| 词条 | Trodusquemine |
| 释义 |
| drug_name = | INN = | type = | IUPAC_name = [(3R,6R)-6-[(3S,5R,7R,8R,9S,10S,13R,14S,17R)-3-[3-[4-(3-Aminopropylamino)butylamino]propylamino]-7-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-methylheptan-3-yl] hydrogen sulfate | image = Trodusquemine.svg | alt = | caption = | pronounce = | tradename = | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_AU_comment = | pregnancy_US = | pregnancy_category= | routes_of_administration = | legal_AU = | legal_AU_comment = | legal_BR = | legal_BR_comment = | legal_CA = | legal_DE = | legal_NZ = | legal_UK = | legal_US = | legal_UN = | legal_status = | bioavailability = | protein_bound = | metabolism = | metabolites = | onset = | elimination_half-life = | duration_of_action = | excretion = | CAS_number = 186139-09-3 | class = | ATCvet = | ATC_prefix = | ATC_suffix = | PubChem = 9917968 | ChemSpiderID = 8093615 | DrugBank = DB06333 | UNII = KKC12PIF16 |KEGG=D06252 |ChEMBL=508583 | synonyms = MSI-1436, produlestan[1] | C=37|H=72|N=4|O=5|S=1 | StdInChI=1S/C37H72N4O5S/c1-26(2)34(46-47(43,44)45)13-10-27(3)30-11-12-31-35-32(15-17-37(30,31)5)36(4)16-14-29(24-28(36)25-33(35)42)41-23-9-22-40-20-7-6-19-39-21-8-18-38/h26-35,39-42H,6-25,38H2,1-5H3,(H,43,44,45)/t27-,28-,29+,30-,31+,32+,33-,34-,35+,36+,37-/m1/s1 | StdInChIKey = WUJVPODXELZABP-FWJXURDUSA-N | smiles=C[C@H](CC[C@H](C(C)C)OS(=O)(=O)O)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2[C@@H](C[C@@H]4[C@@]3(CC[C@@H](C4)NCCCNCCCCNCCCN)C)O)C }}Trodusquemine is an aminosterol (a polyamine-steroid) similar to squalamine that is an allosteric inhibitor of PTP1B.[1][2] It was isolated from the dogfish shark by scientists at Magainin Pharmaceuticals (subsequently called Genaera) in 2000 and underwent some drug development as a potential treatment for diabetes or obesity, but the company ran out of money and closed in 2009.[3][1][4] Trodusquemine and some other drug assets were sold to Ohr Pharmaceutical for $200,000 by Genaera's liquidator.[5] In 2014 a company called Depymed was formed based on work done on PTP1B inhibitors at Cold Spring Harbor Laboratory, and it licensed rights to troduscemine from Ohr; Depymed wanted to develop it for HER2-positive breast cancer.[6] As of 2017 Depymed was running a Phase I trial of the drug.[3] Coronary Heart DiseaseBritish Heart Foundation trials using mice with atherosclerosis which were conducted at the University of Aberdeen suggests a link between atherosclerosis and insulin resistance due to impaired insulin receptor (IR) signalling. Inhibiting the activity of protein tyrosine phosphatase 1B (PTPN1), which is the major negative regulator of the insulin receptor appeared to inhibit atherosclerotic plaque formation. The trial mice reportedly had less fatty plaques in their arteries following a single dose of Trodusquemine.[7] References1. ^1 {{cite web |url=https://www.acs.org/content/acs/en/molecule-of-the-week/archive/t/trodusquemine.html |title=Molecule of the Week: Trodusquemine |date=April 13, 2015 |publisher=American Chemical Society }} 2. ^{{cite journal|last1=Cho|first1=H|title=Protein tyrosine phosphatase 1B (PTP1B) and obesity.|journal=Vitamins and hormones|date=2013|volume=91|pages=405-24|doi=10.1016/B978-0-12-407766-9.00017-1|pmid=23374726}} 3. ^1 2 {{cite web|title=Trodusquemine|url=http://adisinsight.springer.com/drugs/800009018|publisher=AdisInsight|accessdate=16 January 2018|language=en}} 4. ^{{cite news|last1=George|first1=John|title=Biotech Genaera shutting down: Never brought drug to market|url=https://www.bizjournals.com/philadelphia/stories/2009/04/27/daily31.html|work=Philadelphia Business Journal|date=April 29, 2009}} 5. ^{{cite web|title=Ohr Pharmaceutical 10-K for the fiscal year ended September 30, 2009|url=https://www.sec.gov/Archives/edgar/data/1173281/000135448810000035/ohrp_10k.htm|publisher=Ohr via SEC Edgar|page=11|date=January 8, 2010}} 6. ^{{cite news|title=Clinical trials for DepYMed|url=http://www.innovateli.com/clinical-trials-for-depymed/|work=Innovate Long Island|date=17 March 2015}} 7. ^`http://www.clinsci.org/content/ppclinsci/early/2017/09/11/CS20171066.full.pdf Pharmacological inhibition of protein tyrosine phosphatase 1B (PTP1B) protects against atherosclerotic plaque formation in the LDLR-/-mouse model of atherosclerosis. (Clinical science DOI10. 1024/CS217 1066) 5 : Experimental drugs|Enzyme inhibitors|Organosulfates|Polyamines|Cholestanes |
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