MidWest Drug Development Conference
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2021-10-04 08:00:00
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Selective GRK5 inhibitors can treat heart failure, breast cancer

Purdue University

Researchers at Purdue University have developed selective small molecule inhibitors of G protein-coupled receptor kinase 5 (GRK5) for preventing heart failure and treating breast cancer. GRK5 is a signaling protein prevalent in the lungs and heart and is an attractive target for disease including heart failure and cancers. Purdue researchers designed a series of selective, irreversible GRK5 inhibitors. Mass spectrometry analysis supports the hypothesis that the best of these compounds interacts with a flexible loop on GRK5 containing a non-conserved cysteine, suggesting high potency and selectivity. This new pharmaceutical development promises to improve patient care by allowing for lower dosing and minimized side effects compared to current treatments of heart related conditions. Further, the new small molecule drug candidates show promise to treat hyperproliferative diseases including breast cancer. A top compound has a nanomolar half maximal inhibitory concentration and over 1000 times selectivity for GRK5 over GRK2.

Advantages:

  • Can Minimize Side Effects and Enables Lower Therapeutic Dosing for Treating Heart Related Conditions and Breast Cancer
  • Highly Potent
  • Highly Selective to GRK5

Potential Applications:

  • Prevention of Heart Failure
  • Treatment of Breast Cancer
  • Pharmaceutical Research and Development

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MIDWEST DRUG DEVELOPMENT CONFERENCE
Bringing together industry and the best university drug development researchers in the Midwest
An Online Event
Oct. 4-5, 2021

Latest News
  • Presentation schedule set for 2021 September 21, 2021
  • MWDD moves to a virtual event in 2021 August 17, 2021
  • Sponsorship, presentation slots nearly full July 29, 2021
  • Registrations are now open for 2021 March 25, 2021
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