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Immunology and enzymology drug discovery

Profile Summary

Dr. Augustin Amour is a highly experienced pharmaceutical scientist with over 24 years in the industry, primarily at GSK plc. Renowned for his expertise in immunology and molecular pharmacology, particularly in enzyme inhibitors, he has led numerous R&D projects, demonstrating strong leadership and project management skills. Professional Experience: • GSK Medicines Centre (2000-present): • Immunology Project Leader (2019-present): Led functional and chemo-genomic projects, managing teams and translating pre-clinical data into clinical studies. • Respiratory Biology Lead (2006-2018): Managed pre-clinical programs, leading to multiple candidate selections and two First Time in Human studies. • Molecular Discovery Team Leader (2000-2006): Directed a team in developing biochemical and cellular assays for lead identification across various therapeutic areas. Notable Projects: • Developed an inhaled PI3Kδ inhibitor for asthma and COPD, advancing it into late-stage clinical trials. • Led pre-clinical programs resulting in significant advancements in respiratory treatments. Current Role: • Consultant at Kuano: Advising senior management on enzymatic franchises. Academic Background: • PhD in Biochemistry, University of Paris XI. • M.Sc. in Cell Biology, University of Paris VII. Contributions: • Authored over 50 publications and patents. • Council member and trustee at the Biochemical Society, contributing to strategic planning and advancement of biochemical research. Dr. Amour’s extensive background in immunology, molecular pharmacology, and drug discovery, combined with his leadership in various high-impact projects, makes him a valuable consultant and collaborator in the field of pharmaceutical research.

Subject Matter Expertise

• ☆ Biochemistry
• ☆ Enzyme Activity Assays
• ☆ Drug Discovery
• ☆ High Throughput Screening (HTS)
• ☆ Drug Target Identification
• ☆ Hit-to-Lead & Lead Optimization
• ☆ Phenotypic Assays
• ☆ High Content Screening/Imaging
• ☆ Drug Design
• ☆ Allergy & Clinical Immunology
• ☆ Clinical Immunology

Services

• Writing
• Research
• Consulting
• Data & AI

Writing Technical Writing, General Proofreading & Editing, Translation

Research Fact Checking, Gap Analysis, Scientific and Technical Research, Systematic Literature Review

Consulting Scientific and Technical Consulting

Data & AI Data Visualization, Data Processing

Work Experience

Immunology Research Project Leader

GSK Pharmaceutical

January 2018 - April 2024

Respiratory Research Project Leader

GSK Pharmaceutical

January 2006 - December 2017

Biochemical and cellular assay lead

GSK Pharmaceutical

October 1999 - December 2005

Education

Post-doctoral Fellow

Cambridge

June 1996 - September 1999

Certifications

• PhD in Enzymology

  University of Paris

  June 1996 - Present

Publications

JOURNAL ARTICLE

Begg, M., Amour, A., Jarvis, E., Tang, T., Franco, S.S., Want, A., Beerahee, M., Fernando, D., Karkera, Y., Sander, C., et al.(2023). An open label trial of nemiralisib, an inhaled PI3 kinase delta inhibitor for the treatment of Activated PI3 kinase Delta Syndrome . Pulmonary Pharmacology and Therapeutics. 79. Academic Press

Miller, N.A., Graves, R.H., Edwards, C.D., Amour, A., Taylor, E., Robb, O., O’Brien, B., Patel, A., Harrell, A.W., Hessel, E.M.(2022). Physiologically Based Pharmacokinetic Modelling of Inhaled Nemiralisib: Mechanistic Components for Pulmonary Absorption, Systemic Distribution, and Oral Absorption . Clinical Pharmacokinetics. 61. (2). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 281-293. Adis

Candarlioglu, P.L., Dal Negro, G., Hughes, D., Balkwill, F., Harris, K., Screen, H., Morgan, H., David, R., Beken, S., Guenat, O., et al.(2022). Organ-on-a-chip: current gaps and future directions . Biochemical Society Transactions. 50. (2). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 665-673. Portland Press Ltd

Down, K., Amour, A., Anderson, N.A., Barton, N., Campos, S., Cannons, E.P., Clissold, C., Convery, M.A., Coward, J.J., Doyle, K., et al.(2021). Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode . Journal of Medicinal Chemistry. 64. (18). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 13780-13792. American Chemical Society

