Fragment-based drug design relies heavily on structural information for the elaboration and optimisation of hits. The ability to identify neighbouring binding hot spots, energetically favourable interactions and conserved binding motifs in protein structures through X-ray crystallography can inform the evolution of fragments into lead-like compounds through structure-based design. The composition of fragment libraries can be designed and curated to fit this purpose and herein, we describe and compare screening libraries containing compounds comprising between 2 and 18 heavy atoms. We evaluate the properties of the compounds in these libraries and assess their ability to probe protein surfaces for binding hot spots.
Join us for the November edition of the CFBD Seminar Series. A/Prof Anders Bach from the University of Copenhagen will give a talk on Targeting Protein-Protein Interactions Involved in Oxidative Stress using Fragment-Based Drug Discovery.
The Royal Australian Chemical Institute (RACI) is the national professional body for chemists in industry, academia and government and is the primary voice of chemistry in Australia. Every five years the RACI holds a national Congress, with the RACI 2022 National Congress held from 3 to 8 July in Brisbane. This was a significant meeting (last held in 2017) with 1,148 people registered to attend, 615 speakers, 21 exhibitors, 12 sponsors and 325 poster presentations.
The CFBD members were heavily involved in the fabric of this significant meeting. CI Prof Sally-Ann Poulsen (Griffith Uni) was on the RACI2022 Congress Organising Committee and was Symposium Chair of the 4-day Medicinal Chemistry & Chemical Biology Symposium (the largest of all the Symposiums within the Congress). CI Prof Michael Kassiou (Uni Sydney) and Dr Louise Sternicki (Griffith Uni) were invited speakers, with Dr Luke Adams (Monash) and PhD Candidate Ashley Taylor (Monash) giving contributed talks and PhD Candidate Jamie Currie (Monash)- together showcasing the breadth of ARC CFBD research, while ARC CFBD Chief Investigators, ECRs and PhD candidates from the three universities and several of our industry partners were well represented. We were fortunate to have a catch-up dinner during the Congress – meeting face-2-face for the first time and a lot of laughs to be had. ‘The First Scientists’ artwork for the Congress is by Artist Steven Bekue.
Congratulations to Centre Affiliate Dr David Hilko (Griffith Uni) on the award of a Bridge and BridgeTech Industry Fellowship Placement through the MTPConnect QUT (Queensland University of Technology) David will work on site with GRIDD’s industry partner A/Prof Rakesh N. Veedu founder of SynGenis, a Western Australian based company that works in the exciting oligonucleotide research space.
The Bridge and BridgeTech Industry Fellowship Placement
The Bridge and BridgeTech Industry Fellowships, facilitated by QUT and funded by MTPConnect’s Researcher Exchange and Development within Industry (REDI) initiative for the Australian Government’s Medical Research Future Fund, provide up to $10,000 to support the placement of participants and alumni of the Bridge Program and BridgeTech Program within industry. More on the program can be found here.
Compounds Australia, through Therapeutic Innovation Australia (TIA), is part of the National Collaborative Research Infrastructure Strategy (NCRIS), a network of world-class research infrastructure facilities that drives and supports greater innovation in the Australian biomedical research sector and associated economic impact. Recently, CFBD CI Prof Sally-Ann Poulsen was appointed as acting Director of Compounds Australia. Curating Australia’s largest collection of compounds and natural products (~1.5M), Compounds Australia supports 38 national/international member organizations and >250 research projects annually, including the fragment screening campaigns of the CFBD. Monash University, University of Sydney and Griffith University are all member organizations. CFBD CI Prof Jonathan Baell is an existing Advisory Board Member of Compounds Australia. Many of the fragment libraries that are used by the Centre are currently managed by Compounds Australia. Congratulations to Sally-Ann on this excellent new role.
We are delighted to welcome The Australian Nuclear Science and Technology Organisation (ANSTO) as our new Industry Partner to the Centre. ANSTO, Australia’s knowledge centre for nuclear science and engineering, leverages great science to deliver big outcomes. ANSTO partners with scientists and engineers and applies new technologies to provide real-world benefits. Their work improves human health, saves lives, builds our industries, and protects the environment. ANSTO is the home of Australia’s most significant landmark and national infrastructure for research. Thousands of scientists from industry and academia benefit from gaining access to state-of-the-art instruments every year.
Please join us in welcoming Dr Rachel Williamson and Dr Alan Riboldi-Tunnicliffe as our new Partner Investigators. You can also meet them in person at our Joint ANSTO & CSIRO workshop on 12 August 2022. Don’t forget to register your interest with the Centre Manager.