Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0022716 (
Menkes
)
1,057
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
We present the synthesis and characterization of octaarginine-conjugated Copper-Gad-2 (Arg
8
CG2
), a new copper-responsive magnetic resonance imaging (MRI) contrast agent that combines a Gd
3+
-DO3A scaffold with a thioether-rich receptor for copper recognition. The inclusion of a polyarginine appendage leads to a marked increase in cellular uptake compared to previously reported MRI-based copper sensors of the CG family. Arg
8
CG2
exhibits a 220% increase in relaxivity (
r
1
= 3.9 to 12.5 mM
-1
s
-1
) upon 1 : 1 binding with Cu
+
, with a highly selective response to Cu
+
over other biologically relevant metal ions. Moreover, Arg
8
CG2
accumulates in cells at nine-fold greater concentrations than the parent
CG2
lacking the polyarginine functionality and is retained well in the cell after washing.
In cellulo
relaxivity measurements and
T
1
-weighted phantom images using a
Menkes disease
model cell line demonstrate the utility of Arg
8
CG2
to report on biological perturbations of exchangeable copper pools.
...
PMID:A cell-permeable gadolinium contrast agent for magnetic resonance imaging of copper in a Menkes disease model. 2543 49