Clapp, N., Amour, A., Rowan, W.C., Candarlioglu, P.L.(2021). Organ-on-chip applications in drug discovery: An end user perspective . Biochemical Society Transactions. 49. (4). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 1881-1890. Portland Press Ltd

Begg, M., Hamblin, J.N., Jarvis, E., Bradley, G., Mark, S., Michalovich, D., Lennon, M., Wajdner, H.E., Amour, A., Wilson, R., et al.(2021). Exploring PI3Kδ molecular pathways in stable COPD and following an acute exacerbation, two randomized controlled trials . International Journal of COPD. 16. Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 1621-1636. Dove Medical Press Ltd

Uddin, S., Amour, A., Lewis, D.J., Edwards, C.D., Williamson, M.G., Hall, S., Lione, L.A., Hessel, E.M.(2021). PI3Kδ inhibition prevents IL33, ILC2s and inflammatory eosinophils in persistent airway inflammation . BMC Immunology. 22. (1). BioMed Central Ltd

Michael, M., McCormick, B., Anderson, K.E., Karmakar, U., Vermeren, M., Schurmans, S., Amour, A., Vermeren, S.(2021). The 5-Phosphatase SHIP2 Promotes Neutrophil Chemotaxis and Recruitment . Frontiers in Immunology. 12. Frontiers Media S.A.

Henley, Z.A., Amour, A., Barton, N., Bantscheff, M., Bergamini, G., Bertrand, S.M., Convery, M., Down, K., Dümpelfeld, B., Edwards, C.D., et al.(2020). Optimization of Orally Bioavailable PI3KδInhibitors and Identification of Vps34 as a Key Selectivity Target . Journal of Medicinal Chemistry. 63. (2). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 638-655. American Chemical Society

Lima, B.H.F., Marques, P.E., Gomides, L.F., Mattos, M.S., Kraemer, L., Queiroz-Junior, C.M., Lennon, M., Hirsch, E., Russo, R.C., Menezes, G.B., et al.(2019). Converging TLR9 and PI3Kgamma signaling induces sterile inflammation and organ damage . Scientific Reports. 9. (1). Nature Research

Begg, M., Wilson, R., Hamblin, J.N., Montembault, M., Green, J., Deans, A., Amour, A., Worsley, S., Fantom, K., Cui, Y., et al.(2019). Relationship between pharmacokinetics and pharmacodynamic responses in healthy smokers informs a once-daily dosing regimen for nemiralisib . Journal of Pharmacology and Experimental Therapeutics. 369. (3). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 337-344. American Society for Pharmacology and Experimental Therapy

Khan, A., Southworth, T., Worsley, S., Sriskantharajah, S., Amour, A., Hessel, E.M., Singh, D.(2017). An investigation of the anti-inflammatory effects and a potential biomarker of PI3Kδ inhibition in COPD T cells . Clinical and Experimental Pharmacology and Physiology. 44. (9). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 932-940. Blackwell Publishing

Juss, J.K., House, D., Amour, A., Begg, M., Herre, J., Storisteanu, D.M.L., Hoenderdos, K., Bradley, G., Lennon, M., Summers, C., et al.(2016). Acute respiratory distress syndrome neutrophils have a distinct phenotype and are resistant to phosphoinositide 3-kinase inhibition . American Journal of Respiratory and Critical Care Medicine. 194. (8). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 961-973. American Thoracic Society

Amour, A., Barton, N., Cooper, A.W.J., Inglis, G., Jamieson, C., Luscombe, C.N., Morrell, J., Peace, S., Perez, D., Rowland, P., et al.(2016). Evolution of a Novel, Orally Bioavailable Series of PI3KΔ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease . Journal of Medicinal Chemistry. 59. (15). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 7239-7251. American Chemical Society

Gupta, V., Khan, A., Higham, A., Lemon, J., Sriskantharajah, S., Amour, A., Hessel, E.M., Southworth, T., Singh, D.(2016). The effect of phosphatidylinositol-3 kinase inhibition on matrix metalloproteinase-9 and reactive oxygen species release from chronic obstructive pulmonary disease neutrophils . International Immunopharmacology. 35. Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 155-162. Elsevier B.V.

