title: Open access high throughput drug discovery in the public domain: a Mount Everest in the making.
abstract: High throughput screening (HTS) facilitates screening large numbers of compounds against a biochemical target of interest using validated biological or biophysical assays. In recent years, a significant number of drugs in clinical trails originated from HTS campaigns, validating HTS as a bona fide mechanism for hit finding. In the current drug discovery landscape, the pharmaceutical industry is embracing open innovation strategies with academia to maximize their research capabilities and to feed their drug discovery pipeline. The goals of academic research have therefore expanded from target identification and validation to probe discovery, chemical genomics, and compound library screening. This trend is reflected in the emergence of HTS centers in the public domain over the past decade, ranging in size from modestly equipped academic screening centers to well endowed Molecular Libraries Probe Centers Network (MLPCN) centers funded by the NIH Roadmap initiative. These centers facilitate a comprehensive approach to probe discovery in academia and utilize both classical and cutting-edge assay technologies for executing primary and secondary screening campaigns. The various facets of academic HTS centers as well as their implications on technology transfer and drug discovery are discussed, and a roadmap for successful drug discovery in the public domain is presented. New lead discovery against therapeutic targets, especially those involving the rare and neglected diseases, is indeed a Mount Everestonian size task, and requires diligent implementation of pharmaceutical industry's best practices for a successful outcome.
authors.affiliation: High Throughput Screening Laboratory, Institute for Advancing Medical Innovations, University of Kansas, Lawrence, KS 66047, USA.
authors.forename: Anuradha
authors.initials: A
authors.lastname: Roy
authors.forename: Peter R
authors.initials: PR
authors.lastname: McDonald
authors.forename: Sitta
authors.initials: S
authors.lastname: Sittampalam
authors.forename: Rathnam
authors.initials: R
authors.lastname: Chaguturu
mesh_terms: D022126:Access to Information / Q000331:legislation & jurisprudence; D000818:Animals; D055808:Drug Discovery / Q000331:legislation & jurisprudence / Q000379:methods* / Q000639:trends; D004353:Drug Evaluation, Preclinical / Q000379:methods / Q000639:trends; D004345:Drug Industry / Q000331:legislation & jurisprudence / Q000379:methods* / Q000639:trends; D057166:High-Throughput Screening Assays / Q000379:methods* / Q000639:trends; D006801:Humans; D004364:Pharmaceutical Preparations / Q000737:chemistry; D017150:Public Sector / Q000331:legislation & jurisprudence / Q000639:trends; D054852:Small Molecule Libraries / Q000737:chemistry / Q000378:metabolism; D014495:Universities / Q000331:legislation & jurisprudence / Q000639:trends
chemical_list: D004364:Pharmaceutical Preparations; D054852:Small Molecule Libraries
references.citation: Nat Rev Drug Discov. 2004 Apr;3(4):301-17
references.pmid: 15060526
references.citation: Nat Rev Drug Discov. 2009 Dec;8(12):959-68
references.pmid: 19949401
references.citation: Nat Rev Drug Discov. 2003 Jan;2(1):63-9
references.pmid: 12509760
references.citation: Comb Chem High Throughput Screen. 2008 Mar;11(3):216-30
references.pmid: 18336214
references.citation: Curr Genomics. 2009 Apr;10(2):93-101
references.pmid: 19794881
references.citation: Nat Rev Drug Discov. 2004 Oct;3(10):853-62
references.pmid: 15459676
references.citation: Nat Rev Drug Discov. 2002 Sep;1(9):727-30
references.pmid: 12209152
references.citation: Annu Rev Med. 2004;55:1-13
references.pmid: 14746506
references.citation: Curr Opin Pharmacol. 2007 Oct;7(5):527-34
references.pmid: 17652026
references.citation: Drug Discov Today. 2009 Dec;14(23-24):1150-8
references.pmid: 19793546
references.citation: Science. 2004 Nov 12;306(5699):1138-9
references.pmid: 15542455
references.citation: Health Policy. 2010 May;95(2-3):216-28
references.pmid: 20036435
references.citation: Curr Drug Discov Technol. 2007 Jun;4(1):48-58
references.pmid: 17630928
references.citation: Structure. 2000 Jul 15;8(7):R137-42
references.pmid: 10903952
references.citation: ACS Chem Biol. 2007 Jan 23;2(1):9-16
references.pmid: 17243777
references.citation: Nat Chem Biol. 2006 Dec;2(12):649-53
references.pmid: 17108976
references.citation: Biotechnol J. 2008 Apr;3(4):484-95
references.pmid: 18412175
references.citation: Nat Chem Biol. 2009 Jul;5(7):441-7
references.pmid: 19536101
references.citation: Nat Rev Drug Discov. 2003 Oct;2(10):831-8
references.pmid: 14526386
references.citation: Nat Rev Drug Discov. 2004 Jul;3(7):541
references.pmid: 15272492
references.citation: Nat Rev Drug Discov. 2006 Dec;5(12):993-6
references.pmid: 17139284
references.citation: Curr Opin Chem Biol. 2007 Oct;11(5):503-10
references.pmid: 17931958
references.citation: Expert Opin Ther Targets. 2009 Sep;13(9):1027-35
references.pmid: 19650760
references.citation: Comb Chem High Throughput Screen. 2009 Sep;12(8):741-51
references.pmid: 19531009
references.citation: Nat Chem Biol. 2007 Aug;3(8):466-79
references.pmid: 17637779