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1.
Clin Lab Med ; 27(1): 139-54, 2007 Mar.
Article in English | MEDLINE | ID: mdl-17416307

ABSTRACT

With the transition from manual to robotic HTS in the last several years, assay optimization has become a significant bottleneck. Recent advances in robotic liquid handling have made it feasible to reduce assay optimization timelines with the application of statistically designed experiments. When implemented, they can efficiently optimize assays by rapidly identifying significant factors, complex interactions, and nonlinear responses. This article focuses on the use of statistically designed experiments in assay optimization.


Subject(s)
Biological Assay/methods , Research Design , Automation , Data Interpretation, Statistical , Image Processing, Computer-Assisted , Reproducibility of Results
2.
J Nat Prod ; 65(4): 624-7, 2002 Apr.
Article in English | MEDLINE | ID: mdl-11975520

ABSTRACT

A MeOH/CH(2)Cl(2) extract of the bud covers of Artocarpus altilis collected in Micronesia showed activity in a cathepsin K inhibition assay. In addition to the three known flavonoids isolated from the bud covers of this species, two new compounds have been identified whose structures were determined on the basis of spectral data. These compounds include a dimeric dihydrochalcone, cycloaltilisin 6 (2), and a new prenylated flavone, cycloaltilisin 7 (3). Novel compounds 2 and 3 have IC(50) values of 98 and 840 nM, respectively, in cathepsin inhibition.


Subject(s)
Cathepsins/antagonists & inhibitors , Chalcone/isolation & purification , Cysteine Proteinase Inhibitors/isolation & purification , Flavonoids/isolation & purification , Moraceae/chemistry , Cathepsin K , Chalcone/analogs & derivatives , Chalcone/chemistry , Chalcone/pharmacology , Chromatography, High Pressure Liquid , Cysteine Proteinase Inhibitors/chemistry , Cysteine Proteinase Inhibitors/pharmacology , Flavonoids/chemistry , Flavonoids/pharmacology , Inhibitory Concentration 50 , Micronesia , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Plants, Medicinal , Spectrophotometry, Infrared
3.
J Nat Prod ; 65(4): 628-9, 2002 Apr.
Article in English | MEDLINE | ID: mdl-11975521

ABSTRACT

As part of a search for novel inhibitors of cathepsin K, the MeOH extract of a Micronesian sponge of the order Haplosclerida was shown to be active. Bioassay-guided fractionation of the extract yielded halitoxins, tryptamine, and a novel tryptamine-derived alkaloid, haploscleridamine (1). The tetrahydro-beta-carboline structure of haploscleridamine (1) was elucidated through spectral techniques. Haploscleridamine (1) was found to be an inhibitor of cathepsin K with an IC(50) of 26 microM.


Subject(s)
Alkaloids/isolation & purification , Cathepsins/antagonists & inhibitors , Cysteine Proteinase Inhibitors/isolation & purification , Porifera/chemistry , Tryptamines/isolation & purification , Alkaloids/chemistry , Alkaloids/pharmacology , Animals , Cathepsin K , Chromatography, Thin Layer , Cysteine Proteinase Inhibitors/chemistry , Cysteine Proteinase Inhibitors/pharmacology , Inhibitory Concentration 50 , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Palau , Spectrophotometry, Infrared , Spectroscopy, Fourier Transform Infrared , Tryptamines/chemistry , Tryptamines/pharmacology
4.
J Biomol Screen ; 7(6): 554-69, 2002 Dec.
Article in English | MEDLINE | ID: mdl-14599354

ABSTRACT

The thrust of early drug discovery in recent years has been toward the configuration of homogeneous miniaturized assays. This has allowed organizations to contain costs in the face of exponential increases in the number of screening assays that need to be run to remain competitive. Miniaturization brings with it an increasing dependence on instrumentation, which over the past several years has seen the development of nanodispensing capability and sophisticated detection strategies. To maintain confidence in the data generated from miniaturized assays, it is critical to ensure that both compounds and reagents have been delivered as expected to the target wells. The authors have developed a standard operating procedure for liquid-handling quality control that has enabled them to evaluate performance on 2 levels. The first level provides for routine daily testing on existing instrumentation, and the second allows for more rigorous testing of new dispensing technologies. The procedure has shown itself to be useful in identifying both method programming and instrumentation performance shortcomings and has provided a means to harmonizing instrumentation usage by assay development and screening groups. The goal is that this type of procedure be used for facilitating the exchange of liquid handler performance data across the industry.


Subject(s)
Microchemistry/instrumentation , Microchemistry/standards , Combinatorial Chemistry Techniques/instrumentation , Combinatorial Chemistry Techniques/standards , Data Interpretation, Statistical , Needles , Quality Control , Stainless Steel
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