Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition
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
Published in Nature communications (04.11.2016)
Published in Nature communications (04.11.2016)
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Journal Article
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,4R)‑1-((S)‑2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy‑N‑(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298)
Soares, Pedro, Gadd, Morgan S, Frost, Julianty, Galdeano, Carles, Ellis, Lucy, Epemolu, Ola, Rocha, Sonia, Read, Kevin D, Ciulli, Alessio
Published in Journal of medicinal chemistry (25.01.2018)
Published in Journal of medicinal chemistry (25.01.2018)
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Journal Article
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 the Illicit Drug Market
Brandon, Andrew M, Antonides, Lysbeth H, Riley, Jennifer, Epemolu, Ola, McKeown, Denise A, Read, Kevin D, McKenzie, Craig
Published in Molecules (Basel, Switzerland) (05.03.2021)
Published in Molecules (Basel, Switzerland) (05.03.2021)
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Journal Article
Anti-Inflammatory Effects of Auranamide and Patriscabratine—Mechanisms and In Silico Studies
Mak, Kit-Kay, Zhang, Shiming, Low, Jun Sheng, Balijepalli, Madhu Katyayani, Sakirolla, Raghavendra, Dinkova-Kostova, Albena T, Epemolu, Ola, Mohd, Zulkefeli, Pichika, Mallikarjuna Rao
Published in Molecules (Basel, Switzerland) (01.08.2022)
Published in Molecules (Basel, Switzerland) (01.08.2022)
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Journal Article
Lysyl-tRNA synthetase, a target for urgently needed M. tuberculosis drugs
Green, Simon R., Davis, Susan H., Damerow, Sebastian, Engelhart, Curtis A., Mathieson, Michael, Baragaña, Beatriz, Robinson, David A., Tamjar, Jevgenia, Dawson, Alice, Tamaki, Fabio K., Buchanan, Kirsteen I., Post, John, Dowers, Karen, Shepherd, Sharon M., Jansen, Chimed, Zuccotto, Fabio, Gilbert, Ian H., Epemolu, Ola, Riley, Jennifer, Stojanovski, Laste, Osuna-Cabello, Maria, Pérez-Herrán, Esther, Rebollo, María José, Guijarro López, Laura, Casado Castro, Patricia, Camino, Isabel, Kim, Heather C., Bean, James M., Nahiyaan, Navid, Rhee, Kyu Y., Wang, Qinglan, Tan, Vee Y., Boshoff, Helena I. M., Converse, Paul J., Li, Si-Yang, Chang, Yong S., Fotouhi, Nader, Upton, Anna M., Nuermberger, Eric L., Schnappinger, Dirk, Read, Kevin D., Encinas, Lourdes, Bates, Robert H., Wyatt, Paul G., Cleghorn, Laura A. T.
Published in Nature communications (11.10.2022)
Published in Nature communications (11.10.2022)
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Journal Article
Studies on the mechanism of anti-inflammatory action of swietenine, a tetranortriterpenoid isolated from Swietenia macrophylla seeds
Mak, Kit-Kay, Shiming, Zhang, Balijepalli, Madhu Katyayani, Dinkova-Kostova, Albena T., Epemolu, Ola, Mohd, Zulkefeli, Pichika, Mallikarjuna Rao
Published in Phytomedicine Plus : International journal of phytotherapy and phytopharmacology (01.02.2021)
Published in Phytomedicine Plus : International journal of phytotherapy and phytopharmacology (01.02.2021)
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Journal Article
Synthesis of New Shogaol Analogues as NRF2 Activators and Evaluation of Their Anti-Inflammatory Activity, Modes of Action and Metabolic Stability
Mak, Kit-Kay, Shiming, Zhang, Sakirolla, Raghavendra, Balijepalli, Madhu Katyayani, Dinkova-Kostova, Albena T, Epemolu, Ola, Mohd, Zulkefeli, Pichika, Mallikarjuna Rao
Published in Antioxidants (01.02.2023)
Published in Antioxidants (01.02.2023)
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Journal Article
Swietenine Alleviates Nonalcoholic Fatty Liver Disease in Diabetic Mice via Lipogenesis Inhibition and Antioxidant Mechanisms
Mak, Kit-Kay, Zhang, Shiming, Chellian, Jestin, Mohd, Zulkefeli, Epemolu, Ola, Dinkova-Kostova, Albena T, Balijepalli, Madhu Katyayani, Pichika, Mallikarjuna Rao
Published in Antioxidants (27.02.2023)
Published in Antioxidants (27.02.2023)
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Journal Article
Synthesis and Anti‐Inflammatory Activity of 2‐Amino‐4,5,6,7‐tetrahydrobenzo[b]thiophene‐Derived NRF2 Activators
