title: ⁹⁹mTc-HYNIC-MPG: a novel SPECT probe for targeting mutated EGFR.
abstract: Mutated epidermal growth factor receptor (EGFR) is an important biomarker for cancer diagnosis and molecular target for many anticancer drugs. Localizing EGFR and evaluating EGFR mutational status can help to identify patients who are potentially the most suitable ones for targeted treatments. Hence, we developed a novel EGFR tyrosine kinase inhibitor labeled with (99m)Tc ((99m)Tc-HYNIC-MPG) and evaluated its EGFR binding capacity in vitro and in vivo. This molecular probe was synthesized by one-step method that is simple and highly efficient. Importantly, the uptake rate for (99m)Tc-HYNIC-MPG in the liver was as low as 28.44 ± 0.15% (mean ± SD, n=3). This finding presents for the first time that (99m)Tc-HYNIC-MPG can bind to mutated EGFR efficiently and thus provides a novel molecular tool to detect mutated EGFR and suppress tumorigenesis.
authors.affiliation: Department of Radiology, The Fourth Hospital of Harbin Medical University, 37 Yiyuan Street, Nangang District, Harbin 150001, PR China; Molecular Imaging Center of Harbin Medical University, 37 Yiyuan Street, Nangang District, Harbin 150001, PR China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Yan
authors.affiliation: Department of Radiology, The Fourth Hospital of Harbin Medical University, 37 Yiyuan Street, Nangang District, Harbin 150001, PR China; Molecular Imaging Center of Harbin Medical University, 37 Yiyuan Street, Nangang District, Harbin 150001, PR China.
authors.forename: Zun-Yu
authors.initials: ZY
authors.lastname: Xiao
authors.affiliation: Department of Radiology, The Fourth Hospital of Harbin Medical University, 37 Yiyuan Street, Nangang District, Harbin 150001, PR China; Molecular Imaging Center of Harbin Medical University, 37 Yiyuan Street, Nangang District, Harbin 150001, PR China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Song
authors.affiliation: Department of Radiology, The Fourth Hospital of Harbin Medical University, 37 Yiyuan Street, Nangang District, Harbin 150001, PR China; Molecular Imaging Center of Harbin Medical University, 37 Yiyuan Street, Nangang District, Harbin 150001, PR China.
authors.forename: Zhao-Ting
authors.initials: ZT
authors.lastname: Kang
authors.affiliation: Molecular Imaging Center of Harbin Medical University, 37 Yiyuan Street, Nangang District, Harbin 150001, PR China.
authors.forename: Ping
authors.initials: P
authors.lastname: Wang
authors.affiliation: Department of Radiology, The Fourth Hospital of Harbin Medical University, 37 Yiyuan Street, Nangang District, Harbin 150001, PR China; Molecular Imaging Center of Harbin Medical University, 37 Yiyuan Street, Nangang District, Harbin 150001, PR China.
authors.forename: Xi-Lin
authors.initials: XL
authors.lastname: Sun
authors.affiliation: Department of Radiology, The Fourth Hospital of Harbin Medical University, 37 Yiyuan Street, Nangang District, Harbin 150001, PR China; Molecular Imaging Center of Harbin Medical University, 37 Yiyuan Street, Nangang District, Harbin 150001, PR China. Electronic address: shenbzh@vip.sina.com.
authors.forename: Bao-Zhong
authors.initials: BZ
authors.lastname: Shen
mesh_terms: D000818:Animals; D002460:Cell Line; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000235:genetics; D005260:Female; D006801:Humans; D051379:Mice; D008815:Mice, Inbred Strains; D057054:Molecular Imaging; D015335:Molecular Probes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D009154:Mutation; D015609:Organotechnetium Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: C000603603:99mTc-HYNIC-MPG; D015335:Molecular Probes; D015609:Organotechnetium Compounds; D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D019275:Radiopharmaceuticals; C512478:EGFR protein, human; D066246:ErbB Receptors
keywords: (99m)Tc; EDDA; EGFR mutation; HYNIC-MPG; Tricine