Down, K., Amour, A., Baldwin, I.R., Cooper, A.W.J., Deakin, A.M., Felton, L.M., Guntrip, S.B., Hardy, C., Harrison, Z.A., Jones, K.L., et al.(2015). Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease . Journal of Medicinal Chemistry. 58. (18). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 7381-7399. American Chemical Society

Sriskantharajah, S., Hamblin, N., Worsley, S., Calver, A.R., Hessel, E.M., Amour, A.(2013). Targeting phosphoinositide 3-kinase δ for the treatment of respiratory diseases . Annals of the New York Academy of Sciences. 1280. (1). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 35-39. Blackwell Publishing Inc.

Rowan, W.C., Smith, J.L., Affleck, K., Amour, A.(2012). Targeting phosphoinositide 3-kinase δ for allergic asthma . Biochemical Society Transactions. 40. (1). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 240-245.

Willenbrock, F., Thomas, D.A., Amour, A.(2010). Kinetic analysis of the inhibition of matrix metalloproteinases: lessons from the study of tissue inhibitors of metalloproteinases . Methods in molecular biology (Clifton, N.J.). 622. Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 435-450.

Alvarez-Iglesias, M., Wayne, G., O'Dea, K.P., Amour, A., Takata, M.(2009). Continuous real-time measurement of tumor necrosis factor-α converting enzyme activity on live cells (Laboratory Investigation (2005) 85 (1440-1448) doi: 10.1038/labinvest.3700340) . Laboratory Investigation. 89. (1). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 106.

Holmes, I.P., Gaines, S., Watson, S.P., Lorthioir, O., Walker, A., Baddeley, S.J., Herbert, S., Egan, D., Convery, M.A., Singh, O.M.P., et al.(2009). The identification of β-hydroxy carboxylic acids as selective MMP-12 inhibitors . Bioorganic and Medicinal Chemistry Letters. 19. (19). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 5760-5763.

Li, M., Luraghi, P., Amour, A., Qian, X.-D., Carter, P.S., Clark, C.J., Deakin, A., Denyer, J., Hobbs, C.I., Surby, M., et al.(2009). Kinetic assay for characterization of spleen tyrosine kinase activity and inhibition with recombinant kinase and crude cell lysates . Analytical Biochemistry. 384. (1). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 56-67. Academic Press Inc.

Abboud, M.A., Needle, S.J., Burns-Kurtis, C.L., Valocik, R.E., Koster, P.F., Amour, A.J., Chan, C., Brown, D., Chaudry, L., Zhou, P., et al.(2008). Antithrombotic potential of GW813893: A novel, orally active, active-site directed factor Xa inhibitor . Journal of Cardiovascular Pharmacology. 52. (1). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 66-71. Lippincott Williams and Wilkins

Wayne, G.J., Deng, S.-J., Amour, A., Borman, S., Matico, R., Carter, H.L., Murphy, G.(2007). TIMP-3 inhibition of ADAMTS-4 (Aggrecanase-1) is modulated by interactions between aggrecan and the C-terminal domain of ADAMTS-4 . Journal of Biological Chemistry. 282. (29). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 20991-20998.

Amour, A., Hutchinson, J., Ruiz Avendaño, A.M., Ratcliffe, S., Alvarez, E., Martin, J., Toomey, J.R., Senger, S., Wolfendale, M., Mooney, C.(2007). The quest for Factor VIIa exosite inhibitors . Biochemical Society Transactions. 35. (3). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 555-558.

Ohtsuka, T., Shiomi, T., Shimoda, M., Kodama, T., Amour, A., Murphy, G., Ohuchi, E., Kobayashi, K., Okada, Y.(2006). ADAM28 is overexpressed in human non-small cell lung carcinomas and correlates with cell proliferation and lymph node metastasis . International Journal of Cancer. 118. (2). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 263-273.

Thomas, D.A., Francis, P., Smith, C., Ratcliffe, S., Ede, N.J., Kay, C., Wayne, G., Martin, S.L., Moore, K., Amour, A., et al.(2006). A broad-spectrum fluorescence-based peptide library for the rapid identification of protease substrates . Proteomics. 6. (7). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 2112-2120.

