c-Kit

Single-cell RNA sequencing identifies an Il1rn+/Trem1+ macrophage subpopulation as a cellular target for mitigating the progression of thoracic aortic aneurysm and dissection

39 views | Dec 08 2023

The study on thoracic aortic aneurysm and dissection (TAAD) utilizing single-cell RNA sequencing in a mouse model identified the Il1rn+/Trem1+ pro-inflammatory macrophage subpopulation as the predominant source of detrimental molecules, highlighting the potential of targeted therapy, specifically via Trem1 blockade, as a promising medical treatment for TAAD. [Read the Full Post]

Identification of potential RapJ hits as sporulation pathway inducer candidates in Bacillus coagulans via structure-based virtual screening and molecular dynamics simulation studies

57 views | Dec 01 2023

Computational analyses identified acarbose as a potential inhibitor of the RapJ enzyme, crucial for inducing the sporulation pathway in Bacillus coagulans, but experimental validation is necessary to confirm its effectiveness. [Read the Full Post]

NR4A1 as a potential therapeutic target in colon adenocarcinoma: a computational analysis of immune infiltration and drug response

19 views | Dec 01 2023

Targeting NR4A1 with OSI-930 may offer a promising therapeutic strategy for colon adenocarcinoma patients with high immune infiltration, pending rigorous clinical validation. [Read the Full Post]

Development of Masitinib Derivatives with Enhanced Mpro Ligand Efficiency and Reduced Cytotoxicity

25 views | Nov 20 2023

Using advanced molecular dynamics simulations, researchers identified masitinib's stable hydrogen bond interactions with the Mpro enzyme, pinpointing the crucial role of His163, leading to the design of effective derivatives M3 and M4 with increased inhibitory efficiency against SARS-CoV-2. [Read the Full Post]

Discovery and pharmacological characterization of AZD3229, a potent KIT/PDGFRα inhibitor for treatment of gastrointestinal stromal tumors

75 views | Aug 26 2023

AZD3229 is a potent and selective small-molecule inhibitor with the potential to be a best-in-class treatment for a broad range of primary and imatinib-resistant secondary mutations in gastrointestinal stromal tumor (GIST). [Read the Full Post]

Ripretinib in advanced gastrointestinal stromal tumors: an overview of current evidence and drug approval

39 views | Aug 24 2023

Ripretinib, a switch-control tyrosine kinase inhibitor, has shown promise in targeting both primary and secondary KIT and PDGFRα resistance mutations, making it a valuable therapeutic option in the management of advanced gastrointestinal stromal tumors (GISTs) that have developed resistance to imatinib and other treatments. [Read the Full Post]

SEOM-GEIS clinical guideline for gastrointestinal stromal tumors (2022)

73 views | Aug 24 2023

The Spanish Society of Medical Oncology (SEOM) and the Spanish Sarcoma Research Group (GEIS) recommend a multidisciplinary approach and centralized management in reference centers for the diagnosis and treatment of gastrointestinal stromal tumor (GIST) patients. [Read the Full Post]

Anti-tumor efficacy of the novel KIT inhibitor IDRX-42 (formerly M4205) in patient- and cell line-derived xenograft models of gastrointestinal stromal tumor (GIST)

28 views | Aug 11 2023

The study found that IDRX-42, a novel selective KIT inhibitor, exhibited significant antitumor activity by inducing tumor volume shrinkage, reducing mitotic activity, and causing characteristic myxoid degeneration in GIST xenograft models with specific KIT mutations. [Read the Full Post]

Current scenario of pyrazole hybrids with in vivo therapeutic potential against cancers

93 views | Aug 01 2023

This review provides a comprehensive overview of the potential of pyrazole hybrids as anticancer agents, summarizing their mechanisms of action, toxicity, and pharmacokinetics, with the aim of facilitating the rational exploitation and development of more effective candidates for cancer therapy. [Read the Full Post]

Successful Treatment and Retreatment With Erdafitinib for a Patient With FGFR3-TACC3 Fusion Squamous NSCLC: A Case Report

119 views | Aug 01 2023

This case report demonstrates the potential efficacy of erdafitinib, an FGFR inhibitor, in achieving disease control and radiographic response in a patient with FGFR3-TACC3 fusion squamous NSCLC, suggesting the need for further investigation and expanding therapeutic options. [Read the Full Post]