Peer-Reviewed Publications

  1. Optimization of a Series of RIPK2 PROTACs. Miah AH, Smith IED, Rackham M, Mares A, Thawani AR, Nagilla R, Haile PA, Votta BJ, Gordon LJ, Watt G, Denyer J, Fisher DT, Dace P, Giffen P, Goncalves A, Churcher I, Scott-Stevens P, Harling JD. Journal of Medicinal Chemistry, (2021) 64(17), 12978-13003. PubMed 34432979, link
  2. The rise and rise of protein degradation: Opportunities and challenges ahead. Hughes SJ, Testa A, Thompson N, Churcher I. Drug Discovery Today. (2021), 26(12), 2889-2897. PubMed 34419629, link
  3. Structural Insights into PROTAC-Mediated Degradation of Bcl-xL. Chung CW, Dai H, Fernandez E, Tinworth CP, Churcher I, Cryan J, Denyer J, Harling JD, Konopacka A, Queisser MA, Tame CJ, Watt G, Jiang F, Qian D, Benowitz AB. ACS Chemical Biology (2020), 15(9), 2316-2323. PubMed 32697072, link
  4. Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2. Alina Mares, Afjal H. Miah, Ian E.D. Smith, Mark Rackham, Aditya R. Thawani, Jenni Cryan, Pamela A. Haile, Bartholomew J. Votta, Allison M. Beal, Carol Capriotti, Michael A. Reilly, Don T. Fisher, Nico Zinn, Marcus Bantscheff, Thomas T. MacDonald, Anna Vossenkamper, Phoebe Dace, Ian Churcher, Andrew B. Benowitz, Gillian Watt, Jane Denyer, Paul Scott-Stevens & John D. Harling Nature Communications Biology, (2020), 3, 140. PubMed 32198438 link.
  5. Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach Bassi, Zuni I.; Fillmore, Martin C.; Miah, Afjal H.; Chapman, Trevor D.; Maller, Claire; Roberts, Emma J.; Davis, Lauren C.; Lewis, Darcy E.; Galwey, Nicholas W.; Waddington, Kirsty E.; Valentino Parravicini, Abigail L. Macmillan-Jones, Celine Gongora, Philip G. Humphreys, Ian Churcher, Rab K. Prinjha, and David F. Tough ACS Chemical Biology (2018), 13(10), 2862-2867. PubMed 30200762 link
  6. Targeted Protein Degradation: Breaking the Rules – or just making new ones? Ian Churcher. Invited Perspective article for Journal of Medicinal Chemistry, (2018), 61(2), 444-452. PubMed 29144739 link
  7. Organic synthesis research is critical for the discovery of new medicines David Blakemore, Luis Castro, Ian Churcher, David Rees, Andrew W. Thomas, David Wilson , Anthony Wood. Nature Chemistry, (2018), 10(4), 383-394. PubMed 29568051 link
  8. Synthesis and Demonstration of the Biological Relevance of sp3-rich Scaffolds Distantly Related to Natural Product Frameworks, Foley, Daniel J.; Craven, Philip G. E.; Collins, Patrick M.; Doveston, Richard G.; Aimon, Anthony; Talon, Romain; Churcher, Ian; von Delft, Frank; Marsden, Stephen P.; Nelson, Adam, Chemistry - A European Journal (2017), 23(60), 15227-15232. PubMed 28983993 link
  9. Small molecule-mediated protein knockdown as a new approach to drug discovery. Tinworth, Christopher P.; Lithgow, Hannah; Churcher, Ian. MedChemComm (2016), 7(12), 2206-2216. Link
  10. Sigmatropic Rearrangement of Vinyl Aziridines: Expedient Synthesis of Cyclic Sulfoximines from Chiral Sulfinimines. Moragas, Toni; Liffey, Ryan M.; Regentova, Dominika; Ward, Jon-Paul S.; Dutton, Justine; Lewis, William; Churcher, Ian; Walton, Lesley; Souto, Jose A.; Stockman, Robert A. Angewandte Chemie, International Edition (2016), 55(34), 10047-10051. PubMed 27409574 link
