848084-17-3Relevant academic research and scientific papers
Development of an effective fluorescence probe for discovery of aminopeptidase inhibitors to suppress biofilm formation
Zhao, Tianhu,Zhang, Jian,Tang, Maomao,Ma, Luyan Z.,Lei, Xiaoguang
, p. 461 - 468 (2019)
The human pathogen Pseudomonas aeruginosa can easily form biofilms. The extracellular matrix produced by the bacterial cells acts as a physical barrier to hinder the antibiotics treatment. It is necessary to destroy the biofilm in order to improve the eff
Dithiocarbamate prodrugs activated by prostate specific antigen to target prostate cancer
Bakthavatsalam, Subha,Franz, Katherine J.,George, Daniel J.,Wiangnak, Petpailin,Zhang, Tian
, (2020)
Disulfiram in conjunction with copper has been shown to be a potent anticancer agent. However, disulfiram's therapeutic potential in prostate cancer is hindered by off-target effects due to its reactive and nucleophilic thiol-containing component, diethyldithiocarbamate (DTC). To minimize undesirable reactivity, we have strategically blocked the thiol moiety in DTC with a cleavable p-aminobenzyl (pAB) group linked to peptide substrates recognized by prostate specific antigen (PSA). Here we report the synthesis and evaluation in cancer cell models of two PSA-activatable prodrugs: HPD (Ac-HSSKLQL-pAB-DTC and RPD (RSSYYSL-pAB-DTC). In vitro exposure to PSA was found to trigger activation of HPD and RPD to release diethyldithiocarbamate, and both prodrugs were found to induce toxicity in prostate cancer cells, with HPD showing the most promising selectivity. With copper supplementation, the IC50 of HPD was 1.4 μM in PSA-expressing LNCaP cells, and 11 μM in PC3 cells that do not express PSA. These studies demonstrate the utility of using peptide recognition handles to direct the activity of dithiocarbamate prodrugs for selective cytotoxicity of cancer cells.
CHEMILUMINESCENCE PROBES FOR TUBERCULOSIS
-
Paragraph 0062-0064; 0070, (2021/08/27)
The present invention provides turn- ON dioxetane-based chemiluminescence probes based on the Schapp's adamantylidene-dioxetane probe, which are useful for determining the presence, or measuring the level, of Mycobacterium tuberculosis (Mtb)- specific protease in a sample, and for assessing the susceptibility of said Mtb to an antibiotic drug.
Novel octapeptide-DTX prodrugs targeting MMP-7 as effective agents for the treatment of colorectal cancer with lower systemic toxicity
Hao, Yun-Peng,Liu, Zheng-Yu,Ning, Jin-Feng,Sun, Xun,Tang, Mei-Lin,Zhou, Lu
, (2020/03/23)
Colorectal cancer (CRC) is the third most common cancer and the fourth leading cause of cancer death around the world. The current treatments of CRC exhibited high occurrence rate of side effects. Docetaxel (DTX), an important drug widely used in cancer c
Polyene taxane targeted prodrug and its anti-colon cancer pharmaceutical use
-
Paragraph 0025; 0027; 0028; 0029, (2019/03/26)
The invention belongs to the field of biological medicine, in particular to a novel polyene taxane targeted prodrug and its medicinal use, the present invention provides includes the general formula (1) represented by the new polyene taxane targeted prodr
PROCHELATORS AS TARGETED PRODRUGS FOR PROSTATE CANCER AND METHODS OF MAKING AND USING SAME
-
Paragraph 00204-00205, (2019/01/21)
The present disclosure provides prochelators as targeted prodrugs for cancer, such as prostate cancer, and methods of making and using the same.
MMP-SENSITIVE TAXANE PRODRUG
-
Page/Page column 11; 12, (2017/07/08)
The present invention harnesses the differential expression of membrane-type matrix metalloproteinases (MT-MMPs) between human solid tumours and normal tissues to provide a systemically inactive prodrug which is selectively activated at the tumour micro-environment. The present invention provides a prodrug which is a conjugate of a taxane and a selective MT-MMP cleavable delivery vehicle.
POLYCONJUGATES FOR DELIVERY OF RNAI TRIGGERS TO TUMOR CELLS IN VIVO
-
Page/Page column 40, (2015/02/25)
The present invention is directed compositions for delivery of RNA interference (RNAi) triggers to integrin positive tumor cells in vivo. The compositions comprise RGD ligand- targeted amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or conjugate) are further covalently linked to an RNAi trigger.
COMPOUNDS CONTAINING MATRIX METALLOPROTEINASE SUBSTRATES AND METHODS OF THEIR USE
-
Page/Page column 114, (2008/06/13)
Compounds for use in a diagnostic agent for detecting, imaging, and/or monitoring a pathological disorder associated with matrix metalloproteinase activity at a site of interest in a patient are disclosed. Compositions and kits containing the compounds are also disclosed. In addition, methods of detecting, imaging, and/or monitoring the presence of matrix metalloproteinase or a pathological disorder associated with matrix metalloproteinase activity in a patient are disclosed.
