Discovery and Characterization of Two Classes of Selective Inhibitors of the Suppressor of the TCR Signaling Family of Proteins.
PTP
Sts
TULA
UBASH3
tetracycline
Journal
ACS infectious diseases
ISSN: 2373-8227
Titre abrégé: ACS Infect Dis
Pays: United States
ID NLM: 101654580
Informations de publication
Date de publication:
08 02 2019
08 02 2019
Historique:
pubmed:
30
11
2018
medline:
18
12
2019
entrez:
29
11
2018
Statut:
ppublish
Résumé
The suppressor of T-cell receptor signaling (Sts) proteins, Sts-1, has recently emerged as a potential immunostimulatory target for drug development. Genetic inactivation of the Sts proteins dramatically increases host survival of systemic infection and leads to improved pathogen clearance. The protein tyrosine phosphatase (PTP) activity of these proteins arises from a C-terminal 2-histidine phosphatase (HP) domain. To identify new inhibitors of the HP activity of Sts-1, we miniaturized a phosphatase assay to a 1536-well format and conducted a 20 580 compound screen. Among the hits were two classes of structurally related compounds, tetracycline variants and sulfonated azo dyes. These hits had low micromolar to nanomolar IC
Identifiants
pubmed: 30485744
doi: 10.1021/acsinfecdis.8b00238
pmc: PMC6368478
mid: NIHMS1007445
doi:
Substances chimiques
Small Molecule Libraries
0
Protein Tyrosine Phosphatases
EC 3.1.3.48
TULA-2 protein, mouse
EC 3.1.3.48
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, U.S. Gov't, Non-P.H.S.
Langues
eng
Sous-ensembles de citation
IM
Pagination
250-259Subventions
Organisme : NIAID NIH HHS
ID : R21 AI130859
Pays : United States
Organisme : NIGMS NIH HHS
ID : R35 GM124898
Pays : United States
Organisme : NIAID NIH HHS
ID : R01 AI141592
Pays : United States
Organisme : NIH HHS
ID : S10 OD020155
Pays : United States
Organisme : NHLBI NIH HHS
ID : U01 HL127522
Pays : United States
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