title: Synthesis and evaluation of a (68)Ga labeled folic acid derivative for targeting folate receptors.
abstract: Present work evaluates the potential of a newly synthesized (68)Ga-NOTA-folic acid conjugate for PET imaging of tumors over-expressing folate receptors (FRs). NOTA-folic acid conjugate was synthesized and characterized. It was radiolabeled with (68)Ga in ≥ 95% radiolabeling yields. In vitro cell binding studies showed a maximum cell uptake of 1.7±0.4% per million KB cells which was completely blocked on addition of cold folic acid showing specificity towards the FRs. However, further studies in tumor xenografts are warranted in order to assess the potential of (68)Ga-folic acid complex for imaging tumors over-expressing FRs.
authors: Isotope Production and Applications Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400085 India.
authors: Akanksha
authors: A
authors: Jain
authors: Radiopharmaceuticals Program, Board of Radiation and Isotope Technology, Navi Mumbai, 400703 India.
authors: Anupam
authors: A
authors: Mathur
authors: Isotope Production and Applications Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400085 India.
authors: Usha
authors: U
authors: Pandey
authors: Isotope Production and Applications Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400085 India.
authors: Jyotsna
authors: J
authors: Bhatt
authors: Isotope Production and Applications Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400085 India.
authors: Archana
authors: A
authors: Mukherjee
authors: Isotope Production and Applications Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400085 India.
authors: Ramu
authors: R
authors: Ram
authors: Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400085 India.
authors: Haladhar Dev
authors: HD
authors: Sarma
authors: Isotope Production and Applications Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400085 India. Electronic address: adash@barc.gov.in.
authors: Ashutosh
authors: A
authors: Dash
mesh_terms: D045744:Cell Line, Tumor; D002470:Cell Survival / Q000528:radiation effects; D058973:Folate Receptors, GPI-Anchored / Q000378:metabolism*; D005492:Folic Acid / Q000493:pharmacokinetics*; D005710:Gallium Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D007624:KB Cells; D058990:Molecular Targeted Therapy / Q000379:methods*; D009374:Neoplasms, Experimental / Q000378:metabolism* / Q000473:pathology / Q000532:radiotherapy*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000627:therapeutic use; D011878:Radiotherapy / Q000379:methods*; D016896:Treatment Outcome
chemical_list: D058973:Folate Receptors, GPI-Anchored; D005710:Gallium Radioisotopes; D019275:Radiopharmaceuticals; D005492:Folic Acid
keywords: Folate receptors; Folic acid; Gallium-68; NOTA-folic acid