Biography:Edward Roberts (chemist)

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Edward Roberts FRSC., is  a British-born American scientist with expertise in biochemistry and synthetic organic chemistry. He is recognized for his significant contributions to medicinal chemistry, the design and discovery of new medicines in the development of novel therapeutics.[1][2]

Education and early career

Edward Roberts pursued his undergraduate studies in biochemistry with a minor in music at the University of Sussex, Brighton, England, earning a Bachelor of Science with Honors degree in 1979.[citation needed] He continued his academic journey with a Ph.D. in synthetic organic chemistry at the University of Newcastle-upon-Tyne, England, under Richard J Stoodley, completing his doctoral studies in 1982.[citation needed]

Career

Roberts worked at the Adden Brookes Hospital Forvie site in Cambridge (UK) for Parke Davis.[3][4][5]

Roberts held the position of senior vice president and Head of Chemistry at F. Hoffmann-La Roche in Basel, Switzerland. He further contributed his expertise as a director and Head of Chemistry at AstraZeneca R&D in Montreal, Canada. He was an adjunct professor in the Department of Chemistry at McGill University, Montreal, Canada. [citation needed]

Roberts was the President and Chief Science Officer at Kémia, a drug development company located in San Diego, California. He currently[when?] serves as a professor in the Departments of Chemistry and Molecular Medicine at Scripps Research in La Jolla, California.

Contributions to medicinal chemistry since joining Scripps research

  • Novel treatments for autoimmune disorders: Edward Roberts and his team designed and synthesized a selective and bitopic S1P1 agonist, RPC1063. This compound showed promise as a safe treatment for autoimmune diseases such as multiple sclerosis, ulcerative colitis, and Crohn's disease. Ozanimod (RPC1063), now marketed as Zeposia, has been approved for use in relapsing multiple sclerosis and inflammatory bowel disease.[6][7]
  • Novel treatments for neuropsychiatric and behavioral Disorders: Roberts' lab designed and developed a series of kappa opioid antagonists for stress-related mood disorders, migraine, and other neuropsychiatric conditions. One such antagonist, Navacaprant (formerly CYM-53093, BTRX-335140), exhibited robust efficacy in early clinical trials and is currently in multiple phase 3 trials for major depressive diseases.[8]
  • Compounds for use in the treatment of autistic spectrum disorders and/or post-traumatic stress disorders: Roberts' team designed and synthesized novel and improved V1a antagonists for potential therapeutic use in various neuropsychological disorders. One representative molecule NMRA-511 is currently in phase 2 clinical trials.[9]
  • Novel compounds for use in fibrotic diseases: Roberts' research explored the therapeutic potential of subtype 3 of the sphingosine-1-phosphate receptors as targets for cardiovascular and pulmonary diseases, fibrosis, and other related conditions.[10]
  • Novel compounds for use in seizures; Roberts and colleagues explored the use of Galanin receptor agonists to delay and prevent seizures in animals displaying excellent activity and better mortality outcomes than current first line treatment.[11][12]

Patents and recognition

Roberts is a inventor or co-inventor on over 100 issued patents. He has received the E.B. Hershberg award and induction into the MEDI Hall of Fame in 2021.[citation needed] He has also been involved in the commercialization of some of his research, contributing to the establishment of biotech companies such as Receptos Pharmaceuticals and BlackThorn Pharmaceuticals.[citation needed] He is a member of the Royal Society of Chemistry, the Royal Society of Medicine, and the Medicinal Chemistry division of the American Chemical Society.[13][14][15][16][17]

