KRAS is one of the most frequently mutated oncogenes in human cancer. Despite more than three decades of research, indirect approaches targeting KRAS-mutant cancers have largely failed to show clinical benefit, and direct approaches have historically been stymied by the apparently ‘undruggable’ nature of KRAS.  In this case study, I’ll describe efforts at Amgen to identify cysteine-reactive molecules capable of selectively inhibiting a prevalent mutated form of KRAS, KRASG12C.  These efforts leveraged iterative screening and structural biology studies, property-based optimization, and careful process engineering to deliver a highly potent and selective covalent inhibitor of KRASG12C: sotorasib (LUMAKRAS®/LUMYKRAS®).  I'll also describe structural insights into the allosteric inhibition of KRASG12C and their implications for inhibitor efficacy and selectivity.

Register for free here.

#GDCh (MedChem Division), #NextGenMedChem.

Renowned International Speakers from France, Italy, Germany and Spain together with established Greek colleagues from universities all over Greece will share their scientific experience, expertise and knowledge with all delegates and they will exchange opinions.  

Scientific Committee recommends abstracts submission (Oral or Poster) through https://helmedchem2023.gr/abstracts/ and encourages scientists to present their scientific work and share their achievements with delegates from all over the world.  

For live or digital attendance, you may register through https://helmedchem2023.gr/registration/. All delegates (live or digital attendance) will get Certificate of Attendance.

The venue of the symposium is in the Conference and Cultural Centre of the University of Patras, a pole for international conferences and the main tool for the development of the cultural life of the region.

Looking forward to welcoming you at Patras for a memorable Symposium in a friendly and warn atmosphere in which we will share our love for Medicinal Chemistry.

The international symposium will focus on current developments, novel approaches and cutting-edge technologies in the field of medicinal chemistry and drug research with sessions on 

• First Disclosures & Medicinal Chemistry Highlights
• Molecular Glues & Degraders
• RNA-Modifying Enzymes
• Translational Science Case Studies
• New Chemical Technologies
• Young Investigators.

The scientific program will include lectures, and poster presentations. It is the goal of the organizers to make this meeting an event of scientific excellence, attractive to both industrial and academic scientists in Medicinal Chemistry, Chemical Biology, and related fields of research.

More information and registration available here.

7^th RSC-BMCS Mastering Medicinal Chemistry

22^nd March 2023, Burlington House

Website: https://www.rscbmcs.org/events/mastermedchem23/

Synopsis: Mastering Medicinal Chemistry VII is the latest in an ongoing series of conferences intended to provide expert advice and guidance to new practitioners in the field of drug discovery. It has been said that “there are two types of drug discovery programmes: those that hit serious problems and those that are going to hit serious problems”. Anticipating and preparing for such problems thus accelerates the delivery of new medicines: this event will feature presentations from experienced ‘drug-hunters’ in both industry and academia, who will talk about the challenges faced in modern drug discovery and will share best practice common to all successful medicinal chemists.

7^th RSC-BMCS / SCI Symposium on Ion Channels as Therapeutic Targets
27^th and 28^th March 2023, Wellcome Genome Campus, Cambridge

Website: https://www.rscbmcs.org/ionchannels23

Synopsis:  Ion channels are important targets for therapeutic intervention due to their extensive roles in human physiology and the pathophysiology of disease. Many successful drugs targeting this gene family have been discovered for diseases such as hypertension, epilepsy and neuropathic pain.

This symposium, the 7th in an ongoing series, will showcase the most recent advances to aid the design of new ion channel therapeutics and promote interaction between scientists with a shared interest in the field of ion channel drug discovery.

10^th SCI/RSC Kinase Symposium on Inhibitor Design

9^thand 10^th May 2023, SCI, London, UK

Website:  https://www.rscbmcs.org/events/kinase/

Synopsis:  With more than 70 FDA-approved small molecules, the field of kinase inhibition continues to attract significant investment from the drug discovery and development community. The 10th SCI/RSC symposium on kinases will encompass plenary lectures on emergent topics and case studies of ongoing programmes as well as successful past programmes. A range of topics including new screening approaches, brain penetrant kinase inhibitors, induced protein degradation, allosteric inhibitors and kinase inhibition for immuno-oncology will be covered, along with views and perspectives on the future of kinase inhibitor research

3^rd Synthesis in Drug Discovery and Development

23^rd – 24^th May 2023, Virtual

Poster abstract closing date is 22^nd February, 2023

Website:  https://www.rscbmcs.org/events/sddd23/

Synopsis:  Synthesis is at the heart of drug discovery and development. The industry has increasingly demanded higher quality clinical candidates and has sought to exploit less druggable biological targets. Densely functionalised small molecules with a high degree of synthetic complexity are often the result of these demands. Successful programmes therefore require the application of innovative synthesis in all stages of discovery and development. The medicinal chemist’s toolbox is also enhanced by the introduction of novel bioisosteres, often made available only through the application of new synthetic methods. This symposium aimed to celebrate the crucial role of synthesis in the success of drug discovery and development

3^rd RSC Anglo-Nordic Medicinal Chemistry Symposium

13^th-16^th June 2023, Hotel Comwell Borupgaard, Snekkersten, Denmark

Deadline for poster abstracts is 4^th May 2023

Website:  https://www.rscbmcs.org/events/anmc/  

Synopsis:  Organised with Nordic affiliations, the scientific programme will feature themed lectures, focusing on medicinal chemistry and related technologies and disciplines across a range of drug targets and modalities. A distinguishing feature of this symposium is the collegiate style which encourages an atmosphere of information sharing and learning.