Literature DB >> 23672690

Contributions of academic laboratories to the discovery and development of chemical biology tools.

Donna M Huryn1, Lynn O Resnick, Peter Wipf.   

Abstract

The academic setting provides an environment that may foster success in the discovery of certain types of small molecule tools while proving less suitable in others. For example, small molecule probes for poorly understood systems, those that exploit a specific resident expertise, and those whose commercial return is not apparent are ideally suited to be pursued in a university setting. In this review, we highlight five projects that emanated from academic research groups and generated valuable tool compounds that have been used to interrogate biological phenomena: reactive oxygen species (ROS) sensors, GPR30 agonists and antagonists, selective CB2 agonists, Hsp70 modulators, and β-amyloid PET imaging agents. By taking advantage of the unique expertise resident in university settings and the ability to pursue novel projects that may have great scientific value but with limited or no immediate commercial value, probes from academic research groups continue to provide useful tools and generate a long-term resource for biomedical researchers.

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Year:  2013        PMID: 23672690      PMCID: PMC3785552          DOI: 10.1021/jm400132d

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  100 in total

1.  CB2 cannabinoid receptor-mediated peripheral antinociception.

Authors:  T P Malan; M M Ibrahim; H Deng; Q Liu; H P Mata; T Vanderah; F Porreca; A Makriyannis
Journal:  Pain       Date:  2001-09       Impact factor: 6.961

Review 2.  Grants4Targets - an innovative approach to translate ideas from basic research into novel drugs.

Authors:  Monika Lessl; Stefanie Schoepe; Anette Sommer; Martin Schneider; Khusru Asadullah
Journal:  Drug Discov Today       Date:  2010-12-01       Impact factor: 7.851

3.  Longitudinal assessment of Aβ and cognition in aging and Alzheimer disease.

Authors:  Victor L Villemagne; Kerryn E Pike; Gaël Chételat; Kathryn A Ellis; Rachel S Mulligan; Pierrick Bourgeat; Uwe Ackermann; Gareth Jones; Cassandra Szoeke; Olivier Salvado; Ralph Martins; Graeme O'Keefe; Chester A Mathis; William E Klunk; David Ames; Colin L Masters; Christopher C Rowe
Journal:  Ann Neurol       Date:  2011-01       Impact factor: 10.422

4.  17β-estradiol inhibits the production of infectious particles of hepatitis C virus.

Authors:  Kazumi Hayashida; Ikuo Shoji; Lin Deng; Da-Peng Jiang; Yoshi-Hiro Ide; Hak Hotta
Journal:  Microbiol Immunol       Date:  2010-11       Impact factor: 1.955

5.  Chronic treatment with estrogen receptor agonists restores acquisition of a spatial learning task in young ovariectomized rats.

Authors:  R Hammond; R Mauk; D Ninaci; D Nelson; R B Gibbs
Journal:  Horm Behav       Date:  2009-06-25       Impact factor: 3.587

6.  Too many roads not taken.

Authors:  Aled M Edwards; Ruth Isserlin; Gary D Bader; Stephen V Frye; Timothy M Willson; Frank H Yu
Journal:  Nature       Date:  2011-02-10       Impact factor: 49.962

7.  Plasmodium falciparum encodes a single cytosolic type I Hsp40 that functionally interacts with Hsp70 and is upregulated by heat shock.

Authors:  Melissa Botha; Annette N Chiang; Patrick G Needham; Linda L Stephens; Heinrich C Hoppe; Simone Külzer; Jude M Przyborski; Klaus Lingelbach; Peter Wipf; Jeffrey L Brodsky; Addmore Shonhai; Gregory L Blatch
Journal:  Cell Stress Chaperones       Date:  2010-12-30       Impact factor: 3.667

8.  A BODIPY-based fluorescent dye for mitochondria in living cells, with low cytotoxicity and high photostability.

Authors:  Si Zhang; Tong Wu; Jiangli Fan; Zhiyong Li; Na Jiang; Jingyun Wang; Bairui Dou; Shiguo Sun; Fengling Song; Xiaojun Peng
Journal:  Org Biomol Chem       Date:  2012-12-11       Impact factor: 3.876

9.  Phase 1 study of the Pittsburgh compound B derivative 18F-flutemetamol in healthy volunteers and patients with probable Alzheimer disease.

Authors:  Natalie Nelissen; Koen Van Laere; Lennart Thurfjell; Rikard Owenius; Mathieu Vandenbulcke; Michel Koole; Guy Bormans; David J Brooks; Rik Vandenberghe
Journal:  J Nucl Med       Date:  2009-07-17       Impact factor: 10.057

10.  PubChem's BioAssay Database.

Authors:  Yanli Wang; Jewen Xiao; Tugba O Suzek; Jian Zhang; Jiyao Wang; Zhigang Zhou; Lianyi Han; Karen Karapetyan; Svetlana Dracheva; Benjamin A Shoemaker; Evan Bolton; Asta Gindulyte; Stephen H Bryant
Journal:  Nucleic Acids Res       Date:  2011-12-02       Impact factor: 16.971

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  9 in total

1.  Challenges with risk mitigation in academic drug discovery: finding the best solution.

Authors:  Anuradha Roy
Journal:  Expert Opin Drug Discov       Date:  2018-12-04       Impact factor: 6.098

2.  A Medicinal Chemist's Perspective on Transitioning from Industry to Academic Drug Discovery.

Authors:  James C Barrow
Journal:  ACS Med Chem Lett       Date:  2019-04-15       Impact factor: 4.345

3.  Consortia's critical role in developing medical countermeasures for re-emerging viral infections: a USA perspective.

Authors:  Maaike Everts; Mark J Suto; George R Painter; Richard J Whitley
Journal:  Future Virol       Date:  2016-02-29       Impact factor: 1.831

Review 4.  Evolution of a strategy for preparing bioactive small molecules by sequential multicomponent assembly processes, cyclizations, and diversification.

Authors:  James J Sahn; Brett A Granger; Stephen F Martin
Journal:  Org Biomol Chem       Date:  2014-08-19       Impact factor: 3.876

Review 5.  International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators.

Authors:  Eric R Prossnitz; Jeffrey B Arterburn
Journal:  Pharmacol Rev       Date:  2015-07       Impact factor: 25.468

6.  Photooxygenation of an amino-thienopyridone yields a more potent PTP4A3 inhibitor.

Authors:  Joseph M Salamoun; Kelley E McQueeney; Kalyani Patil; Steven J Geib; Elizabeth R Sharlow; John S Lazo; Peter Wipf
Journal:  Org Biomol Chem       Date:  2016-07-06       Impact factor: 3.876

Review 7.  Estrogen biology: new insights into GPER function and clinical opportunities.

Authors:  Eric R Prossnitz; Matthias Barton
Journal:  Mol Cell Endocrinol       Date:  2014-02-12       Impact factor: 4.102

8.  Discovery of Mcl-1 inhibitors from integrated high throughput and virtual screening.

Authors:  Ahmed S A Mady; Chenzhong Liao; Naval Bajwa; Karson J Kump; Fardokht A Abulwerdi; Katherine L Lev; Lei Miao; Sierrah M Grigsby; Andrej Perdih; Jeanne A Stuckey; Yuhong Du; Haian Fu; Zaneta Nikolovska-Coleska
Journal:  Sci Rep       Date:  2018-07-05       Impact factor: 4.379

Review 9.  Early Probe and Drug Discovery in Academia: A Minireview.

Authors:  Anuradha Roy
Journal:  High Throughput       Date:  2018-02-09
  9 in total

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