Search Results - "Arendse, Lauren B"

Novel Therapeutic Approaches Targeting the Renin-Angiotensin System and Associated Peptides in Hypertension and Heart Failure by Arendse, Lauren B, Danser, A H Jan, Poglitsch, Marko, Touyz, Rhian M, Burnett, Jr, John C, Llorens-Cortes, Catherine, Ehlers, Mario R, Sturrock, Edward D

“…Despite the success of renin-angiotensin system (RAS) blockade by angiotensin-converting enzyme (ACE) inhibitors and angiotensin II type 1 receptor (AT R)…”
Get full text

Molecular Basis for Multiple Omapatrilat Binding Sites within the ACE C‑Domain: Implications for Drug Design by Cozier, Gyles E, Arendse, Lauren B, Schwager, Sylva L, Sturrock, Edward D, Acharya, K. Ravi

“…Omapatrilat was designed as a vasopeptidase inhibitor with dual activity against the zinc metallopeptidases angiotensin-1 converting enzyme (ACE) and…”
Get full text

Structural Basis for Inhibitor Potency and Selectivity of Plasmodium falciparum Phosphatidylinositol 4‑Kinase Inhibitors by Fienberg, Stephen, Eyermann, Charles J, Arendse, Lauren B, Basarab, Gregory S, McPhail, Jacob A, Burke, John E, Chibale, Kelly

“…Plasmodium falciparum phosphatidylinositol 4-kinase (PfPI4K) has emerged as a promising new drug target for novel antimalarial therapeutics. In the absence of…”
Get full text

Developing kinase inhibitors for malaria: an opportunity or liability? by Mogwera, Koketso S P, Chibale, Kelly, Arendse, Lauren B

“…Highly druggable and essential to almost all aspects of cellular life, the protein and phosphoinositide kinase gene families offer a wealth of potential…”
Get full text

Effects of polymorphic variation on the thermostability of heterogenous populations of CYP3A4 and CYP2C9 enzymes in solution by Arendse, Lauren B., Blackburn, Jonathan M.

“…The effect of non-synonymous single nucleotide polymorphisms (SNPs) on cytochrome P450 (CYP450) drug metabolism is currently poorly understood due to the large…”
Get full text

Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity by Vanaerschot, Manu, Murithi, James M, Pasaje, Charisse Flerida A, Ghidelli-Disse, Sonja, Dwomoh, Louis, Bird, Megan, Spottiswoode, Natasha, Mittal, Nimisha, Arendse, Lauren B, Owen, Edward S, Wicht, Kathryn J, Siciliano, Giulia, Bösche, Markus, Yeo, Tomas, Kumar, T R Santha, Mok, Sachel, Carpenter, Emma F, Giddins, Marla J, Sanz, Olalla, Ottilie, Sabine, Alano, Pietro, Chibale, Kelly, Llinás, Manuel, Uhlemann, Anne-Catrin, Delves, Michael, Tobin, Andrew B, Doerig, Christian, Winzeler, Elizabeth A, Lee, Marcus C S, Niles, Jacquin C, Fidock, David A

“…The search for antimalarial chemotypes with modes of action unrelated to existing drugs has intensified with the recent failure of first-line therapies across…”
Get more information

Selective Inhibition of the C-Domain of ACE (Angiotensin-Converting Enzyme) Combined With Inhibition of NEP (Neprilysin): A Potential New Therapy for Hypertension by Alves-Lopes, Rhéure, Montezano, Augusto C., Neves, Karla B., Harvey, Adam, Rios, Francisco J., Skiba, Dominik S., Arendse, Lauren B., Guzik, Tomasz J., Graham, Delyth, Poglitsch, Marko, Sturrock, Edward, Touyz, Rhian M.

“…Combined inhibition of NEP (neutral endopeptidase) and ACE (angiotensin-converting enzyme), without unwanted effects, remains an attractive therapeutic…”
Get full text

Probing the Requirements for Dual Angiotensin-Converting Enzyme C‑Domain Selective/Neprilysin Inhibition by Arendse, Lauren B, Cozier, Gyles E, Eyermann, Charles J, Basarab, Gregory S, Schwager, Sylva L, Chibale, Kelly, Acharya, K. Ravi, Sturrock, Edward D

“…Selective inhibition of the angiotensin-converting enzyme C-domain (cACE) and neprilysin (NEP), leaving the ACE N-domain (nACE) free to degrade bradykinin and…”
Get full text

