Delving into the Latest Updates on SLF-80721166 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

SPNS2

Action

inhibitors

Mechanism

SPNS2 inhibitors(sphingolipid transporter 2 inhibitors)

Therapeutic Areas

Immune System DiseasesNervous System DiseasesDigestive System Disorders+ [1]

Active Indication

Colitis, UlcerativeMultiple Sclerosis

Inactive Indication-

Originator Organization

Virginia Tech Corporate Research Center, Inc.

Active Organization

Virginia Tech Corporate Research Center, Inc.

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Targeting the S1P pathway has resulted in the development of S1P1 receptor modulators for the treatment of multiple sclerosis and ulcerative colitis. We hypothesize that targeting an upstream node of the S1P pathway may provide an improved adverse event profile. In this report, we performed a structure-activity relationship study focusing on the benzoxazole scaffold in SLB1122168, which lead to the discovery of 11i (SLF80821178) as a potent inhibitor of S1P release from HeLa cells (IC₅₀: 51 ± 3 nM). Administration of SLF80821178 to mice induced ∼50% reduction in circulating lymphocyte counts, recapitulating the lymphopenia characteristic of Spns2 null animals. Molecular modeling studies suggest that SLF80821178 binds Spns2 in its occluded inward-facing state and forms hydrogen bonds with Asn112 and Ser211 and π stacking with Phe234. Taken together, SLF80821178 can serve as a scaffold for future inhibitor development and represents a chemical tool to study the therapeutic implication of inhibiting Spns2.

100 Deals associated with SLF-80721166

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Colitis, Ulcerative	Preclinical	United States	Virginia Tech Corporate Research Center, Inc.	02 Jul 2024
Multiple Sclerosis	Preclinical	United States	Virginia Tech Corporate Research Center, Inc.	02 Jul 2024