Literature DB >> 18054229

Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.

Zhijian Zhao1, Ronald G Robinson, Stanley F Barnett, Deborah Defeo-Jones, Raymond E Jones, George D Hartman, Hans E Huber, Mark E Duggan, Craig W Lindsley.   

Abstract

This letter describes the development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved aqueous solubility (approximately 18 mg/mL) that translates into enhanced cell activity and caspase-3 induction.

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Year:  2007        PMID： 18054229     DOI： 10.1016/j.bmcl.2007.11.015

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  19 in total

Review 1.  Inhibition of Akt with small molecules and biologics: historical perspective and current status of the patent landscape.

Authors:  Margrith E Mattmann; Sydney L Stoops; Craig W Lindsley
Journal:  Expert Opin Ther Pat       Date:  2011-06-02       Impact factor: 6.674

2.  Akt-dependent and isoform-specific regulation of dopamine transporter cell surface expression.

Authors:  Nicole K Speed; Heinrich J G Matthies; J Phillip Kennedy; Roxanne A Vaughan; Jonathan A Javitch; Scott J Russo; Craig W Lindsley; Kevin Niswender; Aurelio Galli
Journal:  ACS Chem Neurosci       Date:  2010-05-25       Impact factor: 4.418

3.  Partial Loss of the Glutamate Transporter GLT-1 Alters Brain Akt and Insulin Signaling in a Mouse Model of Alzheimer's Disease.

Authors:  Kole D Meeker; James S Meabon; David G Cook
Journal:  J Alzheimers Dis       Date:  2015       Impact factor: 4.472

4.  Loss of Akt1 in mice increases energy expenditure and protects against diet-induced obesity.

Authors:  Min Wan; Rachael M Easton; Catherine E Gleason; Bobby R Monks; Kohjiro Ueki; C Ronald Kahn; Morris J Birnbaum
Journal:  Mol Cell Biol       Date:  2011-10-28       Impact factor: 4.272

5.  α-Lipoic acid interaction with dopamine D2 receptor-dependent activation of the Akt/GSK-3β signaling pathway induced by antipsychotics: potential relevance for the treatment of schizophrenia.

Authors:  Jessica Deslauriers; Christian Desmarais; Philippe Sarret; Sylvain Grignon
Journal:  J Mol Neurosci       Date:  2012-09-14       Impact factor: 3.444

6.  Multidimensional Screening and Methodology Development for Condensations Involving Complex 1,2-Diketones.

Authors:  John R Goodell; Bo Leng; Tracy K Snyder; Aaron B Beeler; John A Porco
Journal:  Synthesis (Stuttg)       Date:  2010-07-01       Impact factor: 3.157

7.  AKT kinase activity is required for lithium to modulate mood-related behaviors in mice.

Authors:  Jen Q Pan; Michael C Lewis; Josh K Ketterman; Elizabeth L Clore; Misha Riley; Keenan R Richards; Erin Berry-Scott; Xiulin Liu; Florence F Wagner; Edward B Holson; Rachael L Neve; Travis L Biechele; Randall T Moon; Edward M Scolnick; Tracey L Petryshen; Stephen J Haggarty
Journal:  Neuropsychopharmacology       Date:  2011-03-09       Impact factor: 7.853

Review 8.  Targeting Pyk2 for therapeutic intervention.

Authors:  Christopher A Lipinski; Joseph C Loftus
Journal:  Expert Opin Ther Targets       Date:  2010-01       Impact factor: 6.902

9.  Structural conservation in band 4.1, ezrin, radixin, moesin (FERM) domains as a guide to identify inhibitors of the proline-rich tyrosine kinase 2.

Authors:  Nathalie Meurice; Lei Wang; Christopher A Lipinski; Zhongbo Yang; Christopher Hulme; Joseph C Loftus
Journal:  J Med Chem       Date:  2010-01-28       Impact factor: 7.446

10.  Factor XII and uPAR upregulate neutrophil functions to influence wound healing.

Authors:  Evi X Stavrou; Chao Fang; Kara L Bane; Andy T Long; Clément Naudin; Erdem Kucukal; Agharnan Gandhi; Adina Brett-Morris; Michele M Mumaw; Sudeh Izadmehr; Alona Merkulova; Cindy C Reynolds; Omar Alhalabi; Lalitha Nayak; Wen-Mei Yu; Cheng-Kui Qu; Howard J Meyerson; George R Dubyak; Umut A Gurkan; Marvin T Nieman; Anirban Sen Gupta; Thomas Renné; Alvin H Schmaier
Journal:  J Clin Invest       Date:  2018-01-29       Impact factor: 14.808
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