Search Results - "Masimirembwa, Collen M"

Inhibition of major drug metabolizing CYPs by common herbal medicines used by HIV/AIDS patients in Africa-- implications for herb-drug interactions by Awortwe, Charles, Bouic, Patrick J, Masimirembwa, Collen M, Rosenkranz, Bernd

“…The purpose of this study was to evaluate the potential risk of common herbal medicines used by HIV-infected patients in Africa for herb-drug interactions…”
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The Molecular Basis of CYP2D6-Mediated N-Dealkylation: Balance between Metabolic Clearance Routes and Enzyme Inhibition by BONN, Britta, MASIMIREMBWA, Collen M, ARISTEI, Yasmin, ZAMORA, Ismael

“…N -Dealkylation is a commonly observed metabolic reaction for drugs containing secondary and tertiary amines. On searching the literature, it is obvious that…”
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Exploration of Catalytic Properties of CYP2D6 and CYP3A4 Through Metabolic Studies of Levorphanol and Levallorphan by Britta Bonn, Collen M. Masimirembwa, Neal Castagnoli, Jr

“…CYP2D6 and CYP3A4, two members of the cytochrome P450 superfamily of monooxygenases, mediate the biotransformation of a variety of xenobiotics. The two enzymes…”
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In Vitro and in Silico Identification and Characterization of Thiabendazole as a Mechanism-Based Inhibitor of CYP1A2 and Simulation of Possible Pharmacokinetic Drug-Drug Interactions by THELINGWANI, Roslyn S, ZVADA, Simbarashe P, DOLGOS, Hugues, UNGELL, Anna-Lena B, MASIMIREMBWA, Collen M

“…Thiabendazole (TBZ) and its major metabolite 5-hydroxythiabendazole (5OH-TBZ) were screened for potential time-dependent inhibition (TDI) against CYP1A2…”
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Application of Higher Throughput Screening (HTS) Inhibition Assays to Evaluate the Interaction of Antiparasitic Drugs with Cytochrome P450s by BAPIRO, Tashinga E, EGNELL, Ann-Charlotte, HASLER, Julia A, MASIMIREMBWA, Collen M

“…In this study we have evaluated the application and reliability of using fluorescence (FLUO)-based high throughput screening assays with recombinant CYPs…”
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Warfarin Pharmacogenomics for Precision Medicine in Real-Life Clinical Practice in Southern Africa: Harnessing 73 Variants in 29 Pharmacogenes by Muyambo, Sarudzai, Ndadza, Arinao, Soko, Nyarai D, Kruger, Bianca, Kadzirange, Gerard, Chimusa, Emile, Masimirembwa, Collen M, Ntsekhe, Mpiko, Nhachi, Charles F B, Dandara, Collet

“…Pharmacogenomics is universally relevant for worldwide modern therapeutics and yet needs further development in resource-limited countries. While there is an…”
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Discriminant and quantitative PLS analysis of competitive CYP2C9 inhibitors versus non-inhibitors using alignment independent GRIND descriptors by Afzelius, Lovisa, Masimirembwa, Collen M, Karlén, Anders, Andersson, Tommy B, Zamora, Ismael

“…This study describes the use of alignment-independent descriptors for obtaining qualitative and quantitative predictions of the competitive inhibition of…”
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Antimalarial benzoheterocyclic 4-aminoquinolines: Structure–activity relationship, in vivo evaluation, mechanistic and bioactivation studies by Ongarora, Dennis S.B., Strydom, Natasha, Wicht, Kathryn, Njoroge, Mathew, Wiesner, Lubbe, Egan, Timothy J., Wittlin, Sergio, Jurva, Ulrik, Masimirembwa, Collen M., Chibale, Kelly

“…[Display omitted] A novel class of benzoheterocyclic analogues of amodiaquine designed to avoid toxic reactive metabolite formation was synthesized and…”
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STRUCTURAL ANALYSIS OF CYP2C9 AND CYP2C5 AND AN EVALUATION OF COMMONLY USED MOLECULAR MODELING TECHNIQUES by AFZELIUS, Lovisa, RAUBACHER, Florian, KARLEN, Anders, JØRGENSEN, Flemming Steen, ANDERSSON, Tommy B, MASIMIREMBWA, Collen M, ZAMORA, Ismael

“…This work had two separate aims: to evaluate different modeling techniques and to make a detailed structural characterization of CYP2C9. To achieve these…”
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Genetic polymorphism of cytochrome P450 1A1 (Cyp1A1) and glutathione transferases (M1, T1 and P1) among Africans by Dandara, Collet, Sayi, Jane, Masimirembwa, Collen M, Magimba, Ayoub, Kaaya, Sylvia, De Sommers, Kierk, Snyman, Jacques René, Hasler, Julia A

