Novel Modulators of Oncogenic Targets: A Chemical Biology Perspective
Target selection and validation are some of the key bottlenecks in drug discovery.The need for tool compounds to probe for the biological mechanism of the drug target both in vitro and in vivo are becoming increasingly evident. Especially, small molecules with a mode of binding different to a ‘classical’biochemical inhibitor might modulate the target with a surprisingly different biological outcome.Developing a ‘non-classical’ binder needs extensive chemical synthesis to improve the specificity of the probe and biological characterization to study its mode of action. Such compounds can also be used to change the conformational energy landscape of proteins and hence structural characterization of these binders become crucial to understand its mechanism of action. These ‘non-classical’ binders could potentially open up the target for novel mechanisms of modulation with therapeutic potential.