Lathrop GPM Patent Agent Kyle Pedretty, Ph.D., recently co-authored a research article published in Science titled “Late-stage functionalization with strain-release warheads enables tunable covalent inhibition.”
The article describes a significant advance in covalent drug design, introducing a new chemical platform for installing strained warheads with complete cysteine selectivity. The approach provides a promising alternative to conventional covalent reactive groups and may help address longstanding challenges associated with off-target reactivity and toxicity.
The study further demonstrates successful use of these warheads in FDA-approved covalent inhibitor scaffolds, with preclinical in vivo validation highlighting their potential for next-generation therapeutic development. Pedretty’s contribution to the study reflects his scientific background in medicinal chemistry and research experience at the forefront of drug development and selective covalent inhibition.
Read the in Science: Late-stage functionalization with strain-release warheads enables tunable covalent inhibition.