Literature DB >> 21395284

Use and implications of the harmonic mean model on mixtures for basic research and drug discovery.

Radleigh G Santos1, Marc A Giulianotti, Colette T Dooley, Clemencia Pinilla, Jon R Appel, Richard A Houghten.   

Abstract

The use of the harmonic mean model for predicting the activities of a given mixture and its constituents has not previously been explored in the context of combinatorial libraries and drug discovery. Herein, the analyses of historical data confirm the harmonic mean as an accurate predictor of mixture activity. The implications of these results are discussed.

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Year:  2011        PMID： 21395284      PMCID： PMC3096014          DOI： 10.1021/co100065a

Source DB:  PubMed          Journal:  ACS Comb Sci        ISSN： 2156-8944            Impact factor:   3.784


  23 in total

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Authors:  Charles L Cantrell; Steven L Richheimer; Gillian M Nicholas; Brad K Schmidt; David T Bailey
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3.  Synergy and antagonism of promiscuous inhibition in multiple-compound mixtures.

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Review 4.  The application of cassette dosing for pharmacokinetic screening in small-molecule cancer drug discovery.

Authors:  Nicola F Smith; Florence I Raynaud; Paul Workman
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Review 5.  Drug discovery and natural products: end of an era or an endless frontier?

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Journal:  Science       Date:  2009-07-10       Impact factor: 47.728

6.  Curacin D, an antimitotic agent from the marine cyanobacterium Lyngbya majuscula.

Authors:  B Márquez; P Verdier-Pinard; E Hamel; W H Gerwick
Journal:  Phytochemistry       Date:  1998-12       Impact factor: 4.072

7.  Drug leads from combinatorial phosphodiester libraries.

Authors:  P W Davis; T A Vickers; L Wilson-Lingardo; J R Wyatt; C J Guinosso; Y S Sanghvi; E A DeBaets; O L Acevedo; P D Cook; D J Ecker
Journal:  J Med Chem       Date:  1995-10-27       Impact factor: 7.446

8.  Deconvolution of combinatorial libraries for drug discovery: a model system.

Authors:  S M Freier; D A Konings; J R Wyatt; D J Ecker
Journal:  J Med Chem       Date:  1995-01-20       Impact factor: 7.446

9.  Massetolides A-H, antimycobacterial cyclic depsipeptides produced by two pseudomonads isolated from marine habitats.

Authors:  J Gerard; R Lloyd; T Barsby; P Haden; M T Kelly; R J Andersen
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10.  Use of cassette dosing in sandwich-cultured rat and human hepatocytes to identify drugs that inhibit bile acid transport.

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  12 in total

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Authors:  Clemencia Pinilla; Bruce S Edwards; Jon R Appel; Tina Yates-Gibbins; Marc A Giulianotti; Jose L Medina-Franco; Susan M Young; Radleigh G Santos; Larry A Sklar; Richard A Houghten
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3.  Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa1-Arg-(pI)DPhe-Xaa4-NH2.

Authors:  Skye R Doering; Katie T Freeman; Sathya M Schnell; Erica M Haslach; Marvin Dirain; Ginamarie Debevec; Phaedra Geer; Radleigh G Santos; Marc A Giulianotti; Clemencia Pinilla; Jon R Appel; Robert C Speth; Richard A Houghten; Carrie Haskell-Luevano
Journal:  J Med Chem       Date:  2017-05-15       Impact factor: 7.446

4.  A novel method for the determination of isokinetic ratios and its application in the synthesis of two new positional scanning libraries.

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5.  Discovery of novel inhibitors of a disintegrin and metalloprotease 17 (ADAM17) using glycosylated and non-glycosylated substrates.

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6.  Scaffold ranking and positional scanning utilized in the discovery of nAChR-selective compounds suitable for optimization studies.

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Journal:  J Med Chem       Date:  2013-12-12       Impact factor: 7.446

7.  The mathematics of a successful deconvolution: a quantitative assessment of mixture-based combinatorial libraries screened against two formylpeptide receptors.

Authors:  Radleigh G Santos; Jon R Appel; Marc A Giulianotti; Bruce S Edwards; Larry A Sklar; Richard A Houghten; Clemencia Pinilla
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8.  Direct Phenotypic Screening in Mice: Identification of Individual, Novel Antinociceptive Compounds from a Library of 734,821 Pyrrolidine Bis-piperazines.

Authors:  Richard A Houghten; Michelle L Ganno; Jay P McLaughlin; Colette T Dooley; Shainnel O Eans; Radleigh G Santos; Travis LaVoi; Adel Nefzi; Greg Welmaker; Marc A Giulianotti; Lawrence Toll
Journal:  ACS Comb Sci       Date:  2016-01-05       Impact factor: 3.784

9.  Identification of Protein Palmitoylation Inhibitors from a Scaffold Ranking Library.

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10.  Bridging immunogenetics and immunoproteomics: Model positional scanning library analysis for Major Histocompatibility Complex class II DQ in Tursiops truncatus.

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