18 research outputs found
Secreted frizzled related protein 2 protects cells from apoptosis by blocking the effect of canonical Wnt3a
Testiranje baza podataka je nezastupljen dio testiranja softvera koji uključuje strukturalno, funkcionalno i nefunkcionalno testiranje. Strukturalno testiranje je strukturalna provjera svih komponenata baze podataka koji nisu vidljivi krajnjim korisnicima (sheme, pohranjene procedure, pogledi, okidači i sl.). Funkcionalno se testiranje bavi provjerom funkcionalnosti tih istih komponenata, najčešće usporedbom izlaznih podataka s očekivanima. Dok se funkcionalno testiranje bavi provjerama koje ispituju funkcionira li nešto, nefunkcionalno se bavi provjerama koje ispituju koliko dobro nešto funkcionira. Takve provjere uključuju, na primjer, testiranje baze podataka pod opterećenjem i pronalazak granice zatajenja. Alati za testiranje baza podataka ne dijele se u iste kategorije kao i testiranja, ali se prema svojim funkcionalnostima u njih mogu smjestiti. Dostupni komercijalni alati i besplatni alati otvorenog koda se koriste u većini testnih slučajeva, no u nekim se scenarijima jednostavno koriste alati koji se već ionako koriste za upravljanje bazom podataka. Za dizajniranje kvalitetnih testova, tester mora biti upoznat sa strukturom baze podataka, funkcionalnostima aplikacije izgrađene na toj bazi podataka, ali i mora imati mnoštvo iskustva. Testiranje baza podataka potrebno za svaki projekt, a pogotovo za opsežne projekte velikih tvrtki
Discovery of Potent and Selective Urea-Based ROCK Inhibitors and Their Effects on Intraocular Pressure in Rats
A series of urea-based Rho kinase (ROCK) inhibitors were designed and evaluated. The discovered compounds had excellent enzyme and cellular potency, high kinase selectivity, high aqueous solubility, good porcine corneal penetration, and appropriate DMPK profiles for topical applications as antiglaucoma therapeutics
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Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors
Rho kinase (ROCK) is a promising drug target for the treatment of many diseases including hypertension, multiple sclerosis, cancer, and glaucoma. The structure-activity relationships (SAR) around a series of tetrahydroisoquinolines were evaluated utilizing biochemical and cell-based assays to measure ROCK inhibition. These novel ROCK inhibitors possess high potency, high selectivity, and appropriate pharmacokinetic properties for glaucoma applications. The lead compound, 35, had subnanomolar potency in enzyme ROCK-II assays as well as excellent cell-based potency (IC(50) = 51 nM). In a kinase panel profiling, 35 had an off-target hit rate of only 1.6% against 442 kinases. Pharmacology studies showed that compound 35 was efficacious in reducing intraocular pressure (IOP) in rats with reasonably long duration of action. These results suggest that compound 35 may serve as a promising agent for further development in the treatment of glaucoma