Utilization of a nitrobenzoxadiazole (NBD) fluorophore in the design of a Grb2 SH2 domain-binding peptide mimetic.
Fluorescence labeling has become a general technique for studying the intracellular accumulation and localization of exogenously administered materials. Reported herein is a low nanomolar affinity Grb2 SH2 domain-binding antagonist that utilizes the environmentally-sensitive nitrobenzoxadiazole (NBD) fluorophore as a naphthyl replacement. This novel agent should serve as a useful tool to visualize the actions of this class of Grb2 SH2 domain-binding antagonists in whole cell systems.
Shi
Zhen-Dan
ZD
Laboratory of Medicinal Chemistry, CCR, NCI, NIH, Frederick, MD 21702, USA.
Karki
Rajeshri G
RG
Oishi
Shinya
S
Worthy
Karen M
KM
Bindu
Lakshman K
LK
Dharmawardana
Pathirage G
PG
Nicklaus
Marc C
MC
Bottaro
Donald P
DP
Fisher
Robert J
RJ
Burke
Terrence R
TR
D048868:Adaptor Proteins, Signal Transducing / Q000037:antagonists & inhibitors*; D001667:Binding, Competitive; D015195:Drug Design; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000737:chemistry*; D051380:GRB2 Adaptor Protein; D008024:Ligands; D008968:Molecular Conformation; D018716:Molecular Mimicry; D010069:Oxadiazoles / Q000138:chemical synthesis / Q000737:chemistry*; D010455:Peptides / Q000737:chemistry* / Q000494:pharmacology*; D011485:Protein Binding / Q000187:drug effects; D013194:Staining and Labeling / Q000379:methods; D013329:Structure-Activity Relationship; D018909:src Homology Domains / Q000187:drug effects*
D048868:Adaptor Proteins, Signal Transducing; D005456:Fluorescent Dyes; D051380:GRB2 Adaptor Protein; D008024:Ligands; D010069:Oxadiazoles; D010455:Peptides