Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase: Structure–Activity Relationships Leading to the Chemical Probe (2S...

por Soares, Pedro, Gadd, Morgan S., Frost, Julianty, Galdeano, Carles, Ellis, Lucy, Epemolu, Ola, Rocha, Sonia, Read, Kevin D., Ciulli, Alessio
Publicado 2017

Pharmacokinetics of β-Lactam Antibiotics: Clues from the Past To Help Discover Long-Acting Oral Drugs in the Future

por Smith, Paul W., Zuccotto, Fabio, Bates, Robert H., Martinez-Martinez, Maria Santos, Read, Kevin D., Peet, Caroline, Epemolu, Ola
Publicado 2018

Swietenine Alleviates Nonalcoholic Fatty Liver Disease in Diabetic Mice via Lipogenesis Inhibition and Antioxidant Mechanisms

por Mak, Kit-Kay, Zhang, Shiming, Chellian, Jestin, Mohd, Zulkefeli, Epemolu, Ola, Dinkova-Kostova, Albena T., Balijepalli, Madhu Katyayani, Pichika, Mallikarjuna Rao
Publicado 2023

A Systematic Study of the In Vitro Pharmacokinetics and Estimated Human In Vivo Clearance of Indole and Indazole-3-Carboxamide Synthetic Cannabinoid Receptor Agonists Detected on t...

por Brandon, Andrew M., Antonides, Lysbeth H., Riley, Jennifer, Epemolu, Ola, McKeown, Denise A., Read, Kevin D., McKenzie, Craig
Publicado 2021

Synthesis of New Shogaol Analogues as NRF2 Activators and Evaluation of Their Anti-Inflammatory Activity, Modes of Action and Metabolic Stability

por Mak, Kit-Kay, Shiming, Zhang, Sakirolla, Raghavendra, Balijepalli, Madhu Katyayani, Dinkova-Kostova, Albena T., Epemolu, Ola, Mohd, Zulkefeli, Pichika, Mallikarjuna Rao
Publicado 2023

Synthesis and Anti‐Inflammatory Activity of 2‐Amino‐4,5,6,7‐tetrahydrobenzo[b]thiophene‐Derived NRF2 Activators

por Mak, Kit‐Kay, Shiming, Zhang, Epemolu, Ola, Dinkova‐Kostova, Albena T., Wells, Geoffrey, Gazaryan, Irina G., Sakirolla, Raghavendra, Mohd, Zulkefeli, Pichika, Mallikarjuna Rao
Publicado 2022

Anti-Inflammatory Effects of Auranamide and Patriscabratine—Mechanisms and In Silico Studies

por Mak, Kit-Kay, Shiming, Zhang, Low, Jun Sheng, Balijepalli, Madhu Katyayani, Sakirolla, Raghavendra, Dinkova-Kostova, Albena T., Epemolu, Ola, Mohd, Zulkefeli, Pichika, Mallikarjuna Rao
Publicado 2022

Discovery of super soft-drug modulators of sphingosine-1-phosphate receptor 1

por Bell, Mark, Foley, David, Naylor, Claire, Robinson, Colin, Riley, Jennifer, Epemolu, Ola, Scullion, Paul, Shishikura, Yoko, Katz, Elad, McLean, W.H. Irwin, Wyatt, Paul, Read, Kevin D., Woodland, Andrew
Publicado 2018

Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition

por Frost, Julianty, Galdeano, Carles, Soares, Pedro, Gadd, Morgan S., Grzes, Katarzyna M., Ellis, Lucy, Epemolu, Ola, Shimamura, Satoko, Bantscheff, Marcus, Grandi, Paola, Read, Kevin D., Cantrell, Doreen A., Rocha, Sonia, Ciulli, Alessio
Publicado 2016

Chemical synthesis, characterisation and in vitro and in vivo metabolism of the synthetic opioid MT-45 and its newly identified fluorinated analogue 2F-MT-45 with metabolite confir...

por McKenzie, Craig, Sutcliffe, Oliver B., Read, Kevin D., Scullion, Paul, Epemolu, Ola, Fletcher, Daniel, Helander, Anders, Beck, Olof, Rylski, Alexia, Antonides, Lysbeth H., Riley, Jennifer, Smith, Shannah A., Nic Daeid, Niamh
Publicado 2018

