Department of Pharmacology, Institute of Chemical Biology and Fundamental Medicine, SB RAS, 630090 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
