Literature DB >> 19919087

Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.

Patrick R Verhoest1, Caroline Proulx-Lafrance, Michael Corman, Lois Chenard, Christopher J Helal, Xinjun Hou, Robin Kleiman, Shenping Liu, Eric Marr, Frank S Menniti, Christopher J Schmidt, Michelle Vanase-Frawley, Anne W Schmidt, Robert D Williams, Frederick R Nelson, Kari R Fonseca, Spiros Liras.   

Abstract

By use of chemical enablement and prospective design, a novel series of selective, brain penetrant PDE9A inhibitors have been identified that are capable of producing in vivo elevations of brain cGMP.

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Year:  2009        PMID： 19919087     DOI： 10.1021/jm9015334

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


  12 in total

Review 1.  Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.

Authors:  Roland E Dolle; Bertrand Le Bourdonnec; Karin Worm; Guillermo A Morales; Craig J Thomas; Wei Zhang
Journal:  J Comb Chem       Date:  2010-10-05

2.  Structural Asymmetry of Phosphodiesterase-9A and a Unique Pocket for Selective Binding of a Potent Enantiomeric Inhibitor.

Authors:  Manna Huang; Yongxian Shao; Jianying Hou; Wenjun Cui; Beibei Liang; Yingchun Huang; Zhe Li; Yinuo Wu; Xinhai Zhu; Peiqing Liu; Yiqian Wan; Hengming Ke; Hai-Bin Luo
Journal:  Mol Pharmacol       Date:  2015-08-27       Impact factor: 4.436

3.  Quick Building Blocks (QBB): An Innovative and Efficient Business Model To Speed Medicinal Chemistry Analog Synthesis.

Authors:  Christopher J Helal; Mark Bundesmann; Susan Hammond; Melissa Holmstrom; Jacquelyn Klug-McLeod; Bruce A Lefker; Dale McLeod; Chakrapani Subramanyam; Oleg Zakaryants; Sylvie Sakata
Journal:  ACS Med Chem Lett       Date:  2019-07-05       Impact factor: 4.345

4.  Genome-wide association study of monoamine metabolite levels in human cerebrospinal fluid.

Authors:  J J Luykx; S C Bakker; E Lentjes; M Neeleman; E Strengman; L Mentink; J DeYoung; S de Jong; J H Sul; E Eskin; K van Eijk; J van Setten; J E Buizer-Voskamp; R M Cantor; A Lu; M van Amerongen; E P A van Dongen; P Keijzers; T Kappen; P Borgdorff; P Bruins; E M Derks; R S Kahn; R A Ophoff
Journal:  Mol Psychiatry       Date:  2013-01-15       Impact factor: 15.992

Review 5.  Animal models of Alzheimer disease.

Authors:  Frank M LaFerla; Kim N Green
Journal:  Cold Spring Harb Perspect Med       Date:  2012-11-01       Impact factor: 6.915

6.  Review: Modulation of striatal neuron activity by cyclic nucleotide signaling and phosphodiesterase inhibition.

Authors:  Sarah Threlfell; Anthony R West
Journal:  Basal Ganglia       Date:  2013-12-01

7.  Purification and Characterization of RhoPDE, a Retinylidene/Phosphodiesterase Fusion Protein and Potential Optogenetic Tool from the Choanoflagellate Salpingoeca rosetta.

Authors:  Lindsey B Lamarche; Ramasamy P Kumar; Melissa M Trieu; Erin L Devine; Luke E Cohen-Abeles; Douglas L Theobald; Daniel D Oprian
Journal:  Biochemistry       Date:  2017-10-18       Impact factor: 3.162

8.  Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent.

Authors:  Yong-xian Shao; Manna Huang; Wenjun Cui; Ling-Jun Feng; Yinuo Wu; Yinghong Cai; Zhe Li; Xinhai Zhu; Peiqing Liu; Yiqian Wan; Hengming Ke; Hai-Bin Luo
Journal:  J Med Chem       Date:  2014-12-08       Impact factor: 7.446

9.  Structure-based discovery of highly selective phosphodiesterase-9A inhibitors and implications for inhibitor design.

Authors:  Fei Meng; Jing Hou; Yong-Xian Shao; Pei-Ying Wu; Manna Huang; Xinhai Zhu; Yonghong Cai; Zhe Li; Jie Xu; Peiqing Liu; Hai-Bin Luo; Yiqian Wan; Hengming Ke
Journal:  J Med Chem       Date:  2012-10-01       Impact factor: 7.446

10.  Computational Study on Selective PDE9 Inhibitors on PDE9-Mg/Mg, PDE9-Zn/Mg, and PDE9-Zn/Zn Systems.

Authors:  Dakshinamurthy Sivakumar; Sathishkumar Mudedla; Seonghun Jang; Hyunjun Kim; Hyunjin Park; Yonwon Choi; Joongyo Oh; Sangwook Wu
Journal:  Biomolecules       Date:  2021-05-10
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