PT  - JOURNAL ARTICLE
AU  - Wienhoff, Brieanne
AU  - Shaffer, Suzanne
AU  - Doll, Stephanie
AU  - Jurisson, Silvia
AU  - Brechbiel, M.
AU  - Nanda, Prasant
AU  - Jackson, Andrew
AU  - Smith, Charles
TI  - Development of site-directed radiopharmaceuticals for treatment of prostate cancer
DP  - 2011 May 01
TA  - Journal of Nuclear Medicine
PG  - 2456--2456
VI  - 52
IP  - supplement 1
4099  - http://jnm.snmjournals.org/content/52/supplement_1/2456.short
4100  - http://jnm.snmjournals.org/content/52/supplement_1/2456.full
SO  - J Nucl Med2011 May 01; 52
AB  - 2456 Objectives The goal of this research project was to create a site-directed radiopharmaceutical reagent of bismuth-213 (5.87, 5.55 MeV α, t1/2 =45.6 min) with high specificity and affinity for targeting and treatment of human prostate tumors. Methods We have designed a radiopharmaceutical conjugate of the formula [213Bi-CHXA-βala-BBN(7-14)] where CHXA = {[(R)-2-amino-3-(p-aminophenyl)propyl]-trans-(S,S)-cyclohexane-1,2-diamine-N,N,N',N'',N''-pentaacetic acid}, βala = β alanine, , and BBN(7-14) = bombesin peptide, synthesized using standard solid phase peptide synthesis techniques. Results Synthetic preparation of the non-metallated CHXA-βala-BBN(7-14) conjugates occurs with CHXA-NHS active ester and commercially available βala-BBN reagent using EDC (1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide) and NHS (N-hydroxysuccinimide). Purification occurs using RP-HPLC. Mass spectrometry results verified synthesis of our new peptide conjugate. Conclusions We are currently optimizing the synthesis of CHXA-βala-BBN and anticipate metallation with bismuth