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Usage

Uses

Used in Pharmaceutical Industry:
C₁₁H₈N₂O₂ is used as a ligand for the activation of human collagen prolyl 4-hydroxylase, an enzyme involved in the hydroxylation of proline residues in collagen. This activation is essential for the proper folding and function of collagen, which is a critical structural protein in the human body. The compound's role in collagen modification makes it a valuable asset in the development of therapies targeting connective tissue disorders and other conditions related to collagen dysfunction.
Used in Research Applications:
In the field of scientific research, C₁₁H₈N₂O₂ serves as a valuable tool for studying the mechanisms of collagen prolyl 4-hydroxylase and its role in collagen synthesis. By using this ligand, researchers can gain insights into the enzyme's activity, regulation, and potential as a therapeutic target for various diseases. Additionally, the compound can be employed in the development of novel inhibitors or activators of the enzyme, which may have applications in the treatment of specific medical conditions.

Upstream product

• 66572-56-3 2-bromoisonicotinic acid 
• 1692-25-7 3-pyridylboronic acid 
• 579476-58-7 methyl [2,3'-bipyridine]-4-carboxylate 
• 26156-48-9 methyl 2-bromoisonicotinate 

Relevant academic research and scientific papers

Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors

The epidermal growth factor receptor (EGFR), when carrying an activating mutation like del19 or L858R, acts as an oncogenic driver in a subset of lung tumors. While tumor responses to tyrosine kinase inhibitors (TKIs) are accompanied by marked tumor shrinkage, the response is usually not durable. Most patients relapse within two years of therapy often due to acquisition of an additional mutation in EGFR kinase domain that confers resistance to TKIs. Crucially, oncogenic EGFR harboring both resistance mutations, T790M and C797S, can no longer be inhibited by currently approved EGFR TKIs. Here, we describe the discovery of BI-4020, which is a noncovalent, wild-type EGFR sparing, macrocyclic TKI. BI-4020 potently inhibits the above-described EGFR variants and induces tumor regressions in a cross-resistant EGFRdel19 T790M C797S xenograft model. Key was the identification of a highly selective but moderately potent benzimidazole followed by complete rigidification of the molecule through macrocyclization.

COMBINATION OF MGLUR2 ANTAGONIST AND ACHE INHIBITOR FOR TREATMENT OF ACUTE AND/OR CHRONIC NEUROLOGICAL DISORDERS

The present invention relates to a method of treatment or prevention of acute and/or chronic neurological disorders, to a pharmaceutical composition comprising an inhibitor of acetylcholinesterase (AChE inhibitor) and a metabotropic Glutamate receptor 2 antagonist (mGluR2 antagonist), to the use of an AChE inhibitor and a mGluR2 antagonist in the preparation of a medicament, and. to kits comprising an AChE inhibitor and a mGluR2 antagonist.