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Last update 23 Jan 2025

RYK

Last update 23 Jan 2025

Basic Info

Synonyms

D3S3195, JTK5, JTK5A

+ [6]

Introduction

May be a coreceptor along with FZD8 of Wnt proteins, such as WNT1, WNT3, WNT3A and WNT5A. Involved in neuron differentiation, axon guidance, corpus callosum establishment and neurite outgrowth. In response to WNT3 stimulation, receptor C-terminal cleavage occurs in its transmembrane region and allows the C-terminal intracellular product to translocate from the cytoplasm to the nucleus where it plays a crucial role in neuronal development.

Drugs associated with RYK

WO2023023600

Patent Mining

Target

RYK

Mechanism-

Active Org.

The Regents of the University of California

Originator Org.

The Regents of the University of California

Active Indication

Neoplasms

Inactive Indication-

Drug Highest PhaseDiscovery

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with RYK

100 Translational Medicine associated with RYK

0 Patents (Medical) associated with RYK

1,851

Literatures (Medical) associated with RYK

01 Dec 2025·Molecular Biology Reports

Antisense oligonucleotides as a targeted therapeutic approach in model of acute myeloid leukemia

Article

Author: Vaňková, Lenka ; Pitule, Pavel ; Bufka, Jiří ; Hošek, Petr ; Moravec, Jiří ; Macečková, Diana

BACKGROUNDThe genetic and epigenetic alterations observed in acute myeloid leukemia (AML) contribute to its heterogeneity, influencing disease progression response to therapy, and patient outcomes. The use of antisense oligonucleotides (ASOs) technology allows for the design of oligonucleotide inhibitors based on gene sequence information alone, enabling precise targeting of key molecular pathways or specific genes implicated in AML.METHODS AND RESULTSMidostaurin, a FLT3 specific inhibitor and ASOs targeting particular genes, exons, or mutations was conducted using AML models. This ASOs treatment was designed to bind to exon 7 of the MBNL1 (muscleblind-like) gene. Another target was the FLT3 gene, focusing on two aspects: (a) FLT3-ITD (internal tandem duplication), to inhibit the expression of this aberrant gene form, and (b) the FLT3 in general. Treated and untreated cells were analyzed using quantitative PCR (qPCR), dot blot, and Raman spectroscopy. This study contrasts midostaurin with ASOs that inhibit FLT3 protein production or its isoforms via mRNA degradation. A trend of increased FLT3 expression was observed in midostaurin-treated cells, while ASO-treated cells showed decreased expression, though these changes were not statistically significant.CONCLUSIONSIn AML, exon 7 of MBNL1 is involved in several cellular processes and in this study, exon 7 of MBNL1 was targeted for method optimization, with the highest block of the exon 7 gene variant observed 48 h post-transfection. Midostaurin, a multitargeted kinase inhibitor, acts against the receptor tyrosine kinase FLT3, a critical molecule in AML pathogenesis. While midostaurin blocks FLT3 signaling pathways, it paradoxically increases FLT3 expression.

01 Feb 2025·Behavioural Brain Research

Modulation of tyrosine receptor imposed by estrogen in memory and cognition in female rats

Article

Author: Goyal, Rohit ; Bajwa, Ishumeet Kaur ; Sharma, Parul

The present study aimed to investigate the potential role of estrogen in modulating the pathogenesis of dementia-type-AD phenotype, possibly by tyrosine kinase. Female Wistar rats were ovariectomized (OVX) and were treated with Diethylstilbesterol (DES), an estrogen analogue (20 μg/kg/day, i.m.), and Imatinib, a tyrosine kinase inhibitor (30 mg/kg/day, orally), for two months. Animals underwent surgical ovariectomy exhibited significant memory deficits in spatial memory assessment as mean dwell time, short-term memory as spontaneous alteration, and novel object recognition after a chronic period of 4 weeks. OVX animals administered with DES produced significant restoration of memory dysfunction in comparison to OVX, as exhibited by Morris water maze (p=0.0003), Y maze (p<0.0001), and NORT. Imatinib prior to DES treatment in OVX animals showed significant decline in memory functions, which confirms the potential involvement of tyrosine receptor kinase activity in improved memory functions offered by estrogen. Levels of estradiol were significantly (p<0.0001) lower in the OVX group compared to normal which was significantly (p<0.0001) restored in the OVX+E group. Biochemical estimations of TBARS, glutathione, and acetylcholinesterase levels in the brain showed a significant increase in oxidative stress among the OVX group. However, a significant restoration of oxidative changes with TBARS (p=0.0496), glutathione (p<0.0001), and acetylcholinesterase activity (p=0.0201) of OVX animals receiving DES was observed in comparison to animals receiving imatinib followed by DES. These implications in the brain signify that estrogen and tyrosine kinase play an important role in the pathogenesis of dementia. In conclusion, estrogen offers neurochemical mediation for cognition and memory possibly via modulation of tyrosine kinase signaling in female subjects.

01 Feb 2025·European Journal of Medicinal Chemistry

Discovery of pyridine-based derivatives as FLT3 inhibitors for the treatment of acute myeloid leukemia

Article

Author: Chen, Qi ; Ouyang, Weiwei ; Zhang, Yu ; Zhang, Ying ; Li, Xiaoxu ; Luo, Bilan ; Sima, Lijie ; Wang, Jianta ; Su, Xiaoming ; Wu, Shengfei ; Zhao, Dongsheng ; Wang, Zhongyuan ; Chen, Beijing ; Liao, Weike ; Li, Aihong ; Tang, Lei

FMS-like tyrosine receptor kinase 3 (FLT3) mutations, the most common genetic alterations found in acute myeloid leukemia (AML) patients, have been pursued as an ideal drug discovery target for the AML therapy. Taking compound 2 as lead, a series of pyridine derivatives bearing 1,2,3-triazole moiety were rationally designed and synthesized. The bioassays confirmed that these derivatives exerted potent antileukemia effects, and compound 12y was found to be the most potent one. 12y displayed double-digital nanomolar inhibitory activities against FLT3-ITD and FLT3-ITD driven human AML MOLM-13 cells as well as high selectivity over FLT3-ITD non-addicted cell lines. In addition, kinase profiling versus over 51 kinases demonstrated that 12y was potent against FLT3-ITD and VEGFR2. Moreover, treatment of MOLM-13 cells with 12y resulted in downregulated phosphorylation levels of FLT3 and STAT5, as well as cell cycle arrest and apoptosis. With the acceptable oral bioavailability of 19.2 % in SD rats, 12y prolonged the survival rate of NSG mice dose-dependently in MOLM-13 inoculated xenograft model without obvious toxicity. Overall, this study might provide a new insight for the development of novel FLT3 inhibitors.

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