Literature DB >> 25909818

Increasing the delivery of next generation therapeutics from high throughput screening libraries.

Mark J Wigglesworth1, David C Murray2, Carolyn J Blackett2, Michael Kossenjans3, J Willem M Nissink4.   

Abstract

The pharmaceutical industry has historically relied on high throughput screening as a cornerstone to identify chemical equity for drug discovery projects. However, with pharmaceutical companies moving through a phase of diminished returns and alternative hit identification strategies proving successful, it is more important than ever to understand how this approach can be used more effectively to increase the delivery of next generation therapeutics from high throughput screening libraries. There is a wide literature that describes HTS and fragment based screening approaches which offer clear direction on the process for these two distinct activities. However, few people have considered how best to identify medium to low molecular weight compounds from large diversity screening sets and increase downstream success.
Copyright © 2015 Elsevier Ltd. All rights reserved.

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Year:  2015        PMID: 25909818     DOI: 10.1016/j.cbpa.2015.04.006

Source DB:  PubMed          Journal:  Curr Opin Chem Biol        ISSN: 1367-5931            Impact factor:   8.822


  6 in total

Review 1.  Small molecules as therapeutic agents for inborn errors of metabolism.

Authors:  Leslie Matalonga; Laura Gort; Antonia Ribes
Journal:  J Inherit Metab Dis       Date:  2016-12-13       Impact factor: 4.982

Review 2.  Combinatorial chemistry in drug discovery.

Authors:  Ruiwu Liu; Xiaocen Li; Kit S Lam
Journal:  Curr Opin Chem Biol       Date:  2017-05-08       Impact factor: 8.822

3.  Trends in Hit-to-Lead Optimization Following DNA-Encoded Library Screens.

Authors:  Christopher A Reiher; David P Schuman; Nicholas Simmons; Scott E Wolkenberg
Journal:  ACS Med Chem Lett       Date:  2021-02-11       Impact factor: 4.345

Review 4.  Pimping up Drugs Recovered, Superannuated and Under Exploited Drugs - An Introduction to the Basics of Drug Reprofiling.

Authors:  Suzanne J Dilly; George S Morris
Journal:  Curr Drug Discov Technol       Date:  2017

5.  Automated screening for small organic ligands using DNA-encoded chemical libraries.

Authors:  Willy Decurtins; Moreno Wichert; Raphael M Franzini; Fabian Buller; Michael A Stravs; Yixin Zhang; Dario Neri; Jörg Scheuermann
Journal:  Nat Protoc       Date:  2016-03-17       Impact factor: 13.491

6.  Changing the HTS Paradigm: AI-Driven Iterative Screening for Hit Finding.

Authors:  Gabriel H S Dreiman; Magda Bictash; Paul V Fish; Lewis Griffin; Fredrik Svensson
Journal:  SLAS Discov       Date:  2020-08-18       Impact factor: 3.341

  6 in total

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