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Area of Science:

  • Pharmacology
  • Biochemistry
  • Medicinal Chemistry

Background:

  • The atypical chemokine receptor 3 (ACKR3), also known as CXCR7, plays a role in regulating platelet function and thrombus formation.
  • Developing targeted therapeutics for ACKR3 could offer new avenues for treating thrombotic disorders.

Purpose of the Study:

  • To discover and develop novel, first-in-class agonists targeting ACKR3.
  • To investigate the potential of these agonists in modulating platelet activity and their therapeutic implications for thrombosis.

Main Methods:

  • Utilized in silico screening with an ACKR3 homology model to identify initial hits.
  • Conducted extensive structure-activity relationship (SAR) studies through synthesis and testing of chemical derivatives.
  • Assessed agonist potency using β-arrestin recruitment assays and evaluated platelet function via P-selectin expression in degranulation assays.

Main Results:

  • Identified two initial hits, C10 and C11, from in silico screening.
  • Developed novel thiadiazolopyrimidinone-based compounds, 26 (LN5972) and 27 (LN6023), with superagonistic ACKR3 properties (Emax up to 160%).
  • Compounds 26 and 27 demonstrated high potency (EC50 3.4-3.5 μM), selectivity for ACKR3 over CXCR4, metabolic stability, and significantly reduced P-selectin expression (up to 97%) in platelet degranulation assays.

Conclusions:

  • Successfully discovered and developed potent, selective ACKR3 superagonists.
  • These novel compounds exhibit significant potential for inhibiting platelet degranulation.
  • The findings suggest these ACKR3 agonists are promising candidates for the treatment of platelet-mediated thrombosis.