Evidence map›Paper›PMID 42800620›Full record

ArticleBioorganic & medicinal chemistry letters2027

Structure-activity profiling of indazole-based derivatives as spinster homolog 2 (Spns2)-dependent S1P release inhibitors.

Mario Hernandez, Deija J Hawkins, Yugesh Kharel, Tao Huang, Audrey D Prendergast, Anne M Brown, Kevin R Lynch, Webster L Santos

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2027. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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0citing papers in PubMed
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1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

0 citing papers in PubMed.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors.

Mario HernandezDepartment of Chemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA 24061, United States.
Deija J HawkinsDepartment of Chemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA 24061, United States.
Yugesh KharelDepartment of Pharmacology, University of Virginia, Charlottesville, VA 22904, United States.
Tao HuangDepartment of Pharmacology, University of Virginia, Charlottesville, VA 22904, United States.
Audrey D PrendergastDepartment of Biochemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA 24061, United States.
Anne M BrownDepartment of Biochemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA 24061, United States.
Kevin R LynchDepartment of Pharmacology, University of Virginia, Charlottesville, VA 22904, United States.
Webster L SantosDepartment of Chemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA 24061, United States. Electronic address: santosw@vt.edu.

Funding

Blockade of S1P pathway for renal fibrosis therapyR01DK137181 · NIDDK · VIRGINIA POLYTECHNIC INST AND ST UNIV · PI KEVIN R. LYNCH, Webster L Santos · 2024 to 2026
$1.8M
NIDDK NIH HHS R01 DK137181
6 · The paper itself

Abstract

Sphingosine-1-phosphate (S1P) signaling is a bona fide drug target as evidenced by the S1P receptor modulator drug class for treating multiple sclerosis and ulcerative colitis. Despite this clinical success, on-target adverse events have been reported. To circumvent these, we hypothesized that interdicting the S1P transport cascade will have the same physiological benefits without undesired events. This led to the first reported S1P release inhibitor (SRI), SLF1081851, that supported this concept. Subsequent structural improvements led to new generations of SRIs. Herein, we report a structure-activity relationship study of novel indazole compounds inspired by modifications on a previously reported scaffold. Studies revealed compounds 6c (IC

Indexed as

IndazolesLysophospholipidsSphingosineDose-Response Relationship, DrugHumansModels, MolecularMolecular StructureStructure-Activity RelationshipIndazolesLysophospholipidsSphingosinesphingosine 1-phosphateHomologation studyImmune cell traffickingSphingosine-1-phosphateSpns2Transport inhibition

Identifiers

PMID42800620
PMCPMC13660608

What OpenQuestion holds

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.