ALK4 inhibitors(activin A receptor type 1B inhibitors), ALK5 inhibitors(Transforming growth factor beta receptor 1 inhibitors), ALK7 inhibitors(activin A receptor type 1C inhibitors)

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GSK Plc

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100 Clinical Results associated with SB-505124

100 Translational Medicine associated with SB-505124

100 Patents (Medical) associated with SB-505124

Literatures (Medical) associated with SB-505124

01 Mar 2025·Biochemistry and Biophysics Reports

An integrated machine learning framework for developing and validating a prognostic risk model of gastric cancer based on endoplasmic reticulum stress-associated genes

Article

Author: Liu, Lei ; Wei, Gang ; Liu, Ru ; Wang, Yan

BackgroundGastric cancer (GC), a prevalent and deadly malignancy, demonstrates poor survival outcomes. Evidence has emerged indicating that disruptions in endoplasmic reticulum homeostasis are significantly implicated in the onset and progression of various oncological conditions. This study was designed to construct a prognostic model based on genes related to endoplasmic reticulum stress(ERS) to predict survival outcomes in patients with GC.MethodsExpression profiling data for GC samples were extracted and analyzed from TCGA-STAD, revealing 214 genes related to endoplasmic reticulum stress that show differential expression when compared with normal gastric tissue. Building on these insights, a prognostic model was formulated using data from TCGA-STAD and validated through subsequent analyses of GEO datasets. The tumor immune dysfunction and exclusion(TIDE) algorithm was applied to determine the susceptibility of individuals in high- and low-risk categories to immunotherapy. The presence of immune and stromal cells within the tumor microenvironment was assessed with the aid of the ESTIMATE algorithm. Sensitivity variations to prevalent anticancer drugs between the risk groups were evaluated using the Genomics of Drug Sensitivity in Cancer(GDSC) database, and prospective therapeutic agents were confirmed through molecular docking techniques.ResultsThirty-one endoplasmic reticulum stress (ERS)-related differentially expressed genes (DEGs) crucial for prognosis in GC were pinpointed. These DEGs were then used to construct a prognostic model and were considered as independent prognostic factors for GC patients. This risk model proved to have a good predictive performance for estimating the overall survival of these patients. The patients placed into the high-risk group showed worse results and lower sensitivity to immunotherapy. Moreover, five specific targeted therapy drugs, namely BMS-754807, Dasatinib, JQ1, AZD8055 and SB505124, produced better results in the treatment of the high-risk group of patients.ConclusionsA new molecular prognostic model associated with ERS was established and validated for GC and showed relatively good discriminative and predictive ability. This model greatly expands the collection of weapons in the armoury of prognostic analysis in GC.

01 Nov 2024·Acta Crystallographica Section F Structural Biology Communications

Human transforming growth factor β type I receptor in complex with kinase inhibitor SB505124

Article

Author: Landström, Maréne ; Rodriguez Buitrago, Jhon A ; Wolf-Watz, Magnus

The crystal structure of the intracellular domain of transforming growth factor β type I receptor (TβR1) in complex with the competitive inhibitor SB505124 is presented. The study provides insights into the structure and function of TβR1 in complex with SB505124, and as such offers molecular-level understanding of the inhibition of this critical signalling pathway. The potential of SB505124 as an avenue for therapy in cancer treatment is discussed on basis of the results.

01 Apr 2024·Cell Biochemistry and Function

Adenosine increases PD‐L1 expression in mesenchymal stromal cells derived from cervical cancer through its interaction with A_2AR/A_2BR and the production of TGF‐β1

Article

Author: Torres‐Pineda, Daniela Berenice ; García‐Rocha, Rosario ; Sánchez‐Torres, Luvia Enid ; López‐Santiago, Ruben ; Don‐López, Christian Azucena ; Moreno‐Lafont, Martha C. ; Mora‐García, María de Lourdes ; Marín‐Aquino, Luis Antonio ; Monroy‐García, Alberto ; Weiss‐Steider, Benny ; Hernández‐Montes, Jorge ; Montesinos‐Montesinos, Juan José

AbstractMesenchymal stromal cells (MSCs) together with malignant cells present in the tumor microenvironment (TME), participate in the suppression of the antitumor immune response through the production of immunosuppressive factors, such as transforming growth factor beta 1 (TGF‐β1). In previous studies, we reported that adenosine (Ado), generated by the adenosinergic activity of cervical cancer (CeCa) cells, induces the production of TGF‐β1 by interacting with A2AR/A2BR. In the present study, we provide evidence that Ado induces the production of TGF‐β1 in MSCs derived from CeCa tumors (CeCa‐MSCs) by interacting with both receptors and that TGF‐β1 acts in an autocrine manner to induce the expression of programmed death ligand 1 (PD‐L1) in CeCa‐MSCs, resulting in an increase in their immunosuppressive capacity on activated CD8+ T lymphocytes. The addition of the antagonists ZM241385 and MRS1754, specific for A2AR and A2BR, respectively, or SB‐505124, a selective TGF‐β1 receptor inhibitor, in CeCa‐MSC cultures significantly inhibited the expression of PD‐L1. Compared with CeCa‐MSCs, MSCs derived from normal cervical tissue (NCx‐MSCs), used as a control and induced with Ado to express PD‐L1, showed a lower response to TGF‐β1 to increase PD‐L1 expression. Those results strongly suggest the presence of a feedback mechanism among the adenosinergic pathway, the production of TGF‐β1, and the induction of PD‐L1 in CeCa‐MSCs to suppress the antitumor response of CD8+ T lymphocytes. The findings of this study suggest that this pathway may have clinical importance as a therapeutic target.

100 Deals associated with SB-505124

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