ac-his-dphe-arg-trp-nh2 and Skin-Neoplasms

ac-his-dphe-arg-trp-nh2 has been researched along with Skin-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for ac-his-dphe-arg-trp-nh2 and Skin-Neoplasms

Article	Year
Design, synthesis, and biological studies of efficient multivalent melanotropin ligands: tools toward melanoma diagnosis and treatment. Journal of medicinal chemistry, 2011, Oct-27, Volume: 54, Issue:20 To achieve early detection and specific cancer treatment, we propose the use of multivalent interactions in which a series of binding events leads to increased affinity and consequently to selectivity. Using melanotropin (MSH) ligands, our aim is to target melanoma cells which overexpress melanocortin receptors. In this study, we report the design and efficient synthesis of new trivalent ligands bearing MSH ligands. Evaluation of these multimers on a cell model engineered to overexpress melanocortin 4 receptors (MC4R) showed up to a 350-fold increase in binding compared to the monomer, resulting in a trivalent construct with nanomolar affinity starting from a micromolar affinity ligand. Cyclic adenosine monophosphate (cAMP) production was also investigated, leading to more insights into the effects of multivalent compounds on transduction mechanisms. Topics: Binding, Competitive; Cyclic AMP; Dendrimers; Drug Design; HEK293 Cells; Humans; Ligands; Melanocyte-Stimulating Hormones; Melanoma; Peptides; Receptor, Melanocortin, Type 4; Skin Neoplasms; Structure-Activity Relationship	2011

Article

Year

Design, synthesis, and biological studies of efficient multivalent melanotropin ligands: tools toward melanoma diagnosis and treatment.

Journal of medicinal chemistry, 2011, Oct-27, Volume: 54, Issue:20

To achieve early detection and specific cancer treatment, we propose the use of multivalent interactions in which a series of binding events leads to increased affinity and consequently to selectivity. Using melanotropin (MSH) ligands, our aim is to target melanoma cells which overexpress melanocortin receptors. In this study, we report the design and efficient synthesis of new trivalent ligands bearing MSH ligands. Evaluation of these multimers on a cell model engineered to overexpress melanocortin 4 receptors (MC4R) showed up to a 350-fold increase in binding compared to the monomer, resulting in a trivalent construct with nanomolar affinity starting from a micromolar affinity ligand. Cyclic adenosine monophosphate (cAMP) production was also investigated, leading to more insights into the effects of multivalent compounds on transduction mechanisms.

Topics: Binding, Competitive; Cyclic AMP; Dendrimers; Drug Design; HEK293 Cells; Humans; Ligands; Melanocyte-Stimulating Hormones; Melanoma; Peptides; Receptor, Melanocortin, Type 4; Skin Neoplasms; Structure-Activity Relationship

2011