Discovery of Soft-Drug Topical Tool Modulators of Sphingosine-1-phosphate Receptor 1 (S1PR1)

por Bell, Mark, Foley, David, Naylor, Claire, Wood, Gavin, Robinson, Colin, Riley, Jennifer, Epemolu, Ola, Ellis, Lucy, Scullion, Paul, Shishikura, Yoko, Osuna-Cabello, Maria, Ferguson, Liam, Pinto, Erika, Fletcher, Daniel, Katz, Elad, McLean, W. H. Irwin, Wyatt, Paul, Read, Kevin D, Woodland, Andrew
Publicado 2019

Chemical Validation of Methionyl-tRNA Synthetase as a Druggable Target in Leishmania donovani

por Torrie, Leah S., Brand, Stephen, Robinson, David A., Ko, Eun Jung, Stojanovski, Laste, Simeons, Frederick R. C., Wyllie, Susan, Thomas, John, Ellis, Lucy, Osuna-Cabello, Maria, Epemolu, Ola, Nühs, Andrea, Riley, Jennifer, MacLean, Lorna, Manthri, Sujatha, Read, Kevin D., Gilbert, Ian H., Fairlamb, Alan H., De Rycker, Manu
Publicado 2017

Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent In Vitro Antileishmanial Activity: Initial SAR and Assessment of In Vivo Activity

por Thomas, Michael G., De Rycker, Manu, Wall, Richard J., Spinks, Daniel, Epemolu, Ola, Manthri, Sujatha, Norval, Suzanne, Osuna-Cabello, Maria, Patterson, Stephen, Riley, Jennifer, Simeons, Frederick R. C., Stojanovski, Laste, Thomas, John, Thompson, Stephen, Naylor, Claire, Fiandor, Jose M., Wyatt, Paul G., Marco, Maria, Wyllie, Susan, Read, Kevin D., Miles, Timothy J., Gilbert, Ian H.
Publicado 2020

Identification and Optimization of Novel Inhibitors of the Polyketide Synthase 13 Thioesterase Domain with Antitubercular Activity

por Green, Simon R., Wilson, Caroline, Eadsforth, Thomas C., Punekar, Avinash S., Tamaki, Fabio K., Wood, Gavin, Caldwell, Nicola, Forte, Barbara, Norcross, Neil R., Kiczun, Michael, Post, John M., Lopez-Román, Eva Maria, Engelhart, Curtis A., Lukac, Iva, Zuccotto, Fabio, Epemolu, Ola, Boshoff, Helena I. M., Schnappinger, Dirk, Walpole, Chris, Gilbert, Ian H., Read, Kevin D., Wyatt, Paul G., Baragaña, Beatriz
Publicado 2023

Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB

por Cleghorn, Laura A. T., Ray, Peter C., Odingo, Joshua, Kumar, Anuradha, Wescott, Heather, Korkegian, Aaron, Masquelin, Thierry, Lopez Moure, Abraham, Wilson, Caroline, Davis, Susan, Huggett, Margaret, Turner, Penelope, Smith, Alasdair, Epemolu, Ola, Zuccotto, Fabio, Riley, Jennifer, Scullion, Paul, Shishikura, Yoko, Ferguson, Liam, Rullas, Joaquin, Guijarro, Laura, Read, Kevin D., Green, Simon R., Hipskind, Phil, Parish, Tanya, Wyatt, Paul G.
Publicado 2018

Development of a Novel Lead that Targets M. tuberculosis Polyketide Synthase 13

por Aggarwal, Anup, Parai, Maloy K., Shetty, Nishant, Wallis, Deeann, Woolhiser, Lisa, Hastings, Courtney, Dutta, Noton K., Galaviz, Stacy, Dhakal, Ramesh C., Shrestha, Rupesh, Wakabayashi, Shoko, Walpole, Chris, Matthews, David, Floyd, David, Scullion, Paul, Riley, Jennifer, Epemolu, Ola, Norval, Suzanne, Snavely, Thomas, Robertson, Gregory T., Rubin, Eric J., Ioerger, Thomas R., Sirgel, Frik A., van der Merwe, Ruben, van Helden, Paul D., Keller, Peter, Böttger, Erik C., Karakousis, Petros C., Lenaerts, Anne J., Sacchettini, James C.
Publicado 2017

