scholarly journals Development and Application of Chymase Inhibitors: Development of a Chymase Inhibitor: Pharmacological Characterization of a Chymase Inhibitor in Inflamed Tissue Remodeling and Fibrosis

2002 ◽  
Vol 90 (3) ◽  
pp. 206-209 ◽  
Author(s):  
Masatoshi Nakajima ◽  
Noriyuki Naya
Keyword(s):  
Tissue Remodeling ◽  
Pharmacological Characterization ◽  
Chymase Inhibitor ◽  
Inflamed Tissue

Pharmacological characterization of Tibouchina granulosa

Planta Medica ◽  
2014 ◽  
Vol 80 (16) ◽  
Author(s):  
CC Guilhon ◽  
A Minho ◽  
AS Barros ◽  
PD Fernandes
Keyword(s):  
Pharmacological Characterization

Molecular and Pharmacological Characterization of Hamster HCA1 and HCA2

2016 ◽  
Vol 16 (1) ◽  
pp. 61-69
Author(s):  
Chester Kuei ◽  
Grace Lee ◽  
Victory Joseph ◽  
Jing Qian ◽  
Jingwen Yang ◽  
...  
Keyword(s):  
Pharmacological Characterization

Electrophysiological and pharmacological characterization of a novel and potent neuronal Kv7 channel opener SCR2682 for antiepilepsy

2019 ◽  
Vol 33 (8) ◽  
pp. 9154-9166 ◽  
Author(s):  
Fan Zhang ◽  
Yani Liu ◽  
Feng Tang ◽  
Bo Liang ◽  
Huanming Chen ◽  
...  
Keyword(s):  
Pharmacological Characterization ◽  
Channel Opener

Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H2R and D3R

2021 ◽  
Vol 214 ◽  
pp. 113190
Author(s):  
Sabrina Biselli ◽  
Merlin Bresinsky ◽  
Katharina Tropmann ◽  
Lisa Forster ◽  
Claudia Honisch ◽  
...  
Keyword(s):  
Pharmacological Characterization

scholarly journals Molecular and Pharmacological Characterization of the Interaction between Human Geranylgeranyltransferase Type I and Ras-Related Protein Rap1B

2021 ◽  
Vol 22 (5) ◽  
pp. 2501
Author(s):  
Sonja Hinz ◽  
Dominik Jung ◽  
Dorota Hauert ◽  
Hagen S. Bachmann
Keyword(s):  
Protein Function ◽  
Tumor Development ◽  
Cysteine Residue ◽  
Type I ◽  
Pharmacological Characterization ◽  
Anti Cancer ◽  
And Function ◽  
Caax Motif ◽  
Important Drug

Geranylgeranyltransferase type-I (GGTase-I) represents an important drug target since it contributes to the function of many proteins that are involved in tumor development and metastasis. This led to the development of GGTase-I inhibitors as anti-cancer drugs blocking the protein function and membrane association of e.g., Rap subfamilies that are involved in cell differentiation and cell growth. In the present study, we developed a new NanoBiT assay to monitor the interaction of human GGTase-I and its substrate Rap1B. Different Rap1B prenylation-deficient mutants (C181G, C181S, and ΔCQLL) were designed and investigated for their interaction with GGTase-I. While the Rap1B mutants C181G and C181S still exhibited interaction with human GGTase-I, mutant ΔCQLL, lacking the entire CAAX motif (defined by a cysteine residue, two aliphatic residues, and the C-terminal residue), showed reduced interaction. Moreover, a specific, peptidomimetic and competitive CAAX inhibitor was able to block the interaction of Rap1B with GGTase-I. Furthermore, activation of both Gαs-coupled human adenosine receptors, A2A (A2AAR) and A2B (A2BAR), increased the interaction between GGTase-I and Rap1B, probably representing a way to modulate prenylation and function of Rap1B. Thus, A2AAR and A2BAR antagonists might be promising candidates for therapeutic intervention for different types of cancer that overexpress Rap1B. Finally, the NanoBiT assay provides a tool to investigate the pharmacology of GGTase-I inhibitors.

Pharmacological characterization of receptor guanylyl cyclase reporter cell lines

2013 ◽  
Vol 698 (1-3) ◽  
pp. 131-136 ◽  
Author(s):  
Frank Wunder ◽  
Annette Woermann ◽  
Andreas Geerts ◽  
Markus Milde
Keyword(s):  
Cell Lines ◽  
Guanylyl Cyclase ◽  
Reporter Cell ◽  
Pharmacological Characterization
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