Journal ArticleDOI
Pharmaceutical drug transport: the issues and the implications that it is essentially carrier-mediated only
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TLDR
Comparison of the rate of drug transport in natural versus artificial membranes shows discrepancies in absolute magnitudes of 100-fold or more, with the carrier-containing cells showing the greater permeability.About:
This article is published in Drug Discovery Today.The article was published on 2011-08-01. It has received 167 citations till now.read more
Citations
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Journal ArticleDOI
A Call for Systematic Research on Solute Carriers
Adrián César-Razquin,Berend Snijder,Tristan Frappier-Brinton,Ruth Isserlin,Gergely Gyimesi,Xiaoyun Bai,Reinhart A. F. Reithmeier,David Hepworth,Matthias A. Hediger,Aled M. Edwards,Giulio Superti-Furga,Giulio Superti-Furga +11 more
TL;DR: The time is right for a systematic attack on SLC structure, specificity, and function, taking into account kinship and expression, as well as the dependencies that arise from the common metabolic space.
Journal ArticleDOI
Synthetic biology for the directed evolution of protein biocatalysts: navigating sequence space intelligently
TL;DR: Improving enzymes by directed evolution requires the navigation of very large search spaces; this work surveys how to do this intelligently.
Journal ArticleDOI
Understanding Cell Penetration of Cyclic Peptides.
TL;DR: Common structural features that render most cyclic peptides membrane impermeable, as well as the unique features that allow the minority of sequences to enter the cell interior by passive diffusion, endocytosis/endosomal escape, or other mechanisms are examined.
Journal ArticleDOI
The Biology of Lactoferrin, an Iron-Binding Protein That Can Help Defend Against Viruses and Bacteria.
TL;DR: There is evidence that lactoferrin can bind to at least some of the receptors used by coronaviruses and thereby block their entry, and may consequently be of preventive and therapeutic value during the present COVID-19 pandemic.
Journal ArticleDOI
Cell-penetrating peptides transport therapeutics into cells
Joshua D. Ramsey,Nicholas Flynn +1 more
TL;DR: There are hundreds of cell-penetrating peptides being studied for drug delivery, and ongoing studies are demonstrating their success both in vitro and in vivo.
References
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Journal ArticleDOI
Structure and function of the blood–brain barrier
TL;DR: The structure and function of the BBB is summarised, the physical barrier formed by the endothelial tight junctions, and the transport barrier resulting from membrane transporters and vesicular mechanisms are described.
Journal ArticleDOI
Common SNPs explain a large proportion of the heritability for human height
Jian Yang,Beben Benyamin,Brian P. McEvoy,Scott D. Gordon,Anjali K. Henders,Dale R. Nyholt,Pamela A. F. Madden,Andrew C. Heath,Nicholas G. Martin,Grant W. Montgomery,Michael E. Goddard,Peter M. Visscher +11 more
TL;DR: Evidence is provided that the remaining heritability is due to incomplete linkage disequilibrium between causal variants and genotyped SNPs, exacerbated by causal variants having lower minor allele frequency than the SNPs explored to date.
Journal ArticleDOI
Can the pharmaceutical industry reduce attrition rates
Ismail Kola,John Landis +1 more
TL;DR: The pharmaceutical industry faces considerable challenges, both politically and fiscally, and the fiscal pressures that face the industry from the perspective of R&D are dealt with.
Journal ArticleDOI
Network pharmacology: the next paradigm in drug discovery.
TL;DR: A new appreciation of the role of polypharmacology has significant implications for tackling the two major sources of attrition in drug development--efficacy and toxicity.
Journal ArticleDOI
Membrane transporters in drug development.
Kathleen M. Giacomini,Shiew-Mei Huang,Donald J. Tweedie,Leslie Z. Benet,Kim L. R. Brouwer,Xiaoyan Chu,Amber Dahlin,Raymond Evers,Volker Fischer,Kathleen M. Hillgren,Keith Hoffmaster,Toshihisa Ishikawa,Dietrich Keppler,Richard B. Kim,Caroline A. Lee,Mikko Niemi,Joseph W. Polli,Yuicchi Sugiyama,Peter W. Swaan,Joseph A. Ware,Stephen H. Wright,Sook Wah Yee,Maciej J. Zamek-Gliszczynski,Lei Zhang +23 more
TL;DR: Overall, it is advised that the timing of transporter investigations should be driven by efficacy, safety and clinical trial enrolment questions, as well as a need for further understanding of the absorption, distribution, metabolism and excretion properties of the drug molecule, and information required for drug labelling.
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Paul D. Dobson,Douglas B. Kell +1 more
Membrane transporters in drug development.
Kathleen M. Giacomini,Shiew-Mei Huang,Donald J. Tweedie,Leslie Z. Benet,Kim L. R. Brouwer,Xiaoyan Chu,Amber Dahlin,Raymond Evers,Volker Fischer,Kathleen M. Hillgren,Keith Hoffmaster,Toshihisa Ishikawa,Dietrich Keppler,Richard B. Kim,Caroline A. Lee,Mikko Niemi,Joseph W. Polli,Yuicchi Sugiyama,Peter W. Swaan,Joseph A. Ware,Stephen H. Wright,Sook Wah Yee,Maciej J. Zamek-Gliszczynski,Lei Zhang +23 more