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US 2022/0175742 A1Published application
Collagen p4h1 inhibitor and its use
AssigneeUniversity of Kentucky Research Foundation
InventorsRen Xu, Shike Wang
Life of this patent
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Abstract
The present invention relates to a methods for modulating Collagen Prolyl 4-hydroxylase (C-P4H1) in a cell. The present invention further relates to methods for inhibiting a cancer cell. The instant invention also relates to methods for identifying modulators of Collagen Prolyl 4-hydroxylase (C-P4H1).
Claims16
A method of inhibiting a cancer cell, comprising:
- administering to the cancer cell an effective amount of a compound selected from the group consisting of:
- tripelennamine, fluvastatin, gabapentin, L-adrenaline, methacycline, fenfibrate, beclomethasone dipropionate, roflumilast, promethazine, ticlopidine, amifostine, dinaciclib, pramipexole, bromfenac, flavopiridol, flutamide, sitagiptin, racecadotril, vinblastine, salbutamol, pemetrexed, atovaquone, olanzapine, procainamide, bicalutamide, clindamycin, nafcillin, cysteamine, poziotinib, lomefloxacin, axitinib, valdecoxib, scopolamine, R-atenolol, sildosin, lamotrigine, levobetaxolol, bosentan, ledipasvir, pralatrexate, gabapentin, epinephrine, erlotinib, mesnex, rofecoxib, mezlocillin, serotonin, tranexamic acid, or combinations thereof.
A method of modulating collagen prolyl 4-hydroxylase (C-P4H1) in a cell, comprising:
- administering to the cell an effective amount of (a) a compound selected from the group consisting of:
- tripelennamine, fluvastatin, gabapentin, L-adrenaline, methacycline, fenfibrate, beclomethasone dipropionate, roflumilast, promethazine, ticlopidine, amifostine, dinaciclib, pramipexole, bromfenac, flavopiridol, flutamide, sitagiptin, racecadotril, vinblastine, salbutamol, pemetrexed, atovaquone, olanzapine, procainamide, bicalutamide, clindamycin, nafcillin, cysteamine, poziotinib, lomefloxacin, axitinib, valdecoxib, scopolamine, R-atenolol, sildosin, lamotrigine, levobetaxolol, bosentan, ledipasvir, pralatrexate, gabapentin, epinephrine, erlotinib, mesnex, rofecoxib, mezlocillin, serotonin, tranexamic acid, or combinations thereof;
- or (b) a compound selected from the group consisting of pimavanserin, modafinil, quinapril, rosiglitazone, sulconazole, GSK2126458, cinepazide, methylthiouracil, EPZ-6438, ethosuximide, roxithromycin, atorvastatin, penfluridol, lonafarnib, foscarnet, allylthiourea, halothane, milrinone, maprotiline, famotidine, L-thyroxine, tideglusib, moruisteine, guaifenesin, hydroquinone, nitrendipine, mecarbinate, pramoxine, buflomedil, evacetrapib, oxybutynin, flavoxate, or combinations thereof.
A method of screening for modulators of C-P4H1, comprising:
- (a) expressing a P4H1 complex in a eukaryotic cell;
- (b) purifying the P4H1 complex;
- (c) adding the purified P4H1 complex to a well of a high throughput assay plate;
- (d) adding peptide substrate GlyProProGlyOEt, FeSO4, catalase, ascorbate, and α-ketoglutarate to the well of the high throughput assay plate;
- (e) adding a test molecule or control to the well of the high throughput assay plate;
- (f) adding enzymes that convert succinate into ATP to the well of the high throughput assay plate;
- (g) adding luminescent enzymes that convert ATP into light energy to the well of the high throughput assay plate;
- (h) measuring luminescence of the well of the high throughput assay plate;
- and
- (i) identifying a molecule as a modulator of P4H1 when the molecule increases luminescence of the well relative to negative control or decreases luminescence of the well relative to positive control.
7 more elements
Dependencies are inferred from the claim text.