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

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

ISIakovos SaridakisUniversity of Vienna MSManuel SchuppUniversity of Vienna HZHaoqi ZhangCentre National de la Recherche Scientifique

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.

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Cite This Study

Saridakis et al. (Thu,) studied this question.

synapsesocial.com/papers/69f1a033edf4b46824806d07 https://doi.org/https://doi.org/10.1039/d5sc09554a

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