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Synthesis, Biological Evaluation, and Molecular Modeling of Natural and Unnatural Flavonoidal Alkaloids, Inhibitors of Kinases

Related publications (36)

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Unexpected Off-Targets and Paradoxical Pathway Activation by Kinase Inhibitors

Oliver Hantschel

Protein kinase inhibitors are an increasingly important class of targeted anticancer therapeutics. More than two dozen new drugs of this class have entered routine clinical use over the past decade. This review article focuses on how the development of met ...

2015

In this issue of Structure, Lisa et al. (2015) examine how the PknG protein kinase of M. tuberculosis efficiently binds and phosphorylates substrates. The work highlights interesting parallels between PknG and eukaryotic protein kinases. ...

Elsevier2015

Systematic lipidomic analysis of yeast protein kinase and phosphatase mutants reveals novel insights into regulation of lipid homeostasis

Fabrice David, Howard Riezman, Manuele Piccolis

The regulatory pathways required to maintain eukaryotic lipid homeostasis are largely unknown. We developed a systematic approach to uncover new players in the regulation of lipid homeostasis. Through an unbiased mass spectrometry-based lipidomic screening ...

Amer Soc Cell Biology2014

MAP Kinase Phosphatase 1 (MKP-1/DUSP1) Is Neuroprotective in Huntington's Disease via Additive Effects of JNK and p38 Inhibition

Darlene Goldstein, Meredith Dixon

We previously demonstrated that sodium butyrate is neuroprotective in Huntington's disease (HD) mice and that this therapeutic effect is associated with increased expression of mitogen-activated protein kinase/dual-specificity phosphatase 1 (MKP-1/DUSP1). ...

Soc Neuroscience2013

Phosphorylation of 4E-BP1 in the Mammalian Brain Is Not Altered by LRRK2 Expression or Pathogenic Mutations

Liliane Glauser, Elpida Tsika, Darren Moore, Klodjan Stafa, Alzbeta Trancikova

Mutations in the leucine-rich repeat kinase 2 (LRRK2) gene are a common cause of autosomal dominant familial Parkinson's disease (PD). LRRK2 encodes a multi-domain protein containing GTPase and kinase enzymatic domains. Disease-associated mutations in LRRK ...

Public Library of Science2012

The kinome of the human malaria parasite Plasmodium falciparum comprises representatives of most eukaryotic protein kinase groups, including kinases which regulate proliferation and differentiation processes. Despite extensive research on most plasmodial e ...

Wiley-Blackwell2011

Exploration of signaling cycles using dynamic optimization

Dominique Bonvin, Vassily Hatzimanikatis, Benoît Chachuat, Andrijana Radivojevic

One of the basic characteristics of every living system is the ability to respond to extracellular signals. This is carried out through a limited number of protein-based signaling networks, whose function is not based only on simple transmission of the rec ...

2010

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2010

GTPase Activity Plays a Key Role in the Pathobiology of LRRK2

Darren Moore

Mutations in the leucine-rich repeat kinase 2 (LRRK2) gene are associated with late-onset, autosomal-dominant, familial Parkinson's disease (PD) and also contribute to sporadic disease. The LRRK2 gene encodes a large protein with multiple domains, includin ...

Public Library of Science2010

Parasite Protein Kinases: At Home and Abroad

Two studies identify protein kinases of parasitic protists with roles in either their own development or the control of the behavior of their host cell. ...

2010