scholarly journals Conformational Dynamics of a Regulator of G-Protein Signaling Protein Reveals a Mechanism of Allosteric Inhibition by a Small Molecule

2013 ◽  
Vol 8 (12) ◽  
pp. 2778-2784 ◽  
Author(s):  
Harish Vashisth ◽  
Andrew J. Storaska ◽  
Richard R. Neubig ◽  
Charles L. Brooks
Keyword(s):  
G Protein ◽  
Small Molecule ◽  
Conformational Dynamics ◽  
G Protein Signaling ◽  
Protein Signaling ◽  
Allosteric Inhibition ◽  
Signaling Protein

scholarly journals Interplay of cysteine exposure and global protein dynamics in small-molecule recognition by a regulator of G-protein signaling protein

2018 ◽  
Vol 87 (2) ◽  
pp. 146-156 ◽  
Author(s):  
Mohammadjavad Mohammadi ◽  
Hossein Mohammadiarani ◽  
Vincent S. Shaw ◽  
Richard R. Neubig ◽  
Harish Vashisth
Keyword(s):  
Protein Dynamics ◽  
G Protein ◽  
Small Molecule ◽  
G Protein Signaling ◽  
Protein Signaling ◽  
Signaling Protein ◽  
Molecule Recognition

scholarly journals Regulation of longevity by regulator of G-protein signaling protein, Loco

Aging Cell ◽  
2011 ◽  
Vol 10 (3) ◽  
pp. 438-447 ◽  
Author(s):  
Yuh-Ru Lin ◽  
Keetae Kim ◽  
Yanfei Yang ◽  
Andreas Ivessa ◽  
Junichi Sadoshima ◽  
...  
Keyword(s):  
G Protein ◽  
G Protein Signaling ◽  
Protein Signaling ◽  
Signaling Protein

scholarly journals Screen Targeting Lung and Prostate Cancer Oncogene Identifies Novel Inhibitors of RGS17 and Problematic Chemical Substructures

2018 ◽  
Vol 23 (4) ◽  
pp. 363-374 ◽  
Author(s):  
Christopher R. Bodle ◽  
Josephine H. Schamp ◽  
Joseph B. O’Brien ◽  
Michael P. Hayes ◽  
Meng Wu ◽  
...  
Keyword(s):  
G Protein ◽  
Small Molecule ◽  
High Throughput Screening ◽  
Biochemical Characterization ◽  
Parent Compound ◽  
Receptor Activation ◽  
G Protein Signaling ◽  
Conservation Of Resources ◽  
Protein Signaling ◽  
Rgs Protein

Regulator of G protein signaling (RGS) proteins temporally regulate heterotrimeric G protein signaling cascades elicited by G protein–coupled receptor activation and thus are essential for cell homeostasis. The dysregulation of RGS protein expression has been linked to several pathologies, spurring discovery efforts to identify small-molecule inhibitors of these proteins. Presented here are the results of a high-throughput screening (HTS) campaign targeting RGS17, an RGS protein reported to be inappropriately upregulated in several cancers. A screen of over 60,000 small molecules led to the identification of five hit compounds that inhibit the RGS17-Gαo protein-protein interaction. Chemical and biochemical characterization demonstrated that three of these hits inhibited the interaction through the decomposition of parent compound into reactive products under normal chemical library storage/usage conditions. Compound substructures susceptible to decomposition are reported and the decomposition process characterized, adding to the armamentarium of tools available to the screening field, allowing for the conservation of resources in follow-up efforts and more efficient identification of potentially decomposed compounds. Finally, analogues of one hit compound were tested, and the results establish the first ever structure-activity relationship (SAR) profile for a small-molecule inhibitor of RGS17.

scholarly journals 5-HT1A receptor-mediated phosphorylation of extracellular signal-regulated kinases (ERK1/2) is modulated by regulator of G protein signaling protein 19

2014 ◽  
Vol 26 (9) ◽  
pp. 1846-1852 ◽  
Author(s):  
Qin Wang ◽  
Akiko Terauchi ◽  
Christopher H. Yee ◽  
Hisashi Umemori ◽  
John R. Traynor
Keyword(s):  
G Protein ◽  
G Protein Signaling ◽  
Protein Signaling ◽  
Signaling Protein ◽  
Extracellular Signal

scholarly journals The human regulator of G-protein signaling protein 6 gene (RGS6) maps between markers WI-5202 and D14S277 on chromosome 14q24.3

1999 ◽  
Vol 44 (2) ◽  
pp. 138-140 ◽  
Author(s):  
Naohiko Seki ◽  
Atsushi Hattori ◽  
Akiko Hayashi ◽  
Sumie Kozuma ◽  
Tada-aki Hori ◽  
...  
Keyword(s):  
G Protein ◽  
G Protein Signaling ◽  
Protein Signaling ◽  
Signaling Protein

scholarly journals Regulator of G Protein Signaling Protein Suppression of Gαo Protein-Mediated α2A Adrenergic Receptor Inhibition of Mouse Hippocampal CA3 Epileptiform Activity

2009 ◽  
Vol 75 (5) ◽  
pp. 1222-1230 ◽  
Author(s):  
Brianna L. Goldenstein ◽  
Brian W. Nelson ◽  
Ke Xu ◽  
Elizabeth J. Luger ◽  
Jacquline A. Pribula ◽  
...  
Keyword(s):  
G Protein ◽  
Adrenergic Receptor ◽  
Epileptiform Activity ◽  
G Protein Signaling ◽  
Protein Signaling ◽  
Signaling Protein ◽  
Receptor Inhibition ◽  
Hippocampal Ca3

scholarly journals Expression of Regulator of G-Protein Signaling Protein-2 Gene in the Rat Ovary at the Time of Ovulation1

2000 ◽  
Vol 63 (5) ◽  
pp. 1513-1517 ◽  
Author(s):  
Takeshi Ujioka ◽  
Darryl L. Russell ◽  
Hitoshi Okamura ◽  
JoAnne S. Richards ◽  
Lawrence L. Espey
Keyword(s):  
G Protein ◽  
G Protein Signaling ◽  
Protein Signaling ◽  
Signaling Protein ◽  
Rat Ovary

scholarly journals Reversible, Allosteric Small-Molecule Inhibitors of Regulator of G Protein Signaling Proteins

2010 ◽  
Vol 78 (3) ◽  
pp. 524-533 ◽  
Author(s):  
Levi L. Blazer ◽  
David L. Roman ◽  
Alfred Chung ◽  
Martha J. Larsen ◽  
Benjamin M. Greedy ◽  
...  
Keyword(s):  
G Protein ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
G Protein Signaling ◽  
Signaling Proteins ◽  
Protein Signaling
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