129431-12-5Relevant articles and documents
Mitochondrial heat shock protein-guided photodynamic therapy
Thomas, Ajesh P.,Lee, An-Jung,Palanikumar,Jana, Batakrishna,Kim, Kibeom,Kim, Sangpil,Ok, Haewon,Seol, Jihoon,Kim, Dongseok,Kang, Byoung Heon,Ryu, Ja-Hyoung
, p. 12631 - 12634 (2019)
Mitochondria targeting sensitizers are continuing to gain importance in photodynamic therapy (PDT). Members of the 90 kDa heat shock protein (Hsp90) family, including TRAP1 (Hsp75), are overexpressed in cancer cells and help to control the antiapoptotic protein activity. The present work introduces an Hsp90 inhibitor-mitochondria targeting indocyanine dye conjugate (IR-PU) for high PDT efficacy.
Novel mTOR inhibitor compounds and the use thereof
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Paragraph 0130; 0134-0136, (2021/03/09)
The novel mTOR inhibitor compounds of the present invention are capable of selective drug delivery to bone and released slowly in bone for a long period of time. The present invention relates to a targeted compound linked to a mTOR inhibitory bone disease therapeutic agent.
Compound comprising Hsp90 inhibitor targeting mitochondria and pharmaceutical composition for photodynamic therapy comprising the compound
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, (2020/09/26)
The present invention relates to mitochondrial target Hsp90 inhibitor-based compounds and pharmaceutical compositions for photodynamic therapy comprising the same. According to the present invention, provided are compounds obtained by conjugating an indocyanine derivative and a purine derivative, a diastereomer thereof, or a pharmaceutically acceptable salt thereof. The present invention relates to compositions for photodynamic diagnosis, treatment or cancer treatment comprising the above compounds, diastereomer, and salt as active ingredients.
Design, Synthesis, and Evaluation of Lipopeptide Conjugates of Mercaptoundecahydrododecaborate for Boron Neutron Capture Therapy
Isono, Aoi,Tsuji, Mieko,Sanada, Yu,Matsushita, Akari,Masunaga, Shinichiro,Hirayama, Tasuku,Nagasawa, Hideko
, (2019/03/07)
We developed new 10B carriers for boron neutron capture therapy (BNCT) that can effectively transport and accumulate boron clusters into cells. These carriers consist of a lipopeptide, mercaptoundecahydrododecaborate (BSH), and a disulfide linker. The carriers were conceived according to the structure of pepducin, a membrane-penetrating lipopeptide targeting protease-activated receptor 1 (PAR1). To improve the membrane permeability of BSH, the structure was optimized using various lipopeptides possessing different peptides and lipid moieties. These synthesized lipopeptides were conjugated with BSH and evaluated for intracellular uptake using T98G glioblastoma cells. Among them, the most effectively incorporated and accumulated in the cells was compound 5 a, which contains a peptide of 13 residues derived from the intracellular third loop of PAR1 and a palmitoyl group. For further improvement of 10B accumulation in cells, the introduction of an amine linker was investigated; intracellular uptake similar to that of 5 a was observed for compound 14, which has a piperazine linker. Both compounds 5 a and 14 showed a stronger radiosensitizing effect than BSH along on T98G cells under mixed-neutron beam irradiation. The results demonstrate that lipopeptide conjugation is effective for enhancing intracellular delivery and accumulation of BSH and improving the cytotoxic effect of BNCT.