User profiles for N. Manevski
Nenad ManevskiDMPK/PD Project Lead at Roche Verified email at roche.com Cited by 946 |
Metabolism by aldehyde oxidase: drug design and complementary approaches to challenges in drug discovery
… Imipramine N-oxide and nicotinamide N-oxide were reduced to imipramine and nicotinamide,
respectively, under anaerobic conditions by liver cytosol of rabbits, rats, mice, hamsters, …
respectively, under anaerobic conditions by liver cytosol of rabbits, rats, mice, hamsters, …
Glucocorticoids promote breast cancer metastasis
MMS Obradović, B Hamelin, N Manevski, JP Couto… - Nature, 2019 - nature.com
… n = 88 metastases; n = 7 bone metastases among the 88 metastases in total. Pearson
correlation. b, Flow cytometry analysis of levels of ROR1 in tumours and matched metastases of …
correlation. b, Flow cytometry analysis of levels of ROR1 in tumours and matched metastases of …
Discovery of an MLLT1/3 YEATS domain chemical probe
…, G Farnie, J Heer, N Manevski… - Angewandte Chemie …, 2018 - Wiley Online Library
… -cyclopropyl indazole analogue, compound 94, designed to improve pharmacokinetics,
largely mitigates N dealkylation observed and retains potent binding activity (MLLT1 K d 0.058 μ…
largely mitigates N dealkylation observed and retains potent binding activity (MLLT1 K d 0.058 μ…
Glucuronidation of psilocin and 4-hydroxyindole by the human UDP-glucuronosyltransferases
N Manevski, M Kurkela, C Höglund, T Mauriala… - Drug metabolism and …, 2010 - ASPET
We have examined the glucuronidation of psilocin, a hallucinogenic indole alkaloid, by the
19 recombinant human UDP-glucuronosyltransferases (UGTs) of subfamilies 1A, 2A, and 2B. …
19 recombinant human UDP-glucuronosyltransferases (UGTs) of subfamilies 1A, 2A, and 2B. …
Computational predictions of nonclinical pharmacokinetics at the drug design stage
…, T Schindler, N Manevski - Journal of Chemical …, 2023 - ACS Publications
… Thus, by sorting a set of predictions by their uncertainties and removing n-% of entries, we
expect that the overall prediction error of the subset will decrease. This is shown in Figure 6a …
expect that the overall prediction error of the subset will decrease. This is shown in Figure 6a …
A UGT2B10 splicing polymorphism common in african populations may greatly increase drug exposure
S Fowler, H Kletzl, M Finel, N Manevski… - … of Pharmacology and …, 2015 - ASPET
… , is mainly metabolized in humans by N-glucuronidation. Enzyme studies, using the (then) …
compound, particularly when there is a possibility of N-glucuronidation. Moreover, this study …
compound, particularly when there is a possibility of N-glucuronidation. Moreover, this study …
Phase II metabolism in human skin: skin explants show full coverage for glucuronidation, sulfation, N-acetylation, catechol methylation, and glutathione conjugation
N Manevski, P Swart, KK Balavenkatraman… - Drug Metabolism and …, 2015 - ASPET
Although skin is the largest organ of the human body, cutaneous drug metabolism is often
overlooked, and existing experimental models are insufficiently validated. This proof-of-…
overlooked, and existing experimental models are insufficiently validated. This proof-of-…
Can we predict clinical pharmacokinetics of highly lipophilic compounds by integration of machine learning or in vitro data into physiologically based models? A …
N Parrott, N Manevski… - Molecular …, 2022 - ACS Publications
While high lipophilicity tends to improve potency, its effects on pharmacokinetics (PK) are
complex and often unfavorable. To predict clinical PK in early drug discovery, we built human …
complex and often unfavorable. To predict clinical PK in early drug discovery, we built human …
Bovine serum albumin decreases Km values of human UDP-glucuronosyltransferases 1A9 and 2B7 and increases Vmax values of UGT1A9
N Manevski, PS Moreolo, J Yli-Kauhaluoma… - Drug metabolism and …, 2011 - ASPET
The human UDP-glucuronosyltransferase (UGT) enzymes UGT1A9 and UGT2B7 play
important roles in the hepatic glucuronidation of many drugs. The presence of bovine serum …
important roles in the hepatic glucuronidation of many drugs. The presence of bovine serum …
Evaluation of in vitro models for assessment of human intestinal metabolism in drug discovery
…, A Kotian, M Penney, S Shah, N Manevski - Drug Metabolism and …, 2020 - ASPET
… All incubations were performed in at least two replications (n = 2−6), with midazolam as a …
The f u,inc values were measured by RED for all test compounds (n = 32) in permeabilized …
The f u,inc values were measured by RED for all test compounds (n = 32) in permeabilized …