Efthymios Gavriil received a bursary to attend the SCI/RSC Medicinal Chemistry Symposium in Cambridge in September 2023. Read his event report below:
"Throughout the talks, the concept of ‘undruggable targets’ was constantly challenged, as in the cases of brain penetrant KRAS inhibitors, SOS1 inhibitors which prevent KRAS activation and small molecules targeting IL-1b. Furthermore, the benefit of exploiting allosteric domains was exemplified by the extraordinary potency and selectivity of a novel TYK2-JH2 inhibitor. Positive and negative allosteric CNS receptor modulators as well as kinase, lipase and ion channel inhibitors were also showcased with impressive therapeutic potential for CNS disorders.
"We were introduced to arginase inhibitors for enhancement of T-cell anti-tumour response, as well as NMT, CTPS1, SHP2, pan-BET bromodomain and protein-protein interaction inhibitors for treatment of cancer. The power of AI-driven drug discovery was also shown in a case of A2AR antagonists. Novel targets and drug candidates were presented against inflammation, malaria, acne, diabetic foot ulcers, angioedema, kidney and infectious diseases. Especially in the field of antivirals, the story of the first-in-class, long-acting HIV capsid inhibitor Lenacapavir fascinated everyone in the room, whereas the discovery of next generation, unboosted HIV protease and SARS-CoV-2 oral protease inhibitors demonstrated that state-of-the-art drug design can achieve the impossible.
"One of the highlights of the symposium was of course, the presentation of the Malcolm Campbell memorial prize to Charles Coombe and Matt Fuchter, who discovered at Imperial College London, CDK7 inhibitors as a novel anti-cancer therapy. Moreover, RSC Hall of Fame winner, Karin Brinner, delivered an inspiring lecture on the past, present and future of drug discovery. It is important that we, as a drug discovery community, reflect on all the hurdles we have overcome and the challenges we face, while we are getting better equipped with new technologies and emerging modalities.
"Apart from all the wonderful talks, the programme included poster sessions and flash presentations, which gave the opportunity to many young researchers, like me, to engage with the audience and present our research. Additionally, on the first day of the symposium, I had the chance to attend a medicinal chemistry workshop designed for young drug hunters. Through a fun, interactive, ‘game-like’ process, we worked together in small teams experiencing the discovery process of new drugs, from hit identification to nomination of clinical candidates. A dedicated team of professional medicinal chemists from the pharmaceutical industry facilitated our learning experience and helped us understand key factors, which drive drug discovery projects.
"Overall, the SCI / RSC 22nd Medicinal Chemistry Symposium was a fantastic event, representative of the high quality of modern medicinal chemistry and drug discovery. I am grateful to the SCI / RSC for the bursary award that gave me the opportunity to attend this conference and witness the latest advancements in the field. I am sure that everyone is already looking forward to coming back to Cambridge for the next symposium!"
Dr Efthymios S. Gavriil, PhD MRSC
Research Associate in Medicinal Chemistry and Cancer Drug Discovery
Imperial College London
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