A caged E3 ligase ligand for PROTAC-mediated protein degradation with light
Kounde, Cyrille S, Shchepinova, Maria M, Saunders, Charlie N, Muelbaier, Marcel, Rackham, Mark D, Harling, John D, Tate, Edward W
Published in Chemical communications (Cambridge, England) (21.05.2020)
Published in Chemical communications (Cambridge, England) (21.05.2020)
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PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding
Tinworth, Christopher P, Lithgow, Hannah, Dittus, Lars, Bassi, Zuni I, Hughes, Sophie E, Muelbaier, Marcel, Dai, Han, Smith, Ian E. D, Kerr, William J, Burley, Glenn A, Bantscheff, Marcus, Harling, John D
Published in ACS chemical biology (15.03.2019)
Published in ACS chemical biology (15.03.2019)
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Journal Article
Catalytic in vivo protein knockdown by small-molecule PROTACs
Bondeson, Daniel P, Mares, Alina, Smith, Ian E D, Ko, Eunhwa, Campos, Sebastien, Miah, Afjal H, Mulholland, Katie E, Routly, Natasha, Buckley, Dennis L, Gustafson, Jeffrey L, Zinn, Nico, Grandi, Paola, Shimamura, Satoko, Bergamini, Giovanna, Faelth-Savitski, Maria, Bantscheff, Marcus, Cox, Carly, Gordon, Deborah A, Willard, Ryan R, Flanagan, John J, Casillas, Linda N, Votta, Bartholomew J, den Besten, Willem, Famm, Kristoffer, Kruidenier, Laurens, Carter, Paul S, Harling, John D, Churcher, Ian, Crews, Craig M
Published in Nature chemical biology (01.08.2015)
Published in Nature chemical biology (01.08.2015)
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HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins
Buckley, Dennis L, Raina, Kanak, Darricarrere, Nicole, Hines, John, Gustafson, Jeffrey L, Smith, Ian E, Miah, Afjal H, Harling, John D, Crews, Craig M
Published in ACS chemical biology (21.08.2015)
Published in ACS chemical biology (21.08.2015)
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Journal Article
The therapeutic potential of PROTACs
Benowitz, Andrew B, Jones, Katherine L, Harling, John D
Published in Expert opinion on therapeutic patents (2021)
Published in Expert opinion on therapeutic patents (2021)
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Journal Article
Targeting IRAK4 for Degradation with PROTACs
Nunes, Joao, McGonagle, Grant A, Eden, Jessica, Kiritharan, Girieshanie, Touzet, Megane, Lewell, Xiao, Emery, John, Eidam, Hilary, Harling, John D, Anderson, Niall A
Published in ACS medicinal chemistry letters (11.07.2019)
Published in ACS medicinal chemistry letters (11.07.2019)
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Journal Article
Discovery and Characterisation of Highly Cooperative FAK‐Degrading PROTACs
Law, Robert P., Nunes, Joao, Chung, Chun‐wa, Bantscheff, Marcus, Buda, Karol, Dai, Han, Evans, John P., Flinders, Adam, Klimaszewska, Diana, Lewis, Antonia J., Muelbaier, Marcel, Scott‐Stevens, Paul, Stacey, Peter, Tame, Christopher J., Watt, Gillian F., Zinn, Nico, Queisser, Markus A., Harling, John D., Benowitz, Andrew B.
