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Area of Science:

  • Biochemistry
  • Pharmacology
  • Cancer Biology

Background:

  • Lactate dehydrogenase (LDH) is crucial for cancer cell metabolism via glycolysis.
  • Targeting LDH is a promising therapeutic strategy for cancer treatment.
  • Previous inhibitors lacked sufficient in vivo efficacy due to high target concentrations.

Purpose of the Study:

  • To identify potent and selective lactate dehydrogenase (LDH) inhibitors.
  • To overcome challenges of in vivo target engagement for LDH inhibitors.
  • To develop first-in-class inhibitors demonstrating in vivo LDH inhibition.

Main Methods:

  • Structure-based drug design for pyrazole-based compounds.
  • Optimization of cellular potency and in vitro drug-target residence times.
  • Evaluation of in vivo pharmacokinetic (PK) properties and target engagement.

Main Results:

  • Identification of lead compounds NCATS-SM1440 and NCATS-SM1441.
  • Demonstrated successful in vivo inhibition of lactate dehydrogenase (LDH).
  • Achieved desirable drug properties for further in vivo studies.

Conclusions:

  • Developed novel pyrazole-based inhibitors targeting lactate dehydrogenase (LDH).
  • These compounds show potential for studying the therapeutic effects of in vivo LDH inhibition.
  • Represents a significant advancement in developing effective LDH-targeted cancer therapies.