Alvarez-Iglesias, M., Wayne, G., O'Dea, K.P., Amour, A., Takata, M.(2005). Continuous real-time measurement of tumor necrosis factor-α converting enzyme activity on live cells . Laboratory Investigation. 85. (11). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 1440-1448. Nature Publishing Group

Amour, A., Bird, M., Chaudry, L., Deadman, J., Hayes, D., Kay, C.(2004). General considerations for proteolytic cascades . Biochemical Society Transactions. 32. (1). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 15-16.

Scholefield, Z., Yates, E.A., Wayne, G., Amour, A., McDowell, W., Turnbull, J.E.(2003). Heparan sulfate regulates amyloid precursor protein processing by BACE1, the Alzheimer's β-secretase . Journal of Cell Biology. 163. (1). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 97-107.

Murphy, G., Knäuper, V., Lee, M.-H., Amour, A., Worley, J.R., Hutton, M., Atkinson, S., Rapti, M., Williamson, R.(2003). Role of TIMPs (tissue inhibitors of metalloproteinases) in pericellular proteolysis: The specificity is in the detail . Biochemical Society Symposium. (70). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 65-80. Portland Press Ltd

Seibel, J., Brown, D., Amour, A., Macdonald, S.J., Oldham, N.J., Schofield, C.J.(2003). Synthesis and evaluation of δ-lactams (piperazones) as elastase inhibitors . Bioorganic and Medicinal Chemistry Letters. 13. (3). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 387-389.

Amour, A., English, W.R., Knäuper, V., Murphy, G., Webster, A., Slocombe, P.M., Docherty, A.J.P., Knight, C.(2002). The enzymatic activity of ADAM8 and ADAM9 is not regulated by TIMPs . FEBS Letters. 524. (1-3). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 154-158.

Heudi, O., Ramirez-Molina, C., Marshall, P., Amour, A., Peace, S., Mckeown, S., Abou-Shakra, F.(2002). Investigation of bradykinin metabolism in human and rat plasma in the presence of the dual ACE/NEP inhibitors GW660511X and omapatrilat . Journal of Peptide Science. 8. (11). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 591-600.

Marshall, P., Heudi, O., Mckeown, S., Amour, A., Abou-Shakra, F.(2002). Study of bradykinin metabolism in human and rat plasma by liquid chromatography with inductively coupled plasma mass spectrometry and orthogonal acceleration time-of-flight mass spectrometry . Rapid Communications in Mass Spectrometry. 16. (3). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 220-228. John Wiley and Sons Ltd

Lee, M.-H., Verma, V., Maskos, K., Becherer, J.D., Knäuper, V., Dodds, P., Amour, A., Murphy, G.(2002). The C-terminal domains of TACE weaken the inhibitory action of N-TIMP-3 . FEBS Letters. 520. (1-3). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 102-106.

Lee, M.-H., Verma, V., Maskos, K., Nath, D., Knäuper, V., Dodds, P., Amour, A., Murphy, G.(2002). Engineering N-terminal domain of tissue inhibitor of metalloproteinase (TIMP)-3 to be a better inhibitor against tumour necrosis factor-α-converting enzyme . Biochemical Journal. 364. (1). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 227-234. Portland Press Ltd

Macdonald, S.J.F., Dowle, M.D., Harrison, L.A., Clarke, G.D.E., Inglis, G.G.A., Johnson, M.R., Shah, P., Smith, R.A., Amour, A., Fleetwood, G., et al.(2002). Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151) . Journal of Medicinal Chemistry. 45. (18). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 3878-3890.

Kress, J., Zanaletti, R., Amour, A., Ladlow, M., Frey, J.G., Bradley, M.(2002). Enzyme accessibility and solid supports: Which molecular weight enzymes can be used on solid supports? An investigation using confocal raman microscopy . Chemistry - A European Journal. 8. (16). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 3769-3772.

Macdonald, S.J.F., Dowle, M.D., Harrison, L.A., Shah, P., Johnson, M.R., Inglis, G.G.A., Clarke, G.D.E., Smith, R.A., Humphreys, D., Molloy, C.R., et al.(2001). The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase - GW311616A a development candidate . Bioorganic and Medicinal Chemistry Letters. 11. (7). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 895-898.

