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Last update 08 May 2025

STK17B

Last update 08 May 2025

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

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

EP4431508

Patent Mining

Target

STK17B

Mechanism

STK17B inhibitors

Active Org.

Baiji Youtang (Guangdong) Pharmaceutical Technology Co., Ltd.

Originator Org.

Baiji Youtang (Guangdong) Pharmaceutical Technology Co., Ltd.

Active Indication

Autoimmune Diseases [+7]

Inactive Indication-

Drug Highest PhaseDiscovery

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

SGC-STK17B-1

Target

STK17B

Mechanism

STK17B inhibitors

Active Org.-

Originator Org.

The University of North Carolina at Chapel Hill

Active Indication-

Inactive Indication-

Drug Highest PhasePending

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 Apr 2025·Phytochemistry

Bicyclic polyprenylated acylphloroglucinol-related meroterpenoids as potent DRAK2 inhibitors from Hypericum patulum

Article

Author: Huang, Jin-Chang ; Hou, Ai-Jun ; Xu, Hong-Hong ; Li, Jing-Ya ; Jia, Xin-Yu ; Lv, Yi-Fan ; Han, Ming ; Yang, Yang ; Lu, Yu-Ting ; Yang, Hong-Xun ; Yu, Qiang-Qiang

As a both edible and medicinal plant, Hypericum patulum (Hypericaceae) is used as a natural herbal tea, scented tea, and folk medicine. In this study, eight undescribed bicyclic polyprenylated acylphloroglucinol-related meroterpenoids named hyperpatins A-H, along with eight known ones, were isolated from this plant. Their structures were elucidated on the basis of spectroscopic techniques, chemical method, X-ray crystallographic experiments, and electronic circular dichroism analyses. Hyperpatins A-H possess a characteristic pyran ring system diversely fused with the bicyclo[3.3.1]nonane-2,4,9-trione core, and hyperpatins C and D incorporate a unique α,β-unsaturated aldehyde moiety. Some of the isolates exhibited potent inhibitory effects on death-associated protein kinase-related apoptosis-inducing kinase 2 with IC₅₀ values ranging from 2.60 ± 0.29 to 17.93 ± 3.08 μM. This is the first report of DRAK2 inhibitory activity for acylphloroglucinol-related meroterpenoids. The most active molecule hyperpatins C showed binding affinity with DRAK2 by hydrogen-bond and hydrophobic interactions in molecular docking and promoted the glucose-stimulated insulin secretion ability of primary islets.

28 Mar 2025·Journal of Natural Products

Alstolarsines A–E, Indoline Alkaloids with Two Different Carbon Skeletons from Alstonia scholaris

Article

Author: Zhu, Xu-Xin ; Yang, Hong-Ying ; Gao, Kun ; Zheng, Cheng-Yu ; Yue, Jian-Min ; Fan, Yao-Yue

Five complex indoline alkaloids, alstolarsines A-E (1-5) possessing two unprecedented carbon skeletons of 6/5/5/7/6/6(5) fused polycyclic systems, were isolated from Alstonia scholaris. Their structures were characterized using various methods including spectroscopic data, ECD spectra, and single-crystal X-ray diffraction. The inhibitory activities of alstolarsines A-D (1-4) on DRAK2 phosphorylation and ATP-citrate lyase were evaluated, but all of them were inactive.

24 Mar 2025·Journal of Biomolecular Structure and Dynamics

Identification of promising small-molecule inhibitors targeting STK17B for cancer therapeutics: molecular docking and molecular dynamics investigations

Article

Author: Egejuru, Winner Amaka ; Aderemi, Olajide Enoch ; Abdulkareem, Teslim Oluwaseyi ; Akinboade, Modinat Wuraola ; Ibrahim, Ismail Abiola ; Aderemi, Christiana Oluwaseun ; Oluwafemi, Oluwatosin Oluwafunmilola ; Adekola, Adedayo Toluwanimi ; Omotara, Bamidele Samson ; Meejay Kanu, Ihunanya ; Egbemhenghe, Abel Ujaigbe ; Ojeyemi, Toluwalase ; Ddamulira, Christopher ; Ajala, Chinedum Favour ; Afuape, Akinwumi Raphael ; Otuomagie, Osasenaga Israel

Cancer is a complex disease characterized by the uncontrolled growth of abnormal cells, leading to the formation of tumours. STK17B, a member of the DAPK family, has been implicated in various cancers and is considered a potential therapeutic target. However, no drug in the market has been approved for the treatment of STK17 B-associated cancer disease. This research aimed to identify direct inhibitors of STK17B using computational techniques. Ligand-based virtual screening and molecular docking were performed, resulting in the selection of three lead compounds (CID_135698391, CID_135453100, CID_136599608) with superior binding affinities compared to the reference compound dovitinib. While molecular docking simulation revealed specific interactions between the lead compounds and key amino acid residues at the binding pocket of STK17B, molecular dynamics simulations demonstrated that CID_135453100 and CID_136599608 exhibit stable conformations and comparable flexibility to dovitinib. However, CID_135698391 did not perform well using this metric as it displayed poor stability. Overall, small-molecule compounds CID_135453100 and CID_136599608 showed promising binding interactions and stability, suggesting their potential as direct inhibitors of STK17B. These findings could contribute to the exploration of novel therapeutic options targeting STK17B in cancer treatment.

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STK17B

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