2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure–Activity Relationships, Mechanism of Action and Absorption, Distribu...

por Murugesan, Dinakaran, Ray, Peter C., Bayliss, Tracy, Prosser, Gareth A., Harrison, Justin R., Green, Kirsteen, Soares de Melo, Candice, Feng, Tzu-Shean, Street, Leslie J., Chibale, Kelly, Warner, Digby F., Mizrahi, Valerie, Epemolu, Ola, Scullion, Paul, Ellis, Lucy, Riley, Jennifer, Shishikura, Yoko, Ferguson, Liam, Osuna-Cabello, Maria, Read, Kevin D., Green, Simon R., Lamprecht, Dirk A., Finin, Peter M., Steyn, Adrie J. C., Ioerger, Thomas R., Sacchettini, Jim, Rhee, Kyu Y., Arora, Kriti, Barry, Clifton E., Wyatt, Paul G., Boshoff, Helena I. M.
Publicado 2018

Spirocycle MmpL3 Inhibitors with Improved hERG and Cytotoxicity Profiles as Inhibitors of Mycobacterium tuberculosis Growth

por Ray, Peter C., Huggett, Margaret, Turner, Penelope A., Taylor, Malcolm, Cleghorn, Laura A. T., Early, Julie, Kumar, Anuradha, Bonnett, Shilah A., Flint, Lindsay, Joerss, Douglas, Johnson, James, Korkegian, Aaron, Mullen, Steven, Moure, Abraham L., Davis, Susan H., Murugesan, Dinakaran, Mathieson, Michael, Caldwell, Nicola, Engelhart, Curtis A., Schnappinger, Dirk, Epemolu, Ola, Zuccotto, Fabio, Riley, Jennifer, Scullion, Paul, Stojanovski, Laste, Massoudi, Lisa, Robertson, Gregory T., Lenaerts, Anne J., Freiberg, Gail, Kempf, Dale J., Masquelin, Thierry, Hipskind, Philip A., Odingo, Joshua, Read, Kevin D., Green, Simon R., Wyatt, Paul G., Parish, Tanya
Publicado 2021

Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi

por Brand, Stephen, Ko, Eun Jung, Viayna, Elisabet, Thompson, Stephen, Spinks, Daniel, Thomas, Michael, Sandberg, Lars, Francisco, Amanda F., Jayawardhana, Shiromani, Smith, Victoria C., Jansen, Chimed, De Rycker, Manu, Thomas, John, MacLean, Lorna, Osuna-Cabello, Maria, Riley, Jennifer, Scullion, Paul, Stojanovski, Laste, Simeons, Frederick R. C., Epemolu, Ola, Shishikura, Yoko, Crouch, Sabrinia D., Bakshi, Tania S., Nixon, Christopher J., Reid, Iain H., Hill, Alan P., Underwood, Tim Z., Hindley, Sean J., Robinson, Sharon A., Kelly, John M., Fiandor, Jose M., Wyatt, Paul G., Marco, Maria, Miles, Timothy J., Read, Kevin D., Gilbert, Ian H.
Publicado 2017

Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target

por Wilson, Caroline, Ray, Peter, Zuccotto, Fabio, Hernandez, Jorge, Aggarwal, Anup, Mackenzie, Claire, Caldwell, Nicola, Taylor, Malcolm, Huggett, Margaret, Mathieson, Michael, Murugesan, Dinakaran, Smith, Alasdair, Davis, Susan, Cocco, Mattia, Parai, Maloy K., Acharya, Arjun, Tamaki, Fabio, Scullion, Paul, Epemolu, Ola, Riley, Jennifer, Stojanovski, Laste, Lopez-Román, Eva Maria, Torres-Gómez, Pedro Alfonso, Toledo, Ana Maria, Guijarro-Lopez, Laura, Camino, Isabel, Engelhart, Curtis A., Schnappinger, Dirk, Massoudi, Lisa M., Lenaerts, Anne, Robertson, Gregory T., Walpole, Chris, Matthews, David, Floyd, David, Sacchettini, James C., Read, Kevin D., Encinas, Lourdes, Bates, Robert H., Green, Simon R., Wyatt, Paul G.
Publicado 2021