References

  1. ↑ Ito, Hisakatsu; Navratilova, Edita; Vagnerova, Barbora; Watanabe, Moe; Kopruszinski, Carol; Moreira de Souza, Luiz H; Yue, Xu; Ikegami, Daigo et al. (2022-04-29). "Chronic pain recruits hypothalamic dynorphin/kappa opioid receptor signalling to promote wakefulness and vigilance". Brain 146 (3): 1186–1199. doi:10.1093/brain/awac153. ISSN 0006-8950. PMID 35485490. PMC 10169443. http://dx.doi.org/10.1093/brain/awac153. 
  2. ↑ Burkert, Kerstin; Zellmann, Tristan; Meier, René; Kaiser, Anette; Stichel, Jan; Meiler, Jens; Mittapalli, Gopi K.; Roberts, Edward et al. (2017-01-05). "A Deep Hydrophobic Binding Cavity is the Main Interaction for Different Y 2 R Antagonists" (in en). ChemMedChem 12 (1): 75–85. doi:10.1002/cmdc.201600433. https://onlinelibrary.wiley.com/doi/10.1002/cmdc.201600433. 
  3. ↑ Harris, R. Adron; Bajo, Michal; Bell, Richard L.; Blednov, Yuri A.; Varodayan, Florence P.; Truitt, Jay M.; de Guglielmo, Giordano; Lasek, Amy W. et al. (2017-02-01). "Genetic and Pharmacologic Manipulation of TLR4 Has Minimal Impact on Ethanol Consumption in Rodents" (in en). The Journal of Neuroscience 37 (5): 1139–1155. doi:10.1523/JNEUROSCI.2002-16.2016. ISSN 0270-6474. PMID 27986929. 
  4. ↑ Beckerman, Josh; Rockoff, Jon D.; Rockoff, Jonathan D. (2015-07-14). "Celgene to Buy Receptos for $7.2 Billion" (in en-US). Wall Street Journal. ISSN 0099-9660. http://www.wsj.com/articles/celgene-to-buy-receptos-for-about-7-2-billion-1436908831. 
  5. ↑ "Updated: J&J backs neuro startup BlackThorn in $40M Series A". 8 August 2023. https://www.fiercebiotech.com/biotech/j-j-backs-neuro-startup-blackthorn-40m-series-a. 
  6. ↑ Crockett Sneed, M. (1998). "125 years of patent information to the people: the US Patent and Trademark Depository Library Program, 22 May 1997". World Patent Information 20 (2): 129–133. doi:10.1016/s0172-2190(98)00032-5. ISSN 0172-2190. http://dx.doi.org/10.1016/s0172-2190(98)00032-5. 
  7. ↑ US Navy, ALUSNA Taipei to CINCFE et al., November 28, 1950, Top Secret/US Military Eyes Only, MACL.. doi:10.1163/9789004346185.usao-02_426. http://dx.doi.org/10.1163/9789004346185.usao-02_426. Retrieved 2023-08-30. 
  8. ↑ Cable, EC 9-2613, US CINCEUR to DEPTAR et al., June 17, 1954, Top Secret.. doi:10.1163/ejb9789004244627.b03285. http://dx.doi.org/10.1163/ejb9789004244627.b03285. Retrieved 2023-08-30. 
  9. ↑ Allwood, M (1999). "Reply to Dr. Lindström et al.". Clinical Nutrition 18 (5): 323. doi:10.1016/s0261-5614(99)80025-9. ISSN 0261-5614. http://dx.doi.org/10.1016/s0261-5614(99)80025-9. 
  10. ↑ Scott, F L; Clemons, B; Brooks, J; Brahmachary, E; Powell, R; Dedman, H; Desale, H G; Timony, G A et al. (2016). "Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P 1 ) and receptor-5 (S1P 5 ) agonist with autoimmune disease-modifying activity: Ozanimod: a S1P 1,5 receptor agonist for autoimmune disease" (in en). British Journal of Pharmacology 173 (11): 1778–1792. doi:10.1111/bph.13476. PMID 26990079. 
  11. ↑ Lu, Xiaoying; Roberts, Edward; Xia, Fengcheng; Sanchez-Alavez, Manuel; Liu, Tianyu; Baldwin, Roger; Wu, Stephanie; Chang, James et al. (2010-08-24). "GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal models" (in en). Proceedings of the National Academy of Sciences 107 (34): 15229–15234. doi:10.1073/pnas.1008986107. ISSN 0027-8424. PMID 20660766. 
  12. ↑ Dillmann, Christina; Ringel, Christian; Ringleb, Julia; Mora, Javier; Olesch, Catherine; Fink, Annika F.; Roberts, Edward; Brüne, Bernhard et al. (2016-02-15). "S1PR4 Signaling Attenuates ILT 7 Internalization To Limit IFN-α Production by Human Plasmacytoid Dendritic Cells" (in en). The Journal of Immunology 196 (4): 1579–1590. doi:10.4049/jimmunol.1403168. ISSN 0022-1767. https://journals.aai.org/jimmunol/article/196/4/1579/43273/S1PR4-Signaling-Attenuates-ILT-7-Internalization. 
  13. ↑ Urbano, Mariangela; Guerrero, Miguel; Rosen, Hugh; Roberts, Edward (May 2014). "Antagonists of the kappa opioid receptor" (in en). Bioorganic & Medicinal Chemistry Letters 24 (9): 2021–2032. doi:10.1016/j.bmcl.2014.03.040. https://linkinghub.elsevier.com/retrieve/pii/S0960894X14002674. 
  14. ↑ Roberts, Edward; Guerrero, Miguel; Urbano, Mariangela; Rosen, Hugh (2013). "Sphingosine 1-phosphate receptor agonists: a patent review (2010 – 2012)" (in en). Expert Opinion on Therapeutic Patents 23 (7): 817–841. doi:10.1517/13543776.2013.783022. ISSN 1354-3776. http://www.tandfonline.com/doi/full/10.1517/13543776.2013.783022. 
  15. ↑ Rosen, Hugh; Stevens, Raymond C.; Hanson, Michael; Roberts, Edward; Oldstone, Michael B.A. (2013-06-02). "Sphingosine-1-Phosphate and Its Receptors: Structure, Signaling, and Influence" (in en). Annual Review of Biochemistry 82 (1): 637–662. doi:10.1146/annurev-biochem-062411-130916. ISSN 0066-4154. https://www.annualreviews.org/doi/10.1146/annurev-biochem-062411-130916. 
  16. ↑ Cencetti, Francesca; Bernacchioni, Caterina; Tonelli, Francesca; Roberts, Edward; Donati, Chiara; Bruni, Paola (2013). "TGFβ1 evokes myoblast apoptotic response via a novel signaling pathway involving S1P 4 transactivation upstream of Rho‐kinase‐2 activation" (in en). The FASEB Journal 27 (11): 4532–4546. doi:10.1096/fj.13-228528. ISSN 0892-6638. https://onlinelibrary.wiley.com/doi/abs/10.1096/fj.13-228528. 
  17. ↑ Sekar, Divya; Hahn, Christina; Brüne, Bernhard; Roberts, Edward; Weigert, Andreas (2012). "Apoptotic tumor cells induce IL-27 release from human DCs to activate Treg cells that express CD69 and attenuate cytotoxicity: Immunomodulation" (in en). European Journal of Immunology 42 (6): 1585–1598. doi:10.1002/eji.201142093. PMID 22678911. 



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