Guanine quadruplexes: Biological relevance and targeting strategies.
Prof. Anne Petitjean
Department of Chemistry
Sinclair Cancer Research Institute
Queen’s University
The past three decades have revealed how much conformational control of nucleic acids impacts their biology. Many aspects of cell regulation are now known to be controlled by nucleic acids non-duplex folding patterns, such as guanine quadruplexes.[1]
It is therefore tempting for synthetic chemists to investigate small molecules that address these particular architectures, in an effort to regulate undesired processes, as in diseased states such as cancer,[1] infections[2] and neurological disorders.[3]
This presentation highlights a few families of guanine quadruplex binders, their promise and limitations, towards possible therapeutic agents and nucleic acids probes.
[1] Kosiol et al. Molecular Cancer 2021, 20, 40.
[2] Zareie et al., Pathogens 2024, 13, 60.
[3] Xu et al. JACS Au, 2021, 1, 2146.
N-heterocyclic carbene platinum complexes: a step forward toward more effective antitumor compounds?
Dr. Stéphane Bellemin-Laponnaz
Institut de physique et de chimie des matériaux de Strasbourg (IPCMS)
Université de Strasbourg & CNRS
The discovery of cisplatin marked a major milestone in the development of effective anticancer therapies. It also stands as a prominent example of translational scientific success, illustrating the power of multidisciplinary research. The clinical success of cisplatin has led chemists to vary the ligands around the platinum metal to improve cisplatin's effectiveness while reducing its side effects. While there have been more failures than successes, key developments in the elucidation of mechanisms of the tumor-resistance properties have been accomplished.
N-heterocyclic carbenes (NHCs) have emerged as promising ligands in organometallic chemistry, which is a relatively recent field with growing impact across areas including bioinorganic research. These ligands fit the prerequisites for metal drug development and recent achievements have demonstrated the great potential of these compounds. The properties of these metal NHC complexes also allow for easy post-functionalization, thus enabling molecular diversity for efficient drug design. Overall, NHC ligands offer exciting new avenues for the advancement of platinum-based anticancer agents.
Organisateurs Jean Marie Lehn & Giulio RAGAZZON
