TY - JOUR
T1 - Studying protein-peptide interactions using benzophenone units
T2 - A case study of protein kinase B/Akt and its inhibitor PTR6154
AU - Tal-Gan, Yftah
AU - Naveh, Shirly
AU - Klein, Shoshana
AU - Moshel, Ofra
AU - Levitzki, Alexander
AU - Gilon, Chaim
PY - 2012/2/15
Y1 - 2012/2/15
N2 - Protein-protein interactions (PPIs) govern nearly all processes in living cells. Peptides play an important role in studying PPIs. Peptides carrying photoaffinity labels that covalently bind the interacting protein can be used to obtain more accurate information regarding PPIs. Benzophenone (BP) is a useful photoaffinity label that is widely used to study PPIs. We developed a one-pot two-step synthesis for the preparation of novel BP units. To map the binding site more thoroughly, linkers of various lengths were attached to the BP moiety. These units can be incorporated into peptide sequences using well-established solid phase peptide synthesis (SPPS) protocols. As a proof of concept, we studied the interaction between protein kinase B (PKB/Akt) and its synthetic peptide inhibitor, PTR6154. The methodology is general and can be implemented to study PPIs in a variety of biological systems.
AB - Protein-protein interactions (PPIs) govern nearly all processes in living cells. Peptides play an important role in studying PPIs. Peptides carrying photoaffinity labels that covalently bind the interacting protein can be used to obtain more accurate information regarding PPIs. Benzophenone (BP) is a useful photoaffinity label that is widely used to study PPIs. We developed a one-pot two-step synthesis for the preparation of novel BP units. To map the binding site more thoroughly, linkers of various lengths were attached to the BP moiety. These units can be incorporated into peptide sequences using well-established solid phase peptide synthesis (SPPS) protocols. As a proof of concept, we studied the interaction between protein kinase B (PKB/Akt) and its synthetic peptide inhibitor, PTR6154. The methodology is general and can be implemented to study PPIs in a variety of biological systems.
KW - Benzophenone
KW - Peptidomimetic
KW - Protein kinase B (PKB/Akt)
KW - Protein-protein interaction
KW - Solid phase peptide synthesis (SPPS)
UR - http://www.scopus.com/inward/record.url?scp=84859705578&partnerID=8YFLogxK
U2 - 10.1016/j.ab.2011.11.032
DO - 10.1016/j.ab.2011.11.032
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C2 - 22197420
AN - SCOPUS:84859705578
SN - 0003-2697
VL - 421
SP - 750
EP - 754
JO - Analytical Biochemistry
JF - Analytical Biochemistry
IS - 2
ER -