Synthesis and preclinical investigation of Tc-p-SCN-Bzl-DTPA-cetuximab for targeting EGFR using head and neck squamous cell carcinoma (HNSCC) xenografts.

To assess the preclinical potential of technetium-99m labelled conjugated para-isothiocyanato-benzyl diethylene triamine penta-acetic acid cetuximab (Tc-p-SCN-Bzl-DTPA cetuximab) for imaging EGFR in HNSCC mice and rabbits xenografts. Cetuximab, a chimeric monoclonal antibody targeting EGFR, was conjugated with p-SCN-Bzl-DTPA followed by labelling with Tc. The labelled conjugate was evaluated for in vitro stability in cysteine at 37 °C.

Imaging prostate cancer (PCa) with [ Tc(CO) ]finasteride dithiocarbamate.

This investigation aimed to modify finasteride (1) to finasteride dithiocarbamate (2) for subsequent synthesis of the rhenium analogue (3) and [ Tc]tricarbonyl complexes (4), to assess its prostate cancer (PCa) targeting potential in a rat model. To validate the identity of (4), reference (3) has been synthesized by using fac-[Net ] [ReBr (CO) ] precursor and characterized by H-NMR, C-NMR, ESI-MS, and elemental analysis. The analogue (4) was synthesized by using fac-[ Tc(H O) (CO) ] precursor, and its structure was confirmed by comparative HPLC by using (3) as a reference.

Phosphorylation sites of HER2/c-erbB-2: role in cell growth and in disease.

The protein kinase c-erbB-2 belongs to the family of receptor tyrosine kinase and is involved in oncogenesis. The present study predicts different phosphorylation sites of HER2/c-erbB-2 which are important in preventing or developing cancer, especially breast cancer. Sequence homology showed highest homology (77%) with epidermal growth factor receptor kinase domain.

Modeling the mutational effects on calmodulin structure: prediction of alteration in the amino acid interactions.

Calmodulin (CaM) is a highly conserved 17kDa eukaryotic protein that can bind specifically to over 100 protein targets in response to a Ca2+ signal. Present study was planned to mutate the crucial residues of N-terminal lobe, central helix, and C-terminal lobe that play important roles in activating and binding of enzymes. In all, 10 mutations were carried out in the predicted 3D structure of calmodulin using the computer program MODELLER 6v2.