Mak, Kit‐Kay, Shiming, Zhang, Epemolu, Ola, Dinkova‐Kostova, Albena T., Wells, Geoffrey, Gazaryan, Irina G., Sakirolla, Raghavendra, Mohd, Zulkefeli, Pichika, Mallikarjuna Rao
Published in ChemistryOpen (Weinheim) (01.10.2022)
Published in ChemistryOpen (Weinheim) (01.10.2022)
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Journal Article
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 confirmation in urine samples from known drug users
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
Published in Forensic toxicology (2018)
Published in Forensic toxicology (2018)
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Journal Article
The First Potent and Selective Inhibitors of the Glycine Transporter Type 2
Caulfield, Wilson L, Collie, Iain T, Dickins, Rachel S, Epemolu, Ola, McGuire, Ross, Hill, David R, McVey, Gillian, Morphy, J. Richard, Rankovic, Zoran, Sundaram, Hardy
Published in Journal of medicinal chemistry (16.08.2001)
Published in Journal of medicinal chemistry (16.08.2001)
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Journal Article
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,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyI)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyppyrrolidine-2-carboxamide (VH298)
Soares, Pedro, Gadd, Morgan S., Frost, Julianty, Galdeano, Carles, Ellis, Lucy, Epemolu, Ola, Rocha, Sonia, Read, Kevin D., Ciulli, Alessio
Published in Journal of medicinal chemistry (25.01.2018)
Published in Journal of medicinal chemistry (25.01.2018)
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Journal Article
Reversal of Neuromusclar Blockade and Simultaneous Increase in Plasma Rocuronium Concentration after the Intravenous Infusion of the Novel Reversal Agent Org 25970
Epemolu, Ola, Bom, Anton, Hope, Frank, Mason, Rona
Published in Anesthesiology (Philadelphia) (01.09.2003)
Published in Anesthesiology (Philadelphia) (01.09.2003)
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Journal Article
The role of DMPK science in improving pharmaceutical research and development efficiency
Mak, Kit-Kay, Epemolu, Ola, Pichika, Mallikarjuna Rao
Published in Drug discovery today (01.03.2022)
Published in Drug discovery today (01.03.2022)
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Journal Article
Development of a Novel Lead that Targets M. tuberculosis Polyketide Synthase 13
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.
Published in Cell (13.07.2017)
Published in Cell (13.07.2017)
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Journal Article
Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB
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
Published in Journal of medicinal chemistry (09.08.2018)
Published in Journal of medicinal chemistry (09.08.2018)
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Journal Article
Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target
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
Published in Journal of medicinal chemistry (13.01.2022)
Published in Journal of medicinal chemistry (13.01.2022)
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Journal Article
Identification and Optimization of Novel Inhibitors of the Polyketide Synthase 13 Thioesterase Domain with Antitubercular Activity
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-Roman, 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., Baragana, Beatriz
Published in Journal of medicinal chemistry (23.11.2023)
Published in Journal of medicinal chemistry (23.11.2023)
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Journal Article
Discovery and Optimization of 5‑Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi
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
Published in Journal of medicinal chemistry (14.09.2017)
Published in Journal of medicinal chemistry (14.09.2017)
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Journal Article
Discovery of super soft-drug modulators of sphingosine-1-phosphate receptor 1
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
Published in Bioorganic & medicinal chemistry letters (15.10.2018)
Published in Bioorganic & medicinal chemistry letters (15.10.2018)
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