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Last update 08 May 2025

WNT1

Last update 08 May 2025

Basic Info

Synonyms

INT1, Proto-oncogene Int-1 homolog, Proto-oncogene Wnt-1

+ [2]

Introduction

Ligand for members of the frizzled family of seven transmembrane receptors (Probable). Acts in the canonical Wnt signaling pathway by promoting beta-catenin-dependent transcriptional activation (PubMed:23499309, PubMed:23656646, PubMed:26902720, PubMed:28528193). In some developmental processes, is also a ligand for the coreceptor RYK, thus triggering Wnt signaling (By similarity). Plays an essential role in the development of the embryonic brain and central nervous system (CNS) (By similarity). Has a role in osteoblast function, bone development and bone homeostasis (PubMed:23499309, PubMed:23656646).

Drugs associated with WNT1

Wnt (Transcell Oncologics)

Target

WNT1

Mechanism

WNT1 inhibitors

Active Org.

Transcell Oncologics Private Limited

Originator Org.

Transcell Oncologics Private Limited

Active Indication

Solid tumor

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

CN117778472

Patent Mining

Target

WNT1

Mechanism-

Active Org.

Peking Union Medical College Hospital [+1]

Originator Org.

Peking Union Medical College Hospital [+1]

Active Indication

Rare Diseases

Inactive Indication-

Drug Highest PhaseDiscovery

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Hetero-DS

Target

DKK1 x WNT1

Mechanism

DKK1 inhibitors [+1]

Active Org.-

Originator Org.

Amgen, Inc.

Active Indication-

Inactive Indication

Osteoporosis

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with WNT1

100 Translational Medicine associated with WNT1

0 Patents (Medical) associated with WNT1

2,340

Literatures (Medical) associated with WNT1

01 Dec 2025·Molecular Biology Reports

Wnt1 oversees microglial activation by the Wnt/LRP5/6 receptor signaling pathway during lipopolysaccharide-mediated toxicity

Article

Author: Jinzhi, Gao ; Xuan, Sun ; Qing, Wang ; Zhihui, Rong ; Hao, Xu

AbstractBackgroundThe protective effects of autophagy-mediated microglial inflammatory regulation on diseases of the central nervous system (CNS) has been a recent field of interest. The canonical signaling pathway activated by Wnt1, the Wnt/β-catenin signaling cascade, also plays a crucial protective role in neurodegenerative diseases. However, the relationship between Wnt1/β-catenin signaling and microglial activation remains unclear. Our study focused on understanding the impact and mechanism of Wnt1 on microglial activation.Methods and resultsTo simulate neuroinflammatory conditions in vitro, BV2 cells were exposed to 1 μg/mL lipopolysaccharide. CD86- and CD206-positive cells were identified by flow cytometry and immunofluorescence assays. Inflammatory and anti-inflammatory factors were measured using enzyme-linked immunosorbent assays. Autophagy was analyzed by expression of LC3B puncta, LC3, P62, and beclin1 expression. The inflammatory activation suppressed by rhWnt1 was restricted by DKK1, siRNA-β-catenin and siRNA-LKB1, respectively, with concomitant changes in β-catenin expression and phosphorylation of NFκB-p65, LKB1, and AMPK. Although the anti-inflammatory effect of Wnt1/LKB1 pathway was independent of β-catenin, Wnt1/LKB1 regulated β-catenin. The reduced inflammation caused by rhWnt1 is linked to its enhancement of autophagy, a process blocked by siRNA-LKB1 and 3-MA partially.ConclusionsThe anti-inflammatory effects of Wnt1 on BV2 cells improved autophagy, a mechanism partly dependent on the β-catenin pathway or the phosphorylation of LKB1. Furthermore, the Wnt1/LKB1 pathway was activated independently of β-catenin and participated in regulating its expression. Our research unveils a previously unknown method through which Wnt1 exerts its anti-inflammatory effects, which may have a potential protective role against CNS diseases.

01 Jun 2025·Experimental Neurology

Activating Wnt1/β-Catenin signaling pathway to restore Otx2 expression in the dopaminergic neurons of ventral midbrain

Article

Author: Liu, Hao ; Zhu, Shunyan ; Ye, Tonglin ; Zheng, Canbing ; Cao, AnQi ; He, Yongqian ; Li, Zhao ; He, Shuaiying ; Cen, Qikai ; Gong, Zhuo ; Duan, Jinhai ; Shen, Danyang ; Lin, Xian

Parkinson's disease (PD) is the world's second most prevalent neurodegenerative disease. Currently, aside from levodopa, there are no other effective drugs clinically available to slow its progression. Otx2 plays a critical role in the differentiation of midbrain dopaminergic neurons (mDANs) during midbrain development. However, in adulthood, Otx2 is primarily expressed in the ventral tegmental area (VTA)-ventral part, and mDANs in the dorsal part of the VTA and the substantia nigra pars compacta (SNc) show no Otx2 expression. Research indicates that Otx2 is essential not only for the development of mDANs but also for their protection against the toxicity of MPTP and rotenone. Consequently, Otx2 is a potential clinical target for mDANs protection. Identifying the upstream mechanism that regulates Otx2 expression is crucial to restoring its expression in the SNc and enhancing its levels in the entire ventral midbrain mDANs. In this study, we have demonstrated the safety of Otx2 overexpression in vitro by using adeno-associate virus (AAV) and explored the feasibility of promoting Otx2 expression through the Wnt/β-Catenin signaling pathway using various drugs, a miR-34 mimic, and an inhibitor. Our results showed that Otx2 overexpression via AAV in the SNc is relatively safe, and CHIR99021 can induce Otx2 expression in mouse mDANs, thereby, alleviating PD-liked motor symptoms induced by MPTP. These findings suggest that modulating Otx2 expression through the Wnt/β-Catenin signaling pathway holds a therapeutic approach for Parkinson's disease.

