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Pharmaceutics
Special Issues
Drug Discovery Tools
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Drug Discovery Tools

A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: closed (15 February 2011) | Viewed by 58729

Special Issue Editor

Prof. Dr. Andreas Vogt

E-Mail Website
Guest Editor
School of Engineering, University of Applied Sciences Northwestern Switzerland, Bahnhofstrasse 6, 5210 Windisch, Switzerland
Interests: electronic voting; formal protocol analysis; design of cryptographic protocols
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Over the last two decades, drug discovery has evolved into a science of its own. Advances in genomics, proteomics, chemical library synthesis, and assay technologies have firmly established high-throughput screening in both industry and academia. This special issue captures and highlights advances, successes, and challenges of contemporary drug discovery. We invite articles on all aspects of drug discovery tool development and utilization, including but not limited to, assay technologies, assay design and optimization, model systems (yeast, cells, worms, flies, zebrafish), biosensors, molecular modeling, and virtual screening.

Andreas Vogt
Guest Editor

Keywords

  • assay technologies
  • high-throughput screening
  • high-content analysis
  • model systems
  • molecular modeling
  • virtual screening

Published Papers (3 papers)

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Research

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1040 KiB  
Article
Design, Synthesis, and Biological Evaluation of PKD Inhibitors
by Kara M. George, Marie-Céline Frantz, Karla Bravo-Altamirano, Courtney R. LaValle, Manuj Tandon, Stephanie Leimgruber, Elizabeth R. Sharlow, John S. Lazo, Q. Jane Wang and Peter Wipf
Pharmaceutics 2011, 3(2), 186-228; https://doi.org/10.3390/pharmaceutics3020186 - 21 Apr 2011
Cited by 54 | Viewed by 11313
Abstract
Protein kinase D (PKD) belongs to a family of serine/threonine kinases that play an important role in basic cellular processes and are implicated in the pathogenesis of several diseases. Progress in our understanding of the biological functions of PKD has been limited due [...] Read more.
Protein kinase D (PKD) belongs to a family of serine/threonine kinases that play an important role in basic cellular processes and are implicated in the pathogenesis of several diseases. Progress in our understanding of the biological functions of PKD has been limited due to the lack of a PKD-specific inhibitor. The benzoxoloazepinolone CID755673 was recently reported as the first potent and kinase-selective inhibitor for this enzyme. For structure-activity analysis purposes, a series of analogs was prepared and their in vitro inhibitory potency evaluated. Full article
(This article belongs to the Special Issue Drug Discovery Tools)
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Review

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2094 KiB  
Review
Live Cell in Vitro and in Vivo Imaging Applications: Accelerating Drug Discovery
by Beverley Isherwood, Paul Timpson, Ewan J McGhee, Kurt I Anderson, Marta Canel, Alan Serrels, Valerie G Brunton and Neil O Carragher
Pharmaceutics 2011, 3(2), 141-170; https://doi.org/10.3390/pharmaceutics3020141 - 04 Apr 2011
Cited by 51 | Viewed by 14330
Abstract
Dynamic regulation of specific molecular processes and cellular phenotypes in live cell systems reveal unique insights into cell fate and drug pharmacology that are not gained from traditional fixed endpoint assays. Recent advances in microscopic imaging platform technology combined with the development of [...] Read more.
Dynamic regulation of specific molecular processes and cellular phenotypes in live cell systems reveal unique insights into cell fate and drug pharmacology that are not gained from traditional fixed endpoint assays. Recent advances in microscopic imaging platform technology combined with the development of novel optical biosensors and sophisticated image analysis solutions have increased the scope of live cell imaging applications in drug discovery. We highlight recent literature examples where live cell imaging has uncovered novel insight into biological mechanism or drug mode-of-action. We survey distinct types of optical biosensors and associated analytical methods for monitoring molecular dynamics, in vitro and in vivo. We describe the recent expansion of live cell imaging into automated target validation and drug screening activities through the development of dedicated brightfield and fluorescence kinetic imaging platforms. We provide specific examples of how temporal profiling of phenotypic response signatures using such kinetic imaging platforms can increase the value of in vitro high-content screening. Finally, we offer a prospective view of how further application and development of live cell imaging technology and reagents can accelerate preclinical lead optimization cycles and enhance the in vitro to in vivo translation of drug candidates. Full article
(This article belongs to the Special Issue Drug Discovery Tools)
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832 KiB  
Review
Cell Migration and Invasion Assays as Tools for Drug Discovery
by Keren I. Hulkower and Renee L. Herber
Pharmaceutics 2011, 3(1), 107-124; https://doi.org/10.3390/pharmaceutics3010107 - 11 Mar 2011
Cited by 288 | Viewed by 32504
Abstract
Cell migration and invasion are processes that offer rich targets for intervention in key physiologic and pathologic phenomena such as wound healing and cancer metastasis. With the advent of high-throughput and high content imaging systems, there has been a movement towards the use [...] Read more.
Cell migration and invasion are processes that offer rich targets for intervention in key physiologic and pathologic phenomena such as wound healing and cancer metastasis. With the advent of high-throughput and high content imaging systems, there has been a movement towards the use of physiologically relevant cell-based assays earlier in the testing paradigm. This allows more effective identification of lead compounds and recognition of undesirable effects sooner in the drug discovery screening process. This article will review the effective use of several principle formats for studying cell motility: scratch assays, transmembrane assays, microfluidic devices and cell exclusion zone assays. Full article
(This article belongs to the Special Issue Drug Discovery Tools)
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