  11. A divergent synthetic approach to diverse molecular scaffolds: assessment of lead-likeness using LLAMA, an open-access computational tool. Colomer, Ignacio; Empson, Christopher J.; Craven, Philip; Owen, Zachary; Doveston, Richard G.; Churcher, Ian; Marsden, Stephen P.; Nelson, Adam. Chemical Communications (Cambridge, United Kingdom) (2016), 52(45), 7209-7212. PubMed 27145833 link
  12. Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening Borthwick, Jennifer A.; Ancellin, Nicolas; Bertrand, Sophie M.; Bingham, Ryan P.; Carter, Paul S.; Chung, Chun-wa; Churcher, Ian; Dodic, Nerina; Fournier, Charlene; Francis, Peter L.; et al Journal of Medicinal Chemistry (2016), 59(6), 2452-2467. PubMed 26938474 link
  13. 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.  Nature Chemical Biology (2015), 11(8), 611-617. PubMed 26075522 link
  14. The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits Bertrand, Sophie M.; Ancellin, Nicolas; Beaufils, Benjamin; Bingham, Ryan P.; Borthwick, Jennifer A.; Boullay, Anne-Benedicte; Boursier, Eric; Carter, Paul S.; Chung, Chun-wa; Churcher, Ian; Dodic, Nerina; Fouchet, Marie-Helene; Fournier, Charlene; Francis, Peter L.; Gummer, Laura A.; Herry, Kenny; Hobbs, Andrew; Hobbs, Clare I.; Homes, Paul; Jamieson, Craig; Nicodeme, Edwige; Pickett, Stephen D.; Reid, Iain H.; Simpson, Graham L.; Sloan, Lisa A.; Smith, Sarah E.; Somers, Donald O'N.; Spitzfaden, Claus; Suckling, Colin J.; Valko, Klara; Washio, Yoshiaki; Young, Robert J. Journal of Medicinal Chemistry (2015), 58(18), 7140-7163. PubMed 26090771 link
  15. A systematic approach to diverse, lead-like scaffolds from α,α-disubstituted amino acids Foley, Daniel J.; Doveston, Richard G.; Churcher, Ian; Nelson, Adam; Marsden, Stephen P. Chemical Communications (Cambridge, United Kingdom)  (2015), 51(56), 11174-11177. Pubmed 26006179 link
  16. A unified lead-oriented synthesis of over fifty molecular scaffold Doveston, Richard G.; Tosatti, Paolo; Dow, Mark; Foley, Daniel J.; Li, Ho Yin; Campbell, Amanda J.; House, David; Churcher, Ian; Marsden, Stephen P.; Nelson, Adam Organic & Biomolecular Chemistry (2015), 13(3), 859-865. PubMed 25408068 link
  17. Asymmetric Synthesis of Trisubstituted Aziridines via Aza-Darzens Reaction of Chiral Sulfinimines Moragas, Toni; Churcher, Ian; Lewis, William; Stockman, Robert A. Organic Letters (2014), 16(24), 6290-6293. PubMed 25479333 link
  18. A phenotypic screening approach in cord blood-derived mast cells to identify anti-​inflammatory compounds Kaur, Rejbinder; Sloan, Lisa A.; Blanchard, Andy D.; Smith, Janet L.; Churcher, Ian; Wayne, Gareth J.; Ludbrook, Steven B.  Journal of Biomolecular Screening (2013), 18(10), 1223-1233. PubMed 23983232 link
  19. A practical drug discovery project at the undergraduate level Jonathan Fray, M.; Macdonald, Simon J. F.; Baldwin, Ian R.; Barton, Nick; Brown, Jack; Campbell, Ian B.; Churcher, Ian; Coe, Diane M.; Cooper, Anthony W. J.; Craven, Andrew P.; Fisher, Gail; Inglis, Graham G. A.; Kelly, Henry A.; Liddle, John; Maxwell, Aoife C.; Patel, Vipulkumar K.; Swanson, Stephen; Wellaway, Natalie Drug Discovery Today (2013), 18(23-24), 1158-1172. PubMed 24051399 link
