title: Using "On/Off" (19)F NMR/Magnetic Resonance Imaging Signals to Sense Tyrosine Kinase/Phosphatase Activity in Vitro and in Cell Lysates.
abstract: Tyrosine kinase and phosphatase are two important, antagonistic enzymes in organisms. Development of noninvasive approach for sensing their activity with high spatial and temporal resolution remains challenging. Herein, we rationally designed a hydrogelator Nap-Phe-Phe(CF3)-Glu-Tyr-Ile-OH (1a) whose supramolecular hydrogel (i.e., Gel 1a) can be subjected to tyrosine kinase-directed disassembly, and its phosphate precursor Nap-Phe-Phe(CF3)-Glu-Tyr(H2PO3)-Ile-OH (1b), which can be subjected to alkaline phosphatase (ALP)-instructed self-assembly to form supramolecular hydrogel Gel 1b, respectively. Mechanic properties and internal fibrous networks of the hydrogels were characterized with rheology and cryo transmission electron microscopy (cryo-TEM). Disassembly/self-assembly of their corresponding supramolecular hydrogels conferring respective "On/Off" (19)F NMR/MRI signals were employed to sense the activity of these two important enzymes in vitro and in cell lysates for the first time. We anticipate that our new (19)F NMR/magnetic resonance imaging (MRI) method would facilitate pharmaceutical researchers to screen new inhibitors for these two enzymes without steric hindrance.
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, Hefei Science Center CAS, Department of Chemistry, University of Science and Technology of China , Hefei, Anhui 230026, China.
authors.forename: Zhen
authors.initials: Z
authors.lastname: Zheng
authors.affiliation: High Magnetic Field Laboratory, Hefei Institutes of Physical Science, Chinese Academy of Sciences , Hefei, Anhui 230031, China.
authors.forename: Hongbin
authors.initials: H
authors.lastname: Sun
authors.affiliation: High Magnetic Field Laboratory, Hefei Institutes of Physical Science, Chinese Academy of Sciences , Hefei, Anhui 230031, China.
authors.forename: Chen
authors.initials: C
authors.lastname: Hu
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, Hefei Science Center CAS, Department of Chemistry, University of Science and Technology of China , Hefei, Anhui 230026, China.
authors.forename: Gongyu
authors.initials: G
authors.lastname: Li
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, Hefei Science Center CAS, Department of Chemistry, University of Science and Technology of China , Hefei, Anhui 230026, China.
authors.forename: Xiaomei
authors.initials: X
authors.lastname: Liu
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, Hefei Science Center CAS, Department of Chemistry, University of Science and Technology of China , Hefei, Anhui 230026, China.
authors.forename: Peiyao
authors.initials: P
authors.lastname: Chen
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, Hefei Science Center CAS, Department of Chemistry, University of Science and Technology of China , Hefei, Anhui 230026, China.
authors.forename: Yusi
authors.initials: Y
authors.lastname: Cui
authors.affiliation: High Magnetic Field Laboratory, Hefei Institutes of Physical Science, Chinese Academy of Sciences , Hefei, Anhui 230031, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Liu
authors.affiliation: High Magnetic Field Laboratory, Hefei Institutes of Physical Science, Chinese Academy of Sciences , Hefei, Anhui 230031, China.
authors.forename: Junfeng
authors.initials: J
authors.lastname: Wang
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, Hefei Science Center CAS, Department of Chemistry, University of Science and Technology of China , Hefei, Anhui 230026, China.
authors.forename: Gaolin
authors.initials: G
authors.lastname: Liang
mesh_terms: D005461:Fluorine / Q000737:chemistry*; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy / Q000379:methods*; D010744:Phosphoric Monoester Hydrolases / Q000378:metabolism*; D011505:Protein-Tyrosine Kinases / Q000378:metabolism*
chemical_list: D005461:Fluorine; D011505:Protein-Tyrosine Kinases; D010744:Phosphoric Monoester Hydrolases