My guess is we are due a really big pay day.....and soon...4 Jun 2026 15:56
I'll attach the link on my next post
The challenge
Enzyme inhibition is critical across numerous applications,
from consumer products to therapeutics. Traditional
small-molecule inhibitors often lack specificity, while
antibodies face significant limitations in accessing enzyme
active sites, struggle with small-molecule cofactors,
and are unstable in many formulation environments.
A new class of enzyme modulators was needed that
could combine the specificity of biologics with the
stability and accessibility advantages of small molecules,
enabling targeted enzyme inhibition across diverse
biological contexts.
The solution
Aptamer Group applied its Optimer® discovery platform
to develop enzyme inhibitors targeting bacterial enzymes
of the skin microbiome. Multiple Optimer® candidates
were developed and screened for their ability to reduce
enzyme activity. When initial full-length candidates
proved too large to penetrate bacterial cells and reach
the cytosolic enzyme, systematic truncation yielded
smaller fragments that crossed the cell membrane while
retaining inhibitory activity.
The results
Of the 12 Optimer® candidates screened, 7 showed measurable enzyme inhibition (Figure 1). This 58% hit rate
demonstrates robust discovery performance.
Systematic truncation of full-length candidates enabled cellular penetration while retaining inhibitory activity,
demonstrating the platform’s ability to optimise properties like cell permeability alongside target binding. This
addresses a critical limitation of antibodies that cannot access intracellular enzyme targets due to their large size.
Stability testing in mixed skin samples showed that over 95% of the Optimer® remained intact for 77 hours, while
control molecules degraded to less than 20% (Figure 2). This exceptional stability in challenging biological
environments enables sustained enzyme modulation in real-world applications.
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