  20. Reaction methodology: Speed dating for reactions Churcher, Ian Nature Chemistry (2013), 5(7), 554-555. PubMed 23787741 link
  21. Lead-Oriented Synthesis: A new opportunity for synthetic chemistry Nadin, Alan; Hattotuwagama, Channa; Churcher, Ian Angewandte Chemie Intl Ed (2012), 51, 1114. PubMed 22271624 link
  22. Fragment-Based Drug Discovery - from hit discovery to FDA approval: lessons learned and future challenges Hughes, Terry; Baldwin, Ian; Churcher, Ian Intl Drug Discovery, (2011), 6, 36. Link
  23. Stereoselective aza-Darzens reaction of tert-butanesulfilimines: convenient access to chiral aziridines Sola, Toni Moragas; Churcher, Ian; Lewis, William; Stockman, Robert A. Organic & Biomolecular Chemistry (2011), 9(14), 5034-5035. PubMed 21643589 link
  24. On the utility of S-mesitylsulfinimines for the stereoselective synthesis of chiral amines and aziridines Roe, Caroline; Sola, Toni Moragas; Sasraku-Neequaye, Leonid; Hobbs, Heather; Churcher, Ian; MacPherson, David; Stockman, Robert A Chemical Communications (2011), 47(26), 7491-7493. PubMed 21629906 link
  25. Small-molecule modulation of cellular chaperones to treat protein misfolding disorders Sloan, Lisa A.; Fillmore, Martin C.; Churcher, Ian. Current Opinion in Drug Discovery & Development (2009), 12(5), 666-681. PubMed 19736625
  26. The novel γ-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]- 1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of notch-related pathology in the Tg2576 mouse.      Best, Jonathan D.; Smith, David W.; Reilly, Michael A.; O'Donnell, Ruth; Lewis, Huw D.; Ellis, Semantha; Wilkie, Neil; Rosahl, Thomas W.; Laroque, Philippe A.; Boussiquet-Leroux, Christine; Churcher, Ian; Atack, John R.; Harrison, Timothy; Shearman, Mark S. Journal of Pharmacology and Experimental Therapeutics (2007),  320(2), 552-558. PubMed 17099072 link
  27. Intra- or Intercomplex Binding to the γ-Secretase Enzyme. A Model to Differentiate Inhibitor Classes.      Clarke, Earl E.; Churcher, Ian; Ellis, Semantha; Wrigley, Jonathan D. J.; Lewis, Huw D.; Harrison, Timothy; Shearman, Mark S.; Beher, Dirk. Journal of Biological Chemistry  (2006),  281(42), 31279-31289. PubMed 16899457 link
  28. Tau therapeutic strategies for the treatment of Alzheimer's disease.      Churcher, Ian.        Current Topics in Medicinal Chemistry (2006), 6(6),  579-595. PubMed 16712493 link
  29. In vivo characterization of Aβ (40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]- 1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat.      Best, Jonathan D.; Jay, Mark T.; Otu, Franklin; Churcher, Ian; Reilly, Michael; Morentin-Gutierrez, Pablo; Pattison, Christine; Harrison, Tim; Shearman, Mark S.; Atack, John R.  Journal of Pharmacology and Experimental Therapeutics  (2006),  317(2),  786-790. PubMed 16443723 link
  30. 4-Substituted cyclohexyl sulfones as potent, orally active γ-secretase inhibitors.      Churcher, Ian; Beher, Dirk; Best, Jonathan D.; Castro, Jose L.; Clarke, Earl E.; Gentry, Amy; Harrison, Timothy; Hitzel, Laure; Kay, Euan; Kerrad, Sonia; Lewis, Huw D.; Morentin-Gutierrez, Pablo; Mortishire-Smith, Russell; Oakley, Paul J.; Reilly, Michael; Shaw, Duncan E.; Shearman, Mark S.; Teall, Martin R.; Williams, Susie; Wrigley, Jonathan D. J. Bioorganic & Medicinal Chemistry Letters (2006),  16(2), 280-284. PubMed 16275079 link
