Organometallic Compounds Improves Crossing of the Blood–Brain Barrier of [Leu5]‐Enkephalin Derivatives in an In Vitro Model System

Estimation of Physicochemical Properties from the Structure-Property Relationship: A New Approach

Modeling and Computer Implementation of a Surface Portion on the Basis of “Clothoid” Curves

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Product

Resources

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Modification with Organometallic Compounds Improves Crossing of the Blood–Brain Barrier of [Leu⁵]‐Enkephalin Derivatives in an In Vitro Model System

Modification with Organometallic Compounds Improves Crossing of the Blood–Brain Barrier of [Leu⁵]‐Enkephalin Derivatives in an In Vitro Model System