Amour, A., Knight, C.G., Webster, A., Slocombe, P.M., Stephens, P.E., Knäuper, V., Docherty, A.J.P., Murphy, G.(2000). The in vitro activity of ADAM-10 is inhibited by TIMP-1 and TIMP-3 . FEBS Letters. 473. (3). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 275-279.

Bond, M., Murphy, G., Bennett, M.R., Amour, A., Knäuper, V., Newby, A.C., Baker, A.H.(2000). Localization of the death domain of tissue inhibitor of metalloproteinase-3 to the N terminus: Metalloproteinase inhibition is associated with proapoptotic activity . Journal of Biological Chemistry. 275. (52). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 41358-41363.

English, W.R., Puente, X.S., Freije, J.M.P., Knäuper, V., Amour, A., Merryweather, A., López-Otín, C., Murphy, G.(2000). Membrane type 4 matrix metalloproteinase (MMP17) has tumor necrosis factor-α convertase activity but does not activate pro-MMP2 . Journal of Biological Chemistry. 275. (19). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 14046-14055.

Amour, A., Hutton, M., Knäuper, V., Slocombe, P.M., Webster, A., Butler, M., Knight, C.G., Smith, B.J., Docherty, A.J.P., Murphy, G.(1999). Inhibition of the metalloproteinase domain of mouse TACE . Annals of the New York Academy of Sciences. 878. Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 728-731. New York Academy of Sciences

Guy, L., Vidal, J., Collet, A., Amour, A., Reboud-Ravaux, M.(1998). Design and synthesis of hydrazinopeptides and their evaluation as human leukocyte elastase inhibitors . Journal of Medicinal Chemistry. 41. (24). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 4833-4843.

Amour, A., Reboud-Ravaux, M., De Rosny, E., Abouabdellah, A., Bégué, J.-P., Bonnet-Delpon, D., Le Gall, M.(1998). Stereoselective synthesis of peptidyl trifluoromethyl alcohols and ketones: Inhibitory potency against human leucocyte elastase, cathepsin G, porcine pancreatic elastase and HIV-1 protease . Journal of Pharmacy and Pharmacology. 50. (6). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 593-600. Blackwell Publishing Ltd

Amour, A., Slocombe, P.M., Webster, A., Butler, M., Knight, C.G., Smith, B.J., Stephens, P.E., Shelley, C., Hutton, M., Knäuper, V., et al.(1998). TNF-α converting enzyme (TACE) is inhibited by TIMP-3 . FEBS Letters. 435. (1). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 39-44.

Amour, A., Smaoui, H., Heudes, D., Reboud-Ravaux, M.(1996). Protection of rat lung from elastase-lnduced elastic fiber degradation in vitro and from emphysema in vivo by a trifluoroacetylpeptide anilide inhibitor . Respiration. 63. (5). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 277-282.

Reboud-Ravaux, M.C., Boggetto, N.D., Doucet, C.E., De Rosny, È.H., Vergely, I.B., Thierry, N.M., Amour, A.J.(1996). Synthetic inhibitors targeting serine and aspartic proteases as potential drugs [INHIBITEURS SYNTHETIQUES A VISEE PHARMACOLOGIQUE CIBLANT LES PROTEASES A SERINE ET A ACIDES ASPARTIQUES] . Journal de Pharmacie de Belgique. 51. (3). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 161-164.

Bégué, J.-P., Bonnet-Delpon, D., Fischer-Durand, N., Amour, A., Reboud-Ravaux, M.(1994). Stereoselective synthesis and inhibitor properties towards human leucocyte elastase of chiral β-peptidyl trifluoromethyl alcohols . Tetrahedron: Asymmetry. 5. (6). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 1099-1110.

AMOUR, A., COLLET, A., DUBAR, C., REBOUD‐RAVAUX, M.(1994). Synthesis and protease‐catalyzed hydrolysis of a novel hydrazinopeptide . International Journal of Peptide and Protein Research. 43. (3). Microsoft.AspNetCore.Mvc.Localization.LocalizedHtmlString 297-304.