Published in Angewandte Chemie International Edition (18.10.2021)
Published in Angewandte Chemie International Edition (18.10.2021)
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Journal Article
Optimization of a Series of RIPK2 PROTACs
Miah, Afjal H, Smith, Ian E. D, Rackham, Mark, Mares, Alina, Thawani, Aditya R, Nagilla, Rakesh, Haile, Pamela A, Votta, Bartholomew J, Gordon, Laurie J, Watt, Gillian, Denyer, Jane, Fisher, Don T, Dace, Phoebe, Giffen, Paul, Goncalves, Andrea, Churcher, Ian, Scott-Stevens, Paul, Harling, John D
Published in Journal of medicinal chemistry (09.09.2021)
Published in Journal of medicinal chemistry (09.09.2021)
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Light-mediated multi-target protein degradation using arylazopyrazole photoswitchable PROTACs (AP-PROTACs)
Zhang, Qisi, Kounde, Cyrille S, Mondal, Milon, Greenfield, Jake L, Baker, Jennifer R, Kotelnikov, Sergei, Ignatov, Mikhail, Tinworth, Christopher P, Zhang, Leran, Conole, Daniel, De Vita, Elena, Kozakov, Dima, McCluskey, Adam, Harling, John D, Fuchter, Matthew J, Tate, Edward W
Published in Chemical communications (Cambridge, England) (29.09.2022)
Published in Chemical communications (Cambridge, England) (29.09.2022)
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Structural Insights into PROTAC-Mediated Degradation of Bcl-xL
Chung, Chun-wa, Dai, Han, Fernandez, Esther, Tinworth, Christopher P, Churcher, Ian, Cryan, Jenni, Denyer, Jane, Harling, John D, Konopacka, Agnieszka, Queisser, Markus A, Tame, Christopher J, Watt, Gillian, Jiang, Fan, Qian, Dongming, Benowitz, Andrew B
Published in ACS chemical biology (18.09.2020)
Published in ACS chemical biology (18.09.2020)
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Journal Article
Challenges and opportunities for in vivo PROTAC delivery
Benowitz, Andrew B, Scott-Stevens, Paul T, Harling, John D
Published in Future medicinal chemistry (01.01.2022)
Published in Future medicinal chemistry (01.01.2022)
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Journal Article
Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2
Mares, Alina, Miah, Afjal H, Smith, Ian E D, Rackham, Mark, Thawani, Aditya R, Cryan, Jenni, Haile, Pamela A, Votta, Bartholomew J, Beal, Allison M, Capriotti, Carol, Reilly, Michael A, Fisher, Don T, Zinn, Nico, Bantscheff, Marcus, MacDonald, Thomas T, Vossenkamper, Anna, Dace, Phoebe, Churcher, Ian, Benowitz, Andrew B, Watt, Gillian, Denyer, Jane, Scott-Stevens, Paul, Harling, John D
Published in Communications biology (20.03.2020)
Published in Communications biology (20.03.2020)
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Journal Article
Activating mechanosensitive channels embedded in droplet interface bilayers using membrane asymmetry
Strutt, Robert, Hindley, James W, Gregg, Jordan, Booth, Paula J, Harling, John D, Law, Robert V, Friddin, Mark S, Ces, Oscar
Published in Chemical science (Cambridge) (18.02.2021)
Published in Chemical science (Cambridge) (18.02.2021)
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Integrated Direct-to-Biology Platform for the Nanoscale Synthesis and Biological Evaluation of PROTACs
Stevens, Rebecca, Bendito-Moll, Enrique, Battersby, David J, Miah, Afjal H, Wellaway, Natalie, Law, Robert P, Stacey, Peter, Klimaszewska, Diana, Macina, Justyna M, Burley, Glenn A, Harling, John D
Published in Journal of medicinal chemistry (23.11.2023)
Published in Journal of medicinal chemistry (23.11.2023)
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Journal Article
Structure-Guided Design and Optimization of Covalent VHL-Targeted Sulfonyl Fluoride PROTACs
Shah, Rishi R., De Vita, Elena, Sathyamurthi, Preethi S., Conole, Daniel, Zhang, Xinyue, Fellows, Elliot, Dickinson, Eleanor R., Fleites, Carlos M., Queisser, Markus A., Harling, John D., Tate, Edward W.
Published in Journal of medicinal chemistry (28.03.2024)
Published in Journal of medicinal chemistry (28.03.2024)
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Journal Article
UV-DIB: label-free permeability determination using droplet interface bilayers
Strutt, Robert, Sheffield, Felix, Barlow, Nathan E, Flemming, Anthony J, Harling, John D, Law, Robert V, Brooks, Nicholas J, Barter, Laura M C, Ces, Oscar
Published in Lab on a chip (01.03.2022)
Published in Lab on a chip (01.03.2022)
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SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7
Inman, Gareth J, Nicolás, Francisco J, Callahan, James F, Harling, John D, Gaster, Laramie M, Reith, Alastair D, Laping, Nicholas J, Hill, Caroline S
Published in Molecular pharmacology (01.07.2002)
Published in Molecular pharmacology (01.07.2002)
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Discovery of Novel Irreversible Inhibitors of Interleukin (IL)-2-inducible Tyrosine Kinase (Itk) by Targeting Cysteine 442 in the ATP Pocket
Harling, John D., Deakin, Angela M., Campos, Sébastien, Grimley, Rachel, Chaudry, Laiq, Nye, Catherine, Polyakova, Oxana, Bessant, Christina M., Barton, Nick, Somers, Don, Barrett, John, Graves, Rebecca H., Hanns, Laura, Kerr, William J., Solari, Roberto
Published in The Journal of biological chemistry (27.09.2013)
Published in The Journal of biological chemistry (27.09.2013)
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