  31. γ-Secretase as a therapeutic target for the treatment of Alzheimer's disease.      Churcher, Ian; Beher, Dirk.    Current Pharmaceutical Design  (2005), 11(26),  3363-3382. PubMed 16250842 link
  32. γ-Secretase as a target for drug intervention in Alzheimer's disease.      Harrison, Timothy; Churcher, Ian; Beher, Dirk.    Current Opinion in Drug Discovery & Development  (2004), 7(5),  709-719. PubMed 15503873
  33. Selected Non-steroidal Anti-inflammatory Drugs and Their Derivatives Target γ-Secretase at a Novel Site: Evidence for an allosteric mechanism.      Beher, Dirk; Clarke, Earl E.; Wrigley, Jonathan D. J.; Martin, Agnes C. L.; Nadin, Alan; Churcher, Ian; Shearman, Mark S.    J. Biol. Chem.  (2004),  279(42), 43419-43426. PubMed 15304503 link
  34. An enantioselective formal total synthesis of (-)-TAN1251A.      Auty, James M. A.; Churcher, Ian; Hayes, Christopher J.   Synlett  (2004),   (8), 1443-1445. Link
  35. Design and Synthesis of Highly Potent Benzodiazepine γ-Secretase Inhibitors: Preparation of (2S,3R)-3-(3,4- Difluorophenyl)-2-(4-fluorophenyl)-4- hydroxy-N-((3S)-1-methyl-2-oxo-5- phenyl-2,3-dihydro-1H-benzo[e][1,4]- diazepin-3-yl)butyramide by Use of an Asymmetric Ireland-Claisen Rearrangement.     Churcher, Ian; Williams, Susie; Kerrad, Sonia; Harrison, Timothy; Castro, Jose L.; Shearman, Mark S.; Lewis, Huw D.; Clarke, Earl E.; Wrigley, Jonathan D. J.; Beher, Dirk; Tang, Yui S.; Liu, Wensheng. Journal of Medicinal Chemistry (2003),  46(12), 2275-2278. PubMed 12773031 link
  36. A new series of potent benzodiazepine γ-secretase inhibitors.      Churcher, Ian; Ashton, Kate; Butcher, John W.; Clarke, Earl E.; Harrison, Timothy; Lewis, Huw D.; Owens, Andrew P.; Teall, Martin R.; Williams, Susie; Wrigley, Jonathan D. J. Bioorganic & Medicinal Chemistry Letters  (2003), 13(2),  179-183. PubMed 12482419 link
  37. Dimerization of o-hydroxycyclohexadienones related to calicheamicinone: SN2 displacement of the 12α -hydroxyl group.      Churcher, Ian; Hallett, David; Magnus, Philip.    Tetrahedron  (1999),  55(6), 1597-1606. Link
  38. Synthesis of the Antitumor Agent Aglycon (±)-Calicheamicinone Using an o-Quinone Monoketal Strategy.      Churcher, Ian; Hallett, David; Magnus, Philip. Journal of the American Chemical Society (1998),  120(40), 10350-10358. Link
  39. Synthesis of the Enediyne Aglycon (±)-Calicheamicinone.      Churcher, Ian; Hallett, David; Magnus, Philip.   Journal of the American Chemical Society  (1998),  120(14),  3518-3519. Link
  40. Stereocontrolled Mukaiyama-type aldol reaction of siloxypyrroles derived from (S)-glutamic acid.      Uno, Hidemitsu; Baldwin, Jack E.; Churcher, Ian; Russell, Andrew T.  Synlett  (1997),   (4),  390-392. Link
  41. Synthesis of the potent potassium channel opener Ro 31-6930 via Claisen rearrangement and tandem regiocontrolled cyclization.      Attwood, Michael R.; Churcher, Ian; Dunsdon, Rachel M.; Hurst, David N.; Jones, Philip S.  Tetrahedron Letters  (1991),  32(6), 811-14. Link


           Also inventor on over 20 published and unpublished PCT patent applications

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