What does this research mean for the field?

The synthetic analog fs-FR4 suppresses cytokine production in human peripheral blood mononuclear cells (PBMCs) with 21-fold higher potency than the parent immunosuppressant (−)-FR252921. Novelty: ClaimNovelty.NOVEL_FINDING. Consensus alignment: ConsensusAlignment.NEUTRAL.

What question did this study set out to answer?

This research aims to explore the structure-activity relationship (SAR) of (−)-FR252921 and its analogs in human immune cells.

April 29, 2026Chemical Science0 citationsOpen Access

View Full Paper

Target-agnostic SAR mapping and immunological evaluation of (−)-FR252921 and analogs against primary human immune cells

ISIakovos Saridakis MSManuel Schupp HZHaoqi Zhang

Key Points

This research aims to explore the structure-activity relationship (SAR) of (−)-FR252921 and its analogs in human immune cells.
Designed and synthesized fifteen analogs of (−)-FR252921.
Evaluated immunosuppressive effects on human peripheral blood mononuclear cells (PBMCs).
Determined cytokine production suppression levels.
fs-FR4 demonstrated a 21-fold higher potency in suppressing cytokine production in human PBMCs.

Abstract

Fifteen synthetic analogs of the immunosuppressant (−)-FR252921 were designed to map its SAR, resulting in the discovery of the highly potent fs-FR4. This compound showed 21-fold higher potency in suppressing cytokine production in human PBMCs.

AIに質問

Bookmark

View Full Paper

AIに質問

Bookmark

View Full Paper

Target-agnostic SAR mapping and immunological evaluation of (−)-FR252921 and analogs against primary human immune cells

Key Points

Abstract

Cite This Study