Abstract:
:G protein-coupled receptor kinase 2 (GRK2) plays a central role in the cellular transduction network. In particular, during chronic heart failure GRK2 is upregulated and believed to contribute to disease progression. Thereby, its inhibition offers a potential therapeutic solution to several pathological conditions. In the present study, we performed a SAR study and a NMR conformational analysis of peptides derived from HJ loop of GRK2 and able to selectively inhibit GRK2. From Ala-scan and D-Ala point replacement, we found that Arg residues don't affect the inhibitory properties, while a D-amino acid at position 5 is key to the activity. Conformational analysis identified two β-turns that involve N-terminal residues, followed by a short extended region. These information can help the design of peptides and peptido-mimetics with enhanced GRK2 inhibition properties.
journal_name
Biopolymersjournal_title
Biopolymersauthors
Gomez-Monterrey I,Carotenuto A,Cipolletta E,Sala M,Vernieri E,Limatola A,Bertamino A,Musella S,Grieco P,Trimarco B,Novellino E,Iaccarino G,Campiglia Pdoi
10.1002/bip.22295subject
Has Abstractpub_date
2014-01-01 00:00:00pages
121-8issue
1eissn
0006-3525issn
1097-0282journal_volume
101pub_type
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