Thursday, August 01, 2019 6:27:44 PM
Well looks like another crack at $7 is tomorrow
Brian D Gray at Molecular Targeting Technologies even knows how vital PS Targeting is and how many at Molecular Targeting Technologies have had their emails monitored with the IP espionage clearly have impacted PS Targeting
Again, no mention of Oncologie Inc here... how many new CDMO contracts are tied to PS Targeting ?
https://www.sbir.gov/sbirsearch/detail/1465077
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Linker Optimization and Therapeutic Evaluation of Phosphatidylserine-Targeting Zinc Dipicolylamine-based Drug Conjugates
Article in Journal of Medicinal Chemistry 62(13) · June 2019 with 4 Reads
DOI: 10.1021/acs.jmedchem.9b00173
Yu-Wei Liu
Yun-Yu Chen
Chia-Yu Hsu
Tai-Yu Chiu
Kuan-Liang Liu
Chen-Fu Lo
Ming-Yu Fang
Yu-Chen Huang
Teng-Kuang Yeh
Koon Pak at Molecular Targeting Technologies
Brian D Gray at molecular targeting technologies, inc
Tsu-An Hsu
Kuan-Hsun Huang at NHRI
Chuan Shih
Kak-Shan Shia
Chiung-Tong Chen at National Health Research Institutes
Lun Kelvin Tsou
Abstract
We report that compound 13, a novel phosphatidylserine-targeting zinc (II) dipicolylamine drug conjugate, readily triggers a positive feedback therapeutic loop through the in situ generation of phosphatidylserine at the tumor microenvironment. Linker modifications, pharmacokinetics profiling, in vivo anti-tumor studies, and microwestern array of treated-tumor tissues were employed to show this class of conjugates induced regeneration of apoptotic signals, which facilitated subsequent recruitment of the circulating conjugates through the zinc (II) dipicolylamine-phosphatidylserine association and resulted in compounding anti-tumor efficacy. Compared to the marketed compound 17, compound 13 not only induced regressions in colorectal and pancreatic tumor models, it also exhibited at least 5-fold enhancement in antitumor efficacy with only 40% of the drug employed during treatment, culminated a >12.5 fold increase in therapeutic potential. Our study discloses a chemically distinct apoptosis-targeting theranostic, with build-in complementary functional moieties between the targeting module and the drug mechanism, to expand the arsenal of antitumor therapy.
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