Last update 01 Nov 2024

STK17B

Last update 01 Nov 2024

Basic Info

Synonyms

DAP kinase-related apoptosis-inducing protein kinase 2, death-associated protein kinase-related 2, DRAK2

+ [4]

Introduction

Phosphorylates myosin light chains (By similarity). Acts as a positive regulator of apoptosis.

Drugs associated with STK17B

SGC-STK17B-1

Target

STK17B

Mechanism

STK17B inhibitors

Active Org.

The University of North Carolina at Chapel Hill

Originator Org.

The University of North Carolina at Chapel Hill

Active Indication-

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

TRD-93

Target

STK17B

Mechanism

STK17B inhibitors

Active Org.

MedPacto, Inc.

Originator Org.

MedPacto, Inc.

Active Indication-

Inactive Indication-

Drug Highest PhaseDiscovery

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with STK17B

100 Translational Medicine associated with STK17B

0 Patents (Medical) associated with STK17B

Literatures (Medical) associated with STK17B

01 Dec 2024·Molecular and Cellular Endocrinology

Identifying prognostic hub genes and key pathways in pediatric adrenocortical tumors through RNA sequencing and Co-expression analysis

Article

Author: Brandalise, Silvia Regina ; Molina, Carlos Augusto Fernandes ; Nagano, Luiz Fernando ; Correa, Carolina Alves Pereira ; Pinto, Emilia Modolo ; Scrideli, Carlos Alberto ; Tone, Luiz Gonzaga ; Baroni, Mirella ; Silva Queiroz, Rosane de Paula ; Santos, Paula ; Veronez, Luciana Chain ; Antonini, Sonir Roberto Rauber ; Borges, Kleiton Silva ; Valera, Elvis Terci ; Yunes, José Andres ; Xavier, Alcides Euzebio Tavares

Pediatric adrenocortical tumors (ACTs), rare conditions with uncertain prognoses, have high incidence in southern and southeastern Brazil. Pediatric ACTs are highly heterogeneous, so establishing prognostic markers for these tumors is challenging. We have conducted transcriptomic analysis on 14 pediatric ACT samples and compared cases with favorable and unfavorable clinical outcomes to identify prognostically significant genes. This comparison showed 1257 differentially expressed genes in favorable and unfavorable cases. Among these genes, 15 out of 60 hub genes were significantly associated with five-year event-free survival (EFS), and 10 had significant diagnostic value for predicting ACT outcomes in an independent microarray dataset of pediatric adrenocortical carcinomas (GSE76019). Overexpression of N4BP2, HSPB6, JUN, APBB1IP, STK17B, CSNK1D, and KDM3A was associated with poorer EFS, whereas lower expression of ISCU, PTPR, PRKAB2, CD48, PRF1, ITGAL, KLK15, and HIST1H3J was associated with worse outcomes. Collectively, these findings underscore the prognostic significance of these hub genes and suggest that they play a potential role in pediatric ACT progression and are useful predictors of clinical outcomes.

18 Oct 2024·Journal of cell science

DRAK2 regulates myosin light chain phosphorylation in T cells.

Article

Author: Harris, Tarsha L ; Pruett-Miller, Shondra M ; Ogden, Stacey K ; Guy, Cliff S ; Wilander, Benjamin A ; Prater, Mollie S ; Mandarano, Alexandra H ; McGargill, Maureen A

Death-associated protein kinase-related apoptosis-inducing kinase-2 (DRAK2 or STK17B) is a serine/threonine kinase expressed in T cells. Drak2-deficient (Drak2-/-) mice respond effectively to tumors and pathogens while displaying resistance to T cell-mediated autoimmune disease. However, the molecular mechanisms by which DRAK2 impacts T cell function remain unclear. Gaining further insight into the function of DRAK2 in T cells will shed light on differentially regulated pathways in autoreactive and pathogen-specific T cells, which is critical for improving autoimmune therapies. Here, we demonstrate that DRAK2 contributes to activation of myosin light chain (MLC) in both murine and human T cells. In the absence of Drak2, the amount of polymerized actin was decreased, suggesting that DRAK2 modulates actomyosin dynamics. We further show that myosin-dependent T cell functions, such as migration, T cell receptor microcluster accumulation, and conjugation to antigen presenting cells are decreased in the absence of Drak2. These findings reveal that DRAK2 plays an important role in regulating MLC activation within T cells.

13 Jun 2024·ACS Medicinal Chemistry Letters

Potent, Selective, and Orally Bioavailable Quinazoline-Based STK17A/B Dual Inhibitors

Article

Author: Shah, Ashish ; Schurer, Stephan C. ; Chaudhry, Sana ; Zhang, Ziming ; Feng, Yangbo ; Castro, Jesus R. ; Afaghani, Jumana ; Taylor, Justin ; Khurshid, Rabia ; Totiger, Tulasigeri M. ; Nicholls, Miah

STK17A is a novel uncharacterized member of the death-associated protein family of serine and threonine kinases.Overexpression of STK17A is observed in many cancers.We identified a lead compound that is based on a quinazoline core.Optimizations of the lead compound led to the discovery of potent and selective STK17A/B inhibitors with drug-like properties and oral bioavailability.Compound 9 had an STK17A inhibitory IC50 of 23 nM.Based on profiling studies against two wild-type kinase panels (375 and 398 kinases, resp.), compound 9 had strong inhibition of both STK17A and STK17B but moderate off-target inhibition only for AAK1, MYLK4, and NEK3/5.In addition, compound 9 had good oral bioavailability, paving the way for in vivo studies against various cancers.

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STK17B

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