Synthesis, Radiolabeling and Biological Evaluation of a Neutral Tripeptide and its Derivatives for Potential Nuclear Medicine Applications
IR@IICB: CSIR-Indian Institute of Chemical Biology, Kolkata
View Archive Info| Field | Value | |
| Title |
Synthesis, Radiolabeling and Biological Evaluation of a Neutral Tripeptide and its Derivatives for Potential Nuclear Medicine Applications
|
|
| Creator |
Chandra, Susmita
De, Kakali Ganguly, Santanu Sarkar, Bhart Misra, Mridula |
|
| Subject |
Chemistry
|
|
| Description |
Peptides are important regulators of growth and cellular functions not only in normal tissue but also in
tumors. So they are becoming radioligands of increasing interest in nuclear oncology for targeted tumor
diagnosis and therapy. So development of new peptide radiopharmaceuticals is becoming one of the
most important areas in nuclear medicine research. A small tripeptide derivative NH2PhePheCys was
synthesized by Fmoc solid phase peptide synthesis using an automated synthesizer. The oxidized form,
i.e. NH2PhePheCysCysPhePheNH2, was also prepared by iodine oxidation method from NH2PhePhe-
Cys(ACM). The ligands were analyzed by HPLC and mass spectroscopy. They were radiolabeled with
99mTc using SnCl2. In vitro analytical studies and biological characterizations were performed using the
peptide radiopharmaceuticals. Images taken under gamma camera showed very high uptake in the liver,
lung and spleen. Significant uptake was also observed in bone marrow and brain for 99mTc-
NH2PhePheCys. Metabolites were produced in vivo when the radiopharmaceuticals were injected
intravenously and were identified from rat brain and liver homogenate studies. Clearance through
kidney did not show any evidence of breaking of the labeled compounds and formation of free 99mTc.
Radiopharmaceuticals prepared using tripeptide and hexapeptide ligands were transported into the
brain through blood brain barrier depending on the size and sequence characteristics. Using this
property of peptide new derivatives can be prepared to develop 99mTc radiopharmaceuticals for imaging
normal brain tissues as well as for diagnosing various brain disorders.
|
|
| Date |
2009
|
|
| Type |
Article
PeerReviewed |
|
| Format |
application/pdf
|
|
| Identifier |
http://www.eprints.iicb.res.in/958/1/3_peptides_2009.pdf
Chandra, Susmita and De, Kakali and Ganguly, Santanu and Sarkar, Bhart and Misra, Mridula (2009) Synthesis, Radiolabeling and Biological Evaluation of a Neutral Tripeptide and its Derivatives for Potential Nuclear Medicine Applications. Peptides, 30 (12). pp. 2399-2408. |
|
| Relation |
http://dx.doi.org/10.1016/j.peptides.2009.08.015
http://www.eprints.iicb.res.in/958/ |
|