Literature DB >> 11865648

Combinatorial chemistry and high-throughput screening in drug discovery: different strategies and formats.

P Seneci1, S Miertus.   

Abstract

Different strategies for the discovery of novel leads interacting with therapeutically relevant targets are thoroughly presented and discussed, using also three recent examples. Emphasis is given to approaches which do not require extensive resources and budgets, but rather prove how cleverness and creativity can provide active compounds in drug discovery.

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Year:  2000        PMID： 11865648     DOI： 10.1023/a:1013824317218

Source DB:  PubMed          Journal:  Mol Divers        ISSN： 1381-1991            Impact factor:   2.943


  25 in total

1.  Potent, low-molecular-weight non-peptide inhibitors of malarial aspartyl protease plasmepsin II.

Authors:  T S Haque; A G Skillman; C E Lee; H Habashita; I Y Gluzman; T J Ewing; D E Goldberg; I D Kuntz; J A Ellman
Journal:  J Med Chem       Date:  1999-04-22       Impact factor: 7.446

Review 2.  High-throughput screening: new technology for the 21st century.

Authors:  R P Hertzberg; A J Pope
Journal:  Curr Opin Chem Biol       Date:  2000-08       Impact factor: 8.822

3.  Crystal structure of protein farnesyltransferase at 2.25 angstrom resolution.

Authors:  H W Park; S R Boduluri; J F Moomaw; P J Casey; L S Beese
Journal:  Science       Date:  1997-03-21       Impact factor: 47.728

4.  A drug that facilitates glutamatergic transmission reduces exploratory activity and improves performance in a learning-dependent task.

Authors:  R Granger; U Staubli; M Davis; Y Perez; L Nilsson; G A Rogers; G Lynch
Journal:  Synapse       Date:  1993-12       Impact factor: 2.562

5.  Facilitation of glutamate receptors enhances memory.

Authors:  U Staubli; G Rogers; G Lynch
Journal:  Proc Natl Acad Sci U S A       Date:  1994-01-18       Impact factor: 11.205

6.  Structure and inhibition of plasmepsin II, a hemoglobin-degrading enzyme from Plasmodium falciparum.

Authors:  A M Silva; A Y Lee; S V Gulnik; P Maier; J Collins; T N Bhat; P J Collins; R E Cachau; K E Luker; I Y Gluzman; S E Francis; A Oksman; D E Goldberg; J W Erickson
Journal:  Proc Natl Acad Sci U S A       Date:  1996-09-17       Impact factor: 11.205

7.  Benzothiadiazides inhibit rapid glutamate receptor desensitization and enhance glutamatergic synaptic currents.

Authors:  K A Yamada; C M Tang
Journal:  J Neurosci       Date:  1993-09       Impact factor: 6.167

8.  Cloning, expression and pharmacological characterization of a human glutamate receptor: hGluR4.

Authors:  E J Fletcher; S L Nutt; K H Hoo; C E Elliott; B Korczak; E A McWhinnie; R K Kamboj
Journal:  Receptors Channels       Date:  1995

9.  Modulation of AMPA/kainate receptors by analogues of diazoxide and cyclothiazide in thin slices of rat hippocampus.

Authors:  M Bertolino; M Baraldi; C Parenti; D Braghiroli; M DiBella; S Vicini; E Costa
Journal:  Receptors Channels       Date:  1993

10.  Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.

Authors:  N S Gray; L Wodicka; A M Thunnissen; T C Norman; S Kwon; F H Espinoza; D O Morgan; G Barnes; S LeClerc; L Meijer; S H Kim; D J Lockhart; P G Schultz
Journal:  Science       Date:  1998-07-24       Impact factor: 47.728
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  4 in total

1.  Combinatorially-generated library of 6-fluoroquinolone analogs as potential novel antitubercular agents: a chemometric and molecular modeling assessment.

Authors:  Nikola Minovski; Andrej Perdih; Tom Solmajer
Journal:  J Mol Model       Date:  2011-08-12       Impact factor: 1.810

Review 2.  Structural biology and bioinformatics in drug design: opportunities and challenges for target identification and lead discovery.

Authors:  Tom L Blundell; Bancinyane L Sibanda; Rinaldo Wander Montalvão; Suzanne Brewerton; Vijayalakshmi Chelliah; Catherine L Worth; Nicholas J Harmer; Owen Davies; David Burke
Journal:  Philos Trans R Soc Lond B Biol Sci       Date:  2006-03-29       Impact factor: 6.237

Review 3.  Status of antiviral therapeutics against rabies virus and related emerging lyssaviruses.

Authors:  Venice Du Pont; Richard K Plemper; Matthias J Schnell
Journal:  Curr Opin Virol       Date:  2019-02-10       Impact factor: 7.090

Review 4.  Discovery of cationic polymers for non-viral gene delivery using combinatorial approaches.

Authors:  Sutapa Barua; James Ramos; Thrimoorthy Potta; David Taylor; Huang-Chiao Huang; Gabriela Montanez; Kaushal Rege
Journal:  Comb Chem High Throughput Screen       Date:  2011-12       Impact factor: 1.339
  4 in total

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