The evolving role of natural products in drug discovery
Recent technological advances that help to address issues such as the lack of compatibility of traditional natural-product extract libraries with high-throughput screening and unrealized expectations from current lead-generation strategies have led to a renewed interest in natural products in drug discovery.
High throughput artificial membrane permeability assay for blood-brain barrier.
- L. Di, E. Kerns, K. Fan, O. Mcconnell, G. Carter
- Biology, ChemistryEuropean journal of medicinal chemistry
- 1 March 2003
Biosynthesis of the immunosuppressants FK506, FK520, and rapamycin involves a previously undescribed family of enzymes acting on chorismate
- J. Andexer, S. Kendrew, B. Wilkinson
- Biology, ChemistryProceedings of the National Academy of Sciences
- 7 March 2011
FkbO, RapK, Hyg5, and Bra8 are founder members of a previously unrecognized family of enzymes acting on chorismate, which includes the product of the bra8 gene from the pathway to the terpenoid natural product brasilicardin.
Drug-like property concepts in pharmaceutical design.
High throughput ADME/TOX assays have been implemented and are being widely used to drive drug discovery projects in parallel with activity screening, and property design has become an integrated and inseparable part of the modern drug discovery paradigm.
Biosynthetic Potential of Phylogenetically Unique Endophytic Actinomycetes from Tropical Plants
The results suggest that tropical plants from New Guinea and the adjacent archipelago are hosts to unique endophytic actinomycetes that possess significant biosynthetic potential.
In vitro solubility assays in drug discovery.
Kinetic solubility is useful for rapid compound assessment, guiding optimization via structure modification, and diagnosing bioassays using conditions that answer specific research questions of drug discovery teams, such as compound selection and vehicle development for pharmacology and PK studies.
In Vitro Permeability of Poorly Aqueous Soluble Compounds Using Different Solubilizers in the PAMPA Assay with Liquid Chromatography/Mass Spectrometry Detection
- Hanlan Liu, Chantel L. Sabus, G. Carter, Chao Du, A. Avdeef, M. Tischler
- BiologyPharmaceutical Research
- 1 November 2003
Although many solubilizers were found to interfere with UV-VIS detection, the LC/MS approach was applicable to determine the permeability values of compounds with normally low aqueous solubility, which means PAMPA can be used in both discovery and pre-formulation applications.
Rapid cloning and heterologous expression of the meridamycin biosynthetic gene cluster using a versatile Escherichia coli-streptomyces artificial chromosome vector, pSBAC.
- Hongbo Liu, Hao-Tian Jiang, M. He
- Biology, EngineeringJournal of Natural Products
- 3 February 2009
The development of a versatile Escherichia coli-Streptomyces shuttle Bacterial Artificial Chromosomal (BAC) conjugation vector, pSBAC, to facilitate the cloning, genetic manipulation, and heterologous expression of actinomycetes secondary metabolite biosynthetic gene clusters is described.
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