Department of Pharmacology, Institute of Chemical Biology and Fundamental Medicine, Novosibirsk, Russia
Research Article
Development of Theranostics Albumin Auristatin Conjugates for Combining Chemotherapy with Boron Neutron Capture Therapy
Author(s): Meiling Wang, Ivan A. Moskalev, Olga D. Zakharova, Anna I. Kasatova, Vladimir N. Silnikov, Tatyana V. Popova* and Tatyana S. Godovikova*
Combining boron neutron capture therapy with chemotherapy can provide good therapy efficacy and is of great relevance today. In this study, we focused on serum albumin, a well-known drug delivery system, and developed homocysteine-functionalized boron albumin conjugate with chemotherapeutic molecules (monomethyl auristatin E, MMAE and auristatin F, MMAF). The new N-acylated homocysteine thiolactone bearing a cobalt bis (dicarbollide) derivative was used to create the fluorophorealbumin based construct. We report on the synthesis of a fluorophorelabeled boron-homocystamide conjugates of human serum albumin and their use in thiol-‘click’ chemistry to prepare a novel multifunctional constructs with the antitubulin agents MMAE or MMAF. We demonstrate that boron-equipped albumin conjugate with MMAE was more potent than MMAF conjugate, in the killing tumor cells. The half-maxi.. View More»
DOI:
10.35248/2322-3308-13.1.007
