Small Molecular Probes for G-Protein-Coupled C5a Receptors:  Conformationally Constrained Antagonists Derived from the C Terminus of the Human Plasma Protein C5a

1998 ◽  
Vol 41 (18) ◽  
pp. 3417-3425 ◽  
Author(s):  
Allan K. Wong ◽  
Angela M. Finch ◽  
Gregory K. Pierens ◽  
David J. Craik ◽  
Stephen M. Taylor ◽  
...  
Keyword(s):  
Human Plasma ◽  
G Protein ◽  
Plasma Protein ◽  
Molecular Probes ◽  
Conformationally Constrained ◽  
Human Plasma Protein ◽  
C Terminus ◽  
C5a Receptors ◽  
G Protein Coupled

scholarly journals A western blot approach to detection of human plasma protein conjugates derived from D-penicillamine.

1994 ◽  
Vol 53 (4) ◽  
pp. 256-260 ◽  
Author(s):  
C A Laycock ◽  
M J Phelan ◽  
R C Bucknall ◽  
J W Coleman
Keyword(s):  
Western Blot ◽  
Human Plasma ◽  
Plasma Protein ◽  
Protein Conjugates ◽  
Human Plasma Protein

Heat Stable Human Plasma Protein Fractions Electrophoretically Rich in Albumin

Vox Sanguinis ◽  
1962 ◽  
Vol 7 (4) ◽  
pp. 406-413 ◽  
Author(s):  
E. H. Mealey ◽  
L. H. Larsen ◽  
R. C. Dwyer ◽  
D. J. Mulford
Keyword(s):  
Human Plasma ◽  
Plasma Protein ◽  
Protein Fractions ◽  
Human Plasma Protein ◽  
Heat Stable

scholarly journals Metabolism and disposition of pyrotinib in healthy male volunteers: covalent binding with human plasma protein

2018 ◽  
Vol 40 (7) ◽  
pp. 980-988 ◽  
Author(s):  
Jian Meng ◽  
Xiao-yun Liu ◽  
Sheng Ma ◽  
Hua Zhang ◽  
Song-da Yu ◽  
...  
Keyword(s):  
Human Plasma ◽  
Plasma Protein ◽  
Covalent Binding ◽  
Healthy Male ◽  
Human Plasma Protein ◽  
Healthy Male Volunteers ◽  
Male Volunteers

scholarly journals Yeast-Based Directed-Evolution For High-Throughput Structural Stabilization of G Protein-Coupled Receptors (GPCRs)

2021 ◽  
Author(s):  
May Meltzer ◽  
Zvagelsky Tatiana ◽  
Niv Papo ◽  
Stanislav Engel
Keyword(s):  
G Protein ◽  
Resistant Cell ◽  
Single Step ◽  
G Protein Coupled Receptors ◽  
Structural Basis ◽  
Diffusion Method ◽  
Structural Stabilization ◽  
C Terminus ◽  
Screening Platform ◽  
G Protein Coupled

Abstract The immense potential of G protein-coupled receptors (GPCRs) as targets for drug discovery is not fully realized due to the enormous difficulties associated with structure elucidation of these profoundly unstable membrane proteins. The existing methods of GPCR stability-engineering are cumbersome and low-throughput; in addition, the scope of GPCRs that could benefit from these techniques is limited. Here, we presented a yeast-based screening platform for a single-step isolation of GRCR variants stable in the presence of short-chain detergents, a feature essential for their successful crystallization using vapor diffusion method. The detergent-resistant cell wall of yeast provides a unique compartmentalization opportunity to physically link the receptor phenotype to its encoding DNA, and thus enable discovery of stable GPCR variants with unprecedent efficiency. The scope of mutations identified by the method offers important insights into the structural basis of GPCR stability, questioning the inherent instability of the GPCR scaffold, and revealing the potential role of the C-terminus in receptor stabilization.

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