Striatal-enriched protein tyrosine phosphatase (STEP) is a brain-specific enzyme that regulates the signaling molecules that control synaptic plasticity and neuronal function. Dysregulation of STEP is linked to the pathophysiology of Alzheimer's disease and other neuropsychiatric disorders. Experimental results from neurological deficit disease models suggest that the modulation of STEP could be beneficial in a number of these disorders. This prompted our work to identify small-molecule modulators of STEP to provide the foundation of a drug discovery program. As a component of our testing funnel to identify small-molecule STEP inhibitors, we have developed a cellular target engagement assay that can identify compounds that interact with STEP. We provide a comprehensive protocol to enable the use of this miniaturized assay, and we demonstrate its utility to benchmark the binding of newly discovered compounds.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10956569 | PMC |
| http://dx.doi.org/10.1007/978-1-0716-3397-7_12 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Mir-615-5p inhibits cervical cancer progression by targeting TMIGD2.
Hereditas
January 2025
Obstetrics and Gynecology Medical Centre, The First Affiliated Hospital of Hunan University of Traditional Chinese Medicine, No.105, Shaoshan Middle Road, Yuhua District, Changsha, 410007, Hunan, China.
Background: Cervical cancer (CC) is a prevalent gynecological malignancy, contributing to a substantial number of fatalities among women. MicroRNAs (miRNAs) have emerged as promising biomarkers with significant potential for the early detection and prognosis of CC.
Objective: This study aimed to explore the clinical significance and biological role of miR-615-5p in CC, with the goal of identifying novel biomarkers for this disease.
Secreted LGALS3BP facilitates distant metastasis of breast cancer.
Breast Cancer Res
January 2025
College of Pharmacy, Seoul National University, Seoul, 08826, South Korea.
Background: Patients with estrogen receptor (ER)-positive breast cancer (BC) can be treated with endocrine therapy targeting ER, however, metastatic recurrence occurs in 25% of the patients who have initially been treated. Secreted proteins from tumors play important roles in cancer metastasis but previous methods for isolating secretory proteins had limitations in identifying novel targets.
Methods: We applied an in situ secretory protein labeling technique using TurboID to analyze secretome from tamoxifen-resistant (TAMR) BC.
Interplay of swine acute diarrhoea syndrome coronavirus and the host intrinsic and innate immunity.
Vet Res
January 2025
Department of Preventive Veterinary Medicine, Research Center for Swine Diseases, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, China.
Swine acute diarrhoea syndrome coronavirus (SADS-CoV), a novel HKU2-related coronavirus of bat origin, is a newly emerged swine enteropathogenic coronavirus that causes severe diarrhoea in piglets. SADS-CoV has a broad cell tropism with the capability to infect a wide variety of cells from human and diverse animals, which implicates its ability to hold high risks of cross-species transmission. The intracellular antiviral immunity, comprised of the intrinsic and innate immunity, represents the first line of host defence against viral infection prior to the onset of adaptive immunity.
View Article and Find Full Text PDFmiR-9-5p/HMMR regulates the tumorigenesis and progression of clear cell renal cell carcinoma through EMT and JAK1/STAT1 signaling pathway.
J Transl Med
January 2025
Department of Urology, The First Affiliated Hospital, Zhejiang University School of Medicine, Qingchun Road 79, Hangzhou, Zhejiang, 310003, China.
Background: The most common malignant type of kidney cancer is clear cell renal cell carcinoma (ccRCC). The expression levels of hyaluronan-mediated motility receptor (HMMR) in many tumor types are significantly elevated. HMMR is closely associated with tumor-related progression, treatment resistance, and poor prognosis, and has yet to be fully investigated in terms of its expression patterns and molecular mechanisms of action in ccRCC.
View Article and Find Full Text PDFOSBPL3 modulates the immunosuppressive microenvironment and predicts therapeutic outcomes in pancreatic cancer.
Biol Direct
January 2025
School of Medicine, South China University of Technology, Guangzhou, 510006, China.
Background: Pancreatic cancer is characterized by a complex tumor microenvironment that hinders effective immunotherapy. Identifying key factors that regulate the immunosuppressive landscape is crucial for improving treatment strategies.
Methods: We constructed a prognostic and risk assessment model for pancreatic cancer using 101 machine learning algorithms, identifying OSBPL3 as a key gene associated with disease progression and prognosis.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!