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From Proteopedia
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| + | -Ligand structures in complex with PRK1 may provide insights to dvelop PRK1 inhibitors | ||
| + | -Staurosporine, lestaurtinib and Ro-31-8220 inhibit PRK1 with IC50s of 2 nM, 27 nM and 9 nM, respectively consistent with known lit binding modes for ligand | ||
| + | -Prk1 expression levels correlate with gleason scores in prostate cancer | ||
| + | -tofacitinib (CP-690550) has extensive immunosuppressive activity | ||
| + | -Tofacitinib makes van der Waals interactions with the sidechain of Phe910 | ||
| + | -tofacitinib does displace another phenylalanine residue from the kinase active site | ||
| + | - tofacitinib-rheumatoid arthritis (RA) in the United States and Russia, and is being studied for treatment of psoriasis, inflammatory bowel disease, and other immunological diseases, as well as for the prevention of organ transplant rejection. | ||
<scene name='48/483882/Prk1_ligand/1'>TextToBeDisplayed</scene> | <scene name='48/483882/Prk1_ligand/1'>TextToBeDisplayed</scene> | ||
| + | <scene name='48/483882/Gly630633/1'>Gly 630 633</scene> | ||
==Quiz Question 1== | ==Quiz Question 1== | ||
Revision as of 17:08, 11 March 2015
| This Sandbox is Reserved from January 19, 2016, through August 31, 2016 for use for Proteopedia Team Projects by the class Chemistry 423 Biochemistry for Chemists taught by Lynmarie K Thompson at University of Massachusetts Amherst, USA. This reservation includes Sandbox Reserved 425 through Sandbox Reserved 439. |
'Protein kinase C related kinase/Tofacitinib (prostrate and ovarian cancer)-4OTI'
Contents |
Introduction
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Protein kinase C, an enzyme that is activated by the receptor-mediated hydrolysis of inositol phospholipids, relays information in the form of a variety of extracellular signals across the membrane to regulate many Ca2+-dependent processes. At an early phase of cellular responses, the enzyme appears to have a dual effect, providing positive forward as well as negative feedback controls over various steps of its own and other signaling pathways, such as the receptors that are coupled to inositol phospholipid hydrolysis and those of some growth factors. In biological systems, a positive signal is frequently followed by immediate negative feedback regulation. Such a novel role of this system seems to give a logical basis for clarifying the biochemical mechanism of signal transduction, and to add a new dimension essential to our understanding of cell-to-cell communication of the protein.
Overall Structure
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Binding Interactions
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Additional Features
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-Ligand structures in complex with PRK1 may provide insights to dvelop PRK1 inhibitors
-Staurosporine, lestaurtinib and Ro-31-8220 inhibit PRK1 with IC50s of 2 nM, 27 nM and 9 nM, respectively consistent with known lit binding modes for ligand
-Prk1 expression levels correlate with gleason scores in prostate cancer
-tofacitinib (CP-690550) has extensive immunosuppressive activity
-Tofacitinib makes van der Waals interactions with the sidechain of Phe910
-tofacitinib does displace another phenylalanine residue from the kinase active site
- tofacitinib-rheumatoid arthritis (RA) in the United States and Russia, and is being studied for treatment of psoriasis, inflammatory bowel disease, and other immunological diseases, as well as for the prevention of organ transplant rejection.
Quiz Question 1
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Quiz Question 2
|
See Also
Credits
Introduction - name of team member
Overall Structure - name of team member
Drug Binding Site - name of team member
Additional Features - name of team member
Quiz Question 1 - name of team member
Quiz Question 2 - name of team member
