title: Utilization of a nitrobenzoxadiazole (NBD) fluorophore in the design of a Grb2 SH2 domain-binding peptide mimetic.
abstract: 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.
authors.affiliation: Laboratory of Medicinal Chemistry, CCR, NCI, NIH, Frederick, MD 21702, USA.
authors.forename: Zhen-Dan
authors.initials: ZD
authors.lastname: Shi
authors.forename: Rajeshri G
authors.initials: RG
authors.lastname: Karki
authors.forename: Shinya
authors.initials: S
authors.lastname: Oishi
authors.forename: Karen M
authors.initials: KM
authors.lastname: Worthy
authors.forename: Lakshman K
authors.initials: LK
authors.lastname: Bindu
authors.forename: Pathirage G
authors.initials: PG
authors.lastname: Dharmawardana
authors.forename: Marc C
authors.initials: MC
authors.lastname: Nicklaus
authors.forename: Donald P
authors.initials: DP
authors.lastname: Bottaro
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Fisher
authors.forename: Terrence R
authors.initials: TR
authors.lastname: Burke
mesh_terms: 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*
chemical_list: D048868:Adaptor Proteins, Signal Transducing; D005456:Fluorescent Dyes; D051380:GRB2 Adaptor Protein; D008024:Ligands; D010069:Oxadiazoles; D010455:Peptides