“…The co-ordinate expression and regulation of the drug metabolising enzymes, cytochrome P4501A1 (CYPlAl) and glutathione transferases (GSTM1, GSTT1 and GSTP1),…”
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Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: Synthesis and pharmacological evaluation by Ongarora, Dennis S.B., Gut, Jiri, Rosenthal, Philip J., Masimirembwa, Collen M., Chibale, Kelly

“…The synthesis and evaluation of antiplasmodial activity of benzothiazole, benzimidazole, benzoxazole and pyridine analogues of amodiaquine is hereby reported…”
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Identification of human cytochrome P450s that metabolise anti-parasitic drugs and predictions of in vivo drug hepatic clearance from in vitro data by LI, Xue-Qing, BJÖRKMAN, Anders, ANDERSSON, Tommy B, GUSTAFSSON, Lars L, MASIMIREMBWA, Collen M

“…Knowledge about the metabolism of anti-parasitic drugs (APDs) will be helpful in ongoing efforts to optimise dosage recommendations in clinical practise. This…”
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Potent inhibition of CYP1A2 by Frutinone A, an active ingredient of the broad spectrum antimicrobial herbal extract from P. fruticosa by Thelingwani, Roslyn S., Dhansay, Kariema, Smith, Peter, Chibale, Kelly, Masimirembwa, Collen M.

“…Frutinone is an active ingredient extracted from the lipophilic fraction of the Polygala Fruticosa demonstrating various antibacterial and fungal properties…”
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Amodiaquine clearance and its metabolism to N-desethylamodiaquine is mediated by CYP2C8: a new high affinity and turnover enzyme-specific probe substrate by Li, Xue-Qing, Björkman, Anders, Andersson, Tommy B, Ridderström, Marianne, Masimirembwa, Collen M

“…Amodiaquine (AQ) metabolism to N-desethylamodiaquine (DEAQ) is the principal route of disposition in humans. Using human liver microsomes and two sets of…”
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Metabolic stability for drug discovery and development: Pharmacokinetic and biochemical challenges by MASIMIREMBWA, Collen M, BREDBERG, Ulf, ANDERSSON, Tommy B

“…Metabolic stability refers to the susceptibility of compounds to biotransformation in the context of selecting and/or designing drugs with favourable…”
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Establishment of a biobank and pharmacogenetics database of African populations by Matimba, Alice, Oluka, Margaret N, Ebeshi, Benjamin U, Sayi, Jane, Bolaji, Oluseye O, Guantai, Anastasia N, Masimirembwa, Collen M

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Exploration of Enzyme−Ligand Interactions in CYP2D6 & 3A4 Homology Models and Crystal Structures Using a Novel Computational Approach by Kjellander, Britta, Masimirembwa, Collen M, Zamora, Ismael

“…New crystal structures of human CYP2D6 and CYP3A4 have recently been reported, and in this study, we wanted to compare them with previously used homology…”
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Evaluation of human liver slices and reporter gene assays as systems for predicting the cytochrome P450 induction potential of drugs in vivo in humans by PERSSON, Kajsa P, EKEHED, Susanne, OTTER, Charlotta, MAREIKE LUTZ, E. S, MCPHEAT, Jane, MASIMIREMBWA, Collen M, ANDERSSON, Tommy B

“…The aim of the study was to investigate the feasibility of predicting human in vivo cytochrome P450 (CYP) induction properties of drugs using in vitro methods…”
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Conformer- and Alignment-Independent Model for Predicting Structurally Diverse Competitive CYP2C9 Inhibitors by Afzelius, Lovisa, Zamora, Ismael, Masimirembwa, Collen M, Karlén, Anders, Andersson, Tommy B, Mecucci, Silvio, Baroni, Massimo, Cruciani, Gabriele

“…A conformer- and alignment-independent three-dimensional structure−activity relationship (3D-QSAR) model has been derived that is based on flexible molecular…”
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Competitive CYP2C9 inhibitors: enzyme inhibition studies, protein homology modeling, and three-dimensional quantitative structure-activity relationship analysis by Afzelius, L, Zamora, I, Ridderström, M, Andersson, T B, Karlén, A, Masimirembwa, C M

“…This study describes the generation of a three-dimensional quantitative structure activity relationship (3D-QSAR) model for 29 structurally diverse,…”
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