Chemical biology tools for probing transcytosis at the blood–brain barrier

Beard, Rhiannon; Gaboriau, David; Gee, Antony D.; Tate, Edward W.

doi:10.1039/c9sc04024b

Cited by 11 publications

(8 citation statements)

References 22 publications

(34 reference statements)

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“…Values of BBB is categorized in two categories viz., BBB > 0.1 is BBB+ and BB ratio <0.1 is BBB-. (Beard, Gaboriau, Gee, & Tate, 2019) All top six noscapines shows BBB+ nature.…”

Section: Distribution Properties Of Top-six Noscapinesmentioning

confidence: 99%

Inhibition of Protease of Novel Corona Virus by Designed Noscapines: Molecular Docking and ADMET Studies

Vishvakarma¹,

Kumari²,

Singh

2020

Preprint

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<p>Nowadays, many people were dying due to infectious coronavirus diseases (COVID-19). It belongs to the betacoronavirus family and also known as SARS-CoV-2. However, COVID-19 is a new form that has some basic difference in the genome which makes it more lethal and infectious. In transmitted in human in late December 2019 and it infected about 20 million till date. Its genome is composed of positive-sense single-stranded RNA, which encodes for the poly-protein. This poly-protein further cleaved into various components of the virus to make the numerous copy of the virus. There are many more similarities in their genome among the SARS-CoV-2, SARS-CoV, MERS-CoV. However, protease proteins are responsible for the cleavage and hence, COVID-19 main protease is a prime therapeutic target. To date, no medicine/ vaccine can fully cure their infection. To inhibit the activity of protease of COVID-19, molecular docking and ADMET studies of 116 noscapine derivatives were performed and the result was compared with 14 reputed antiviral drugs including chloroquine and hydroxychloroquine. The molecular docking result indicates a better binding in comparison of 14 reputed drugs. Further, the top six noscapines was taken into consideration for the pose analysis and ADMET studies. Finally, the top six noscapine was refined by ADMET properties to get the most potent one.</p>

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“…Values of BBB is categorized in two categories viz., BBB > 0.1 is BBB+ and BB ratio <0.1 is BBB-. (Beard, Gaboriau, Gee, & Tate, 2019) All top six noscapines shows BBB+ nature.…”

Section: Distribution Properties Of Top-six Noscapinesmentioning

confidence: 99%

Inhibition of Protease of Novel Corona Virus by Designed Noscapines: Molecular Docking and ADMET Studies

Vishvakarma¹,

Kumari²,

Singh

2020

Preprint

View full text Add to dashboard Cite

show abstract

“…1a). 2,[21][22][23][24][25][26][27] This mechanism allows the TfR to efficiently penetrate tumors and cross the blood-brain barrier to deliver iron to the brain. The attachment of transferrin or ligands of other transcytosis receptors to operational transport systems has been shown to improve delivery into deep tissue.…”

Section: Introductionmentioning

confidence: 99%

“…The attachment of transferrin or ligands of other transcytosis receptors to operational transport systems has been shown to improve delivery into deep tissue. 2,[21][22][23][24][25][26][27] Evidence is emerging that the TfR also participates in thiolmediated uptake [28][29][30][31][32] and viral entry, 28,33,34 including oligonucleotide phosphorothioates 35 and SARS-CoV-2, 28,34 respectively (Fig. 1b).…”

Section: Introductionmentioning

confidence: 99%

Dithiolane quartets: thiol-mediated uptake enables cytosolic delivery in deep tissue

et al. 2021

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“…The blood-brain barrier is formed by specialized endothelial cells (ECs), which are sealed together by a series of complex, tight connections that form a proper biological barrier, 31 limiting the free exchange of most substances between brain extracellular fluid and plasma. 32 Only materials are small enough in size or highly lipophilic can cross BBB.…”

Section: Introductionmentioning

confidence: 99%

Citric acid coated ultrasmall superparamagnetic iron oxide nanoparticles conjugated with lactoferrin for targeted negative MR imaging of glioma

et al. 2020

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The proposed study was to develop the preparation of ultrasmall superparamagnetic iron oxide nanoparticles (USPIONs) modified with citric acid, with surface conjugated with lactoferrin (Lf), which used as a potential targeted contrast agent for magnetic resonance imaging (MRI) of brain glioma. USPIONs were prepared by the thermal decomposition method. The hydrophobic USPIONs were coated with citric acid by the ligand exchange method. Then, Lf was conjugated into the surface of USPIONs. The obtained Lf-USPIONs were analyzed by fourier transform infrared (FTIR) spectroscopy and polyacrylamide gel electrophoresis. The size, size distribution, shape and superparamagnetic property of Lf-USPIONs were investigated with TEM and vibrating sample magnetometer (VSM). Both FTIR and electrophoresis analysis demonstrated the successful conjugation of Lf to the surface of USPIONs. The average size of Lf-USPIONs was about 8.4 ± 0.5 nm, which was determined using the statistics of measured over 100 nanoparticles in the TEM image, with a negative charge of −7.3 ± 0.2 mV. TEM imaging revealed that Lf-USPIONs were good in dispersion and polygonal in morphology. VSM results indicated that Lf-USPIONs were superparamagnetic and the saturated magnetic intensity was about 69.8 emu/g. The Lf-USPIONs also showed good biocompatibility in hemolysis, cytotoxicity, cell migration and blood biochemistry studies. MR imaging results in vitro and in vivo indicated that Lf-USPIONs exhibited good negative contrast enhancement. Taken together, Lf-USPIONs hold great potential for brain gliomas MR imaging as a nanosized targeted contrast agent.

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Chemical biology tools for probing transcytosis at the blood–brain barrier

Abstract: A BBB vehicle library is validated, establishing a SAR for uptake. Merging AMT/RMT motifs chemoselectively increased permeability.

Cited by 11 publications

References 22 publications

Inhibition of Protease of Novel Corona Virus by Designed Noscapines: Molecular Docking and ADMET Studies

Inhibition of Protease of Novel Corona Virus by Designed Noscapines: Molecular Docking and ADMET Studies

Dithiolane quartets: thiol-mediated uptake enables cytosolic delivery in deep tissue

Citric acid coated ultrasmall superparamagnetic iron oxide nanoparticles conjugated with lactoferrin for targeted negative MR imaging of glioma

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