The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple Plasmodium kinases and life cycle stages by Arendse, Lauren B, Murithi, James M, Qahash, Tarrick, Pasaje, Charisse Flerida A, Godoy, Luiz C, Dey, Sumanta, Gibhard, Liezl, Ghidelli-Disse, Sonja, Drewes, Gerard, Bantscheff, Marcus, Lafuente-Monasterio, Maria J, Fienberg, Stephen, Wambua, Lynn, Gachuhi, Samuel, Coertzen, Dina, van der Watt, Mariëtte, Reader, Janette, Aswat, Ayesha S, Erlank, Erica, Venter, Nelius, Mittal, Nimisha, Luth, Madeline R, Ottilie, Sabine, Winzeler, Elizabeth A, Koekemoer, Lizette L, Birkholtz, Lyn-Marie, Niles, Jacquin C, Llinás, Manuel, Fidock, David A, Chibale, Kelly

“…Compounds acting on multiple targets are critical to combating antimalarial drug resistance. Here, we report that the human "mammalian target of rapamycin"…”
Get more information

Structural basis for the C-domain-selective angiotensin-converting enzyme inhibition by bradykinin-potentiating peptide b (BPPb) by Sturrock, Edward D, Lubbe, Lizelle, Cozier, Gyles E, Schwager, Sylva L U, Arowolo, Afolake T, Arendse, Lauren B, Belcher, Emma, Acharya, K Ravi

“…Angiotensin-converting enzyme (ACE) is a zinc metalloprotease best known for its role in blood pressure regulation. ACE consists of two homologous catalytic…”
Get more information

Advances in malaria pharmacology and the online guide to MALARIA PHARMACOLOGY: IUPHAR review 38 by Armstrong, Jane F., Campo, Brice, Alexander, Stephen P. H., Arendse, Lauren B., Cheng, Xiu, Davenport, Anthony P., Faccenda, Elena, Fidock, David A., Godinez‐Macias, Karla P., Harding, Simon D., Kato, Nobutaka, Lee, Marcus C. S., Luth, Madeline R., Mazitschek, Ralph, Mittal, Nimisha, Niles, Jacquin C., Okombo, John, Ottilie, Sabine, Pasaje, Charisse Flerida A., Probst, Alexandra S., Rawat, Mukul, Rocamora, Frances, Sakata‐Kato, Tomoyo, Southan, Christopher, Spedding, Michael, Tye, Mark A., Yang, Tuo, Zhao, Na, Davies, Jamie A.

“…Antimalarial drug discovery has until recently been driven by high‐throughput phenotypic cellular screening, allowing millions of compounds to be assayed and…”
Get full text

Selective Inhibition of the C-Domain of ACE (Angiotensin-Converting Enzyme) Combined With Inhibition of NEP (Neprilysin): A Potential New Therapy for Hypertension by Alves-Lopes, Rhéure, Montezano, Augusto C., Neves, Karla B., Harvey, Adam, Rios, Francisco J., Skiba, Dominik S., Arendse, Lauren B., Guzik, Tomasz J., Graham, Delyth, Poglitsch, Marko, Sturrock, Edward, Touyz, Rhian M.

“…Combined inhibition of NEP (neutral endopeptidase) and ACE (angiotensin-converting enzyme), without unwanted effects, remains an attractive therapeutic…”
Get full text

Plasmodium Kinases as Potential Drug Targets for Malaria: Challenges and Opportunities by Arendse, Lauren B, Wyllie, Susan, Chibale, Kelly, Gilbert, Ian H

“…Protein and phosphoinositide kinases have been successfully exploited as drug targets in various disease areas, principally in oncology. In malaria, several…”
Get full text

New Amidated 3,6-Diphenylated Imidazopyridazines with Potent Antiplasmodium Activity Are Dual Inhibitors of Plasmodium Phosphatidylinositol-4-kinase and cGMP-Dependent Protein Kinase by Cheuka, Peter Mubanga, Centani, Luyanda, Arendse, Lauren B, Fienberg, Stephen, Wambua, Lynn, Renga, Shoneeze S, Dziwornu, Godwin Akpeko, Kumar, Malkeet, Lawrence, Nina, Taylor, Dale, Wittlin, Sergio, Coertzen, Dina, Reader, Janette, van der Watt, Mariette, Birkholtz, Lyn-Marie, Chibale, Kelly

“…Recent studies on 3,6-diphenylated imidazopyridazines have demonstrated impressive activity and efficacy in mouse models of malaria infection. Herein, we…”
Get full text