01 Jun 2025·Bioorganic & Medicinal Chemistry Letters

Synthesis, antiproliferative activity, and biological profiling of C-19 trityl and silyl ether andrographolide analogs in colon cancer and breast cancer cells

Article

Author: Zhou, Carina ; Raval, Rushika ; Tao, Alice ; Wang, Emma ; Shu, Emily ; Chui, Aidan ; Thellakal, Samahith ; Joshi, Aditi ; Bhaskara, Aditya ; Xia, Lorelei ; Jayabalan, Aditi ; Li, Sophia ; Ko, Sanghyuk ; Marimuthu, Anushree ; Gu, Tiffany ; Fang, Yilin ; Shah, Samarth ; Njoo, Edward ; Rim, Kaitlyn ; Hong, Seoyeon ; Zhang, Tracy ; Chen, Zhan ; Venkatesan, Srishti ; Kong, Natalie ; Bashkin, Zachary

Andrographolide, a labdane diterpenoid isolated from Andrographis paniculata, putatively functions through covalent inhibition of NF-κB, a transcription factor that modulates tumor survival and metastasis. Previous studies have found that functionalization of the C-19 hydroxyl alters the primary mode of action from inhibition of NF-κB to the modulation of the Wnt1/β-catenin signaling pathway. Here, we synthesized a series of twelve C-19 trityl and silyl ether analogs, including three novel substituted trityl analogs and four novel substituted silyl analogs of andrographolide. MTT assays revealed cell line selectivity between colorectal and breast cancer cells, which is consistent with known mechanisms of β-catenin-driven cell proliferation in colorectal cancer cell lines. Most compounds exhibited cell line specific antiproliferative activity in HCT-116 and HT-29 colorectal cancer cell lines. Specifically, within 24 h, C-19 analogs of andrographolide exhibit far more limited antiproliferative activity in MCF-7 breast cancer cells compared to HCT-116, HT-29, and MDA-MB-231 cells. Through in vitro TNF-α-dependent NF-κB reporter and Wnt1-dependent luciferase reporter assays, we observed that several analogs generally exhibit greater inhibitory activity compared to andrographolide. Fluorescence imaging demonstrated that cells treated with andrographolide and its C-19 analogs retained similar distributions of active β-catenin, but notable differences in antiproliferative potency upon co-delivery with GSK-3β inhibitor CHIR99021 indicate that several lead compounds exhibit attenuated biological activity selectively in HT-29 cells. Collectively, this work indicates that modest structural modifications at C-19 of andrographolide can have profound implications for its biological activity in mechanisms connected to its anticancer activity.

News (Medical) associated with WNT1

15 Apr 2021

·www.globenewswire.com

PlantX Life Inc. (CSE: VEGA) (Frankfurt: WNT1) (OTCQB: PLTXF) Snatching Market Share in Burgeoning Plant-Based Space

NEW YORK, April 15, 2021 (GLOBE NEWSWIRE) -- NetworkNewsAudio – PlantX Life Inc. (CSE: VEGA) (Frankfurt: WNT1) (OTCQB: PLTXF) announces the availability of a broadcast titled, “Plant-Based Foods Here to Stay.” To hear the AudioPressRelease, please visit: The NetworkNewsAudio News Podcast To view the full editorial, please visit: About PlantX Life Inc. As the digital face of the plant-based community, PlantX’s platform is the one-stop shop for everything plant-based. With its fast-growing category verticals, the company offers customers across North America more than 10,000 plant-based products. In addition to offering meal and indoor plant deliveries, the company currently has plans underway to expand its product lines to include cosmetics, clothing and its own water brand — but the business is not limited to an e-commerce platform. The company uses its digital platform to build a community of like-minded consumers and, most importantly, provide education. Its successful enterprise is being built and fortified on partnerships with top nutritionists, chefs and brands. The company eliminates the barriers to entry for anyone interested in living a plant-based lifestyle and thriving in a longer, healthier and happier life. For more information, visit the company’s website at . NOTE TO INVESTORS: The latest news and updates relating to PLTXF are available in the company’s newsroom at . About NetworkNewsWire NetworkNewsWire (NNW) is an information service that provides (1) access to our news aggregation and syndication servers, (2) NetworkNewsBreaks that summarize corporate news and information, (3) enhanced press release services, (4) social media distribution and optimization services, and (5) a full array of corporate communication solutions. As a multifaceted financial news and content distribution company with an extensive team of contributing journalists and writers, NNW is uniquely positioned to best serve private and public companies that desire to reach a wide audience of investors, consumers, journalists and the general public. NNW has an ever-growing distribution network of more than 5,000 key syndication outlets across the country. By cutting through the overload of information in today’s market, NNW brings its clients unparalleled visibility, recognition and brand awareness. NNW is where news, content and information converge. To receive SMS text alerts from NetworkNewsWire, text “STOCKS” to 77948 (U.S. Mobile Phones Only) For more information please visit Please see full terms of use and disclaimers on the NetworkNewsWire website, applicable to all content provided by NNW wherever published or re-published: NetworkNewsWire (NNW) New York, New York 212.418.1217 Office Editor@NetworkNewsWire.com NetworkNewsWire is part of the InvestorBrandNetwork

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WNT1

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