EventsThe 2nd International Electronic Conference on Synthetic Organic Chemistry
Event submissions
Published
with-doi10.3390/ecsoc-2-01697
This submission belongs to the session c. Medicinal and Bioorganic Application of Organic Synthesis of the event The 2nd International Electronic Conference on Synthetic Organic Chemistry
Published date
01 Nov, 1998
Citation
Adam McCluskey, Mirella A. Keane, Alistair T. R. Sim, Jenette Sakoff, Cantharidin: The Next Generation. Towards Selective Inhibitors of Protein Phosphatase 1 and 2A, in Proceedings of The 2nd International Electronic Conference on Synthetic Organic Chemistry, 1 November–30 November 1998, MDPI: Basel, Switzerland, doi: 10.3390/ecsoc-2-01697
Share
Email
Facebook
Twitter
LinkedIn

Cantharidin: The Next Generation. Towards Selective Inhibitors of Protein Phosphatase 1 and 2A

Adam McCluskey 1
Mirella A. Keane 1
Alistair T. R. Sim 2
Jenette Sakoff 3
1. Department of Chemistry, The University of Newcastle, Callaghan, Newcastle 2308, Australia
2. Discipline of Medical Biochemistry, The University of Newcastle, Callaghan, Newcastle 2308, Australia
3. Medical Oncology, Newcastle Mater Misericordiae Hospital, Waratah, Newcastle 2301, Australia.
Abstract
Reversible protein phosphorylation plays a pivotal role in cellular signal transduction, moderating such diverse functions as neurotransmission, muscle contraction, glycogen synthesis, T-cell activation and cell proliferation.1-5 Serin/threonine phosphatases, which are responsible for protein dephosphorylation. Of the serine/threonine phosphatases, protein phosphatases 1 and 2A (PP1 and PP2A, respectively) share sequence identity between both enzyme subunits (50% for residues 23-292; 43% overall), are present in all eukarytoic cells and are together responsible for 90% of all cellular dephosphorylation. An interesting link between PP1 and PP2A is their shared sensitivity towards a structurally diverse family of natural products: the okadaic acid (1) class of compounds.
Keywords
n/a
RGD Mimetics : Building a Model of RGD Peptidomimetics with Comfa and Comparison with Catalyst
Dansyl-labeled heterobifunctional crosslinker with NHS-ester and protected sulfhydryl groups