Literature DB >> 24409957

The role of HTS in drug discovery at the University of Michigan.

Martha J Larsen, Scott D Larsen, Andrew Fribley, Jolanta Grembecka, Kristoff Homan, Anna Mapp, Andrew Haak, Zaneta Nikolovska-Coleska, Jeanne A Stuckey, Duxin Sun, David H Sherman1.   

Abstract

High throughput screening (HTS) is an integral part of a highly collaborative approach to drug discovery at the University of Michigan. The HTS lab is one of four core centers that provide services to identify, produce, screen and follow-up on biomedical targets for faculty. Key features of this system are: protein cloning and purification, protein crystallography, small molecule and siRNA HTS, medicinal chemistry and pharmacokinetics. Therapeutic areas that have been targeted include anti-bacterial, metabolic, neurodegenerative, cardiovascular, anti-cancer and anti-viral. The centers work in a coordinated, interactive environment to affordably provide academic investigators with the technology, informatics and expertise necessary for successful drug discovery. This review provides an overview of these centers at the University of Michigan, along with case examples of successful collaborations with faculty.

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Year:  2014        PMID: 24409957      PMCID: PMC4166557          DOI: 10.2174/1386207317666140109121546

Source DB:  PubMed          Journal:  Comb Chem High Throughput Screen        ISSN: 1386-2073            Impact factor:   1.339


  113 in total

Review 1.  Antagonists of protein-protein interactions.

Authors:  A G Cochran
Journal:  Chem Biol       Date:  2000-04

Review 2.  Management of cardiac toxicity in patients receiving vascular endothelial growth factor signaling pathway inhibitors.

Authors:  Richard M Steingart; George L Bakris; Helen X Chen; Ming-Hui Chen; Thomas Force; S Percy Ivy; Carl V Leier; Glenn Liu; Daniel Lenihan; JoAnn Lindenfeld; Michael L Maitland; Scot C Remick; W H Wilson Tang
Journal:  Am Heart J       Date:  2012-02       Impact factor: 4.749

3.  Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia.

Authors:  Jolanta Grembecka; Shihan He; Aibin Shi; Trupta Purohit; Andrew G Muntean; Roderick J Sorenson; Hollis D Showalter; Marcelo J Murai; Amalia M Belcher; Thomas Hartley; Jay L Hess; Tomasz Cierpicki
Journal:  Nat Chem Biol       Date:  2012-01-29       Impact factor: 15.040

4.  Crystal structure of menin reveals binding site for mixed lineage leukemia (MLL) protein.

Authors:  Marcelo J Murai; Maksymilian Chruszcz; Gireesh Reddy; Jolanta Grembecka; Tomasz Cierpicki
Journal:  J Biol Chem       Date:  2011-07-13       Impact factor: 5.157

5.  Novel inhibitors of neurotropic alphavirus replication that improve host survival in a mouse model of acute viral encephalitis.

Authors:  Janice A Sindac; Bryan D Yestrepsky; Scott J Barraza; Kyle L Bolduc; Pennelope K Blakely; Richard F Keep; David N Irani; David J Miller; Scott D Larsen
Journal:  J Med Chem       Date:  2012-04-03       Impact factor: 7.446

6.  Cluster cytometry for high-capacity bioanalysis.

Authors:  Bruce S Edwards; Jingshu Zhu; Jun Chen; Mark B Carter; David M Thal; John J G Tesmer; Steven W Graves; Larry A Sklar
Journal:  Cytometry A       Date:  2012-03-21       Impact factor: 4.355

Review 7.  Inhibitors of the anti-apoptotic Bcl-2 proteins: a patent review.

Authors:  Naval Bajwa; Chenzhong Liao; Zaneta Nikolovska-Coleska
Journal:  Expert Opin Ther Pat       Date:  2011-12-23       Impact factor: 6.674

8.  Inhibitor of streptokinase gene expression improves survival after group A streptococcus infection in mice.

Authors:  Hongmin Sun; Yuanxi Xu; Izabela Sitkiewicz; Yibao Ma; Xixi Wang; Bryan D Yestrepsky; Yuping Huang; Martian C Lapadatescu; Martha J Larsen; Scott D Larsen; James M Musser; David Ginsburg
Journal:  Proc Natl Acad Sci U S A       Date:  2012-02-13       Impact factor: 11.205

9.  Complementary cell-based high-throughput screens identify novel modulators of the unfolded protein response.

Authors:  Andrew M Fribley; Patricia G Cruz; Justin R Miller; Michael U Callaghan; Peter Cai; Neha Narula; Richard R Neubig; Hollis D Showalter; Scott D Larsen; Paul D Kirchhoff; Martha J Larsen; Douglas A Burr; Pamela J Schultz; Renju R Jacobs; Giselle Tamayo-Castillo; David Ron; David H Sherman; Randal J Kaufman
Journal:  J Biomol Screen       Date:  2011-08-15

10.  Eukaryotic initiation factor-4E in superficial and muscle invasive bladder cancer and its correlation with vascular endothelial growth factor expression and tumour progression.

Authors:  J P Crew; S Fuggle; R Bicknell; D W Cranston; A de Benedetti; A L Harris
Journal:  Br J Cancer       Date:  2000-01       Impact factor: 7.640

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  4 in total

Review 1.  Targeting protein-protein interactions in hematologic malignancies: still a challenge or a great opportunity for future therapies?

Authors:  Tomasz Cierpicki; Jolanta Grembecka
Journal:  Immunol Rev       Date:  2015-01       Impact factor: 12.988

2.  HTS Identification of Activators and Inhibitors of Endoplasmic Reticulum (ER) Stress and the Unfolded Protein Response (UPR).

Authors:  Mehrnoosh Ghafouri; Chester B Gauss; Andrew M Fribley
Journal:  Methods Mol Biol       Date:  2022

3.  Borrelidin Induces the Unfolded Protein Response in Oral Cancer Cells and Chop-Dependent Apoptosis.

Authors:  Alpa Sidhu; Justin R Miller; Ashootosh Tripathi; Danielle M Garshott; Amy L Brownell; Daniel J Chiego; Carl Arevang; Qinghua Zeng; Leah C Jackson; Shelby A Bechler; Michael U Callaghan; George H Yoo; Seema Sethi; Ho-Sheng Lin; Joseph H Callaghan; Giselle Tamayo-Castillo; David H Sherman; Randal J Kaufman; Andrew M Fribley
Journal:  ACS Med Chem Lett       Date:  2015-09-08       Impact factor: 4.345

Review 4.  Discovery and resupply of pharmacologically active plant-derived natural products: A review.

Authors:  Atanas G Atanasov; Birgit Waltenberger; Eva-Maria Pferschy-Wenzig; Thomas Linder; Christoph Wawrosch; Pavel Uhrin; Veronika Temml; Limei Wang; Stefan Schwaiger; Elke H Heiss; Judith M Rollinger; Daniela Schuster; Johannes M Breuss; Valery Bochkov; Marko D Mihovilovic; Brigitte Kopp; Rudolf Bauer; Verena M Dirsch; Hermann Stuppner
Journal:  Biotechnol Adv       Date:  2015-08-15       Impact factor: 14.227

  4 in total

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