Compound, process for its preparation, a pharmaceutical solution containing the compound, a method of determining the presence of cancer, a kit for cancer detection, and the use of hydrolysis of the compound for the detection of cancer
Inventors
LESNER, Adam • WYSOCKA, Magdalena • NIDZWORSKI, Dawid
Assignees
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Publication Number
US-10556925-B2
Publication Date
2020-02-11
Expiration Date
Abstract
The subject of the invention is a new compound of the following chemical formula: ABZ1-Dap(O2(Cbz))2-Dap(O1)3-Dap(O2)4-Arg5-ANB6-NH2 where: ABZ stands for 2-aminobenzoic acid; DAP stands for diaminopropanoic acid (Dap) derivatives, modified by the functionalised residues of mono-ethylene or diethylene glycol (PEG); ANB stands for 5-amino-2-nitrobenzoic acid The subject of the invention is a method for producing the new compound and a pharmaceutical solution for cancer detection, which contains the above-mentioned compound.The subject of the invention is a method for cancer detection through the in vitro analysis of a human urine sample to which a new compound is added and blended with a buffer of pH 7-9.The subject of the invention is also a kit for detecting cancer, in particular bladder cancer, and the use of hydrolysis of the new compound in the position no. 5 by proteasome 20s for cancer detection, in particular bladder cancer.
Core Innovation
The document discloses a specific peptidomimetic cancer-detection compound defined by the chemical formula ABZ-Dap(O2(Cbz))2-Dap(O1)3-Dap(O2)4-Arg-ANB-NH2, where ABZ is 2-aminobenzoic acid and ANB is 5-amino-2-nitrobenzoic acid. The Dap portion is described as diaminopropanoic acid (Dap) derivatives modified by functionalised mono-ethylene or diethylene glycol (PEG) residues.
The compound incorporates Arg at position 5 and an NH2 end group, and is configured for selective proteasome-dependent hydrolysis in a diagnostic workflow. The document further associates selectivity with proteasome 20S hydrolysis at a defined position and with the trypsin-like subunit PR671A, including use of proteasome-inhibited controls.
In addition to the compound itself, the document describes a pharmaceutical solution formulation containing the active substance and a buffer of pH 7-9. The described application workflow uses in vitro urine incubation and fluorescence readouts to obtain an analytical signal linked to proteasome 20S hydrolysis at the specified position.
Claims Coverage
The independent claims in the provided material cover 2 inventive features: the defined peptidomimetic compound and a cancer-detection method that relies on proteasome 20S hydrolysis and fluorescence readouts in urine. Across the claim family, the inventive features are centered on the compound’s ABZ/Dap(O1)/Dap(O2)/Arg/ANB-NH2 structure with PEG-functionalised Dap residues, and on assay behavior tied to selective proteasome activity at position 5, including PR671A-dependence.
Defined peptidomimetic compound with ABZ/Dap(O1)/Dap(O2)/Arg/ANB-NH2 structure and PEG-functionalised Dap residues
A compound having the chemical formula ABZ-Dap(O2(Cbz))2-Dap(O1)3-Dap(O2)4-Arg-ANB-NH2, where ABZ is 2-aminobenzoic acid; Dap denotes diaminopropanoic acid derivatives modified by functionalised mono-ethylene or diethylene glycol (PEG) residues; and ANB is 5-amino-2-nitrobenzoic acid.
The claim coverage is anchored on the explicitly defined peptidomimetic compound structure with PEG-modified Dap residues and the ABZ/Arg/ANB-NH2 arrangement, together with cancer detection based on proteasome 20S hydrolysis and fluorescence readouts in urine. Additional refinements mention PR671A-associated specificity and position 5 hydrolysis.
Stated Advantages
High specificity constant for cancer detection using the disclosed compound and workflow.
Detection at low proteasome levels.
Selectivity associated with proteasome 20S hydrolysis at position 5 and dependency on the trypsin-like subunit inhibitor PR671A.
Documented Applications
Cancer detection using in vitro urine incubation with fluorescence readouts after selective proteasome 20S hydrolysis at position 5 of the compound, including correlation with proteasome presence in bladder-cancer urine samples.
A test kit for detecting bladder cancer that includes the compound and an inhibitor of the trypsic subunit PR671A.
A pharmaceutical solution for cancer detection containing the active substance of the compound and a buffer having a pH of 7-9.
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