A Small Molecule Targeting the Transmembrane Domain of Death Receptor p75

Autor:	Eddy T H, Goh, Zhi, Lin, Bo Young, Ahn, Vanessa, Lopes-Rodrigues, Ngoc Ha, Dang, Shuhailah, Salim, Bryan, Berger, Brian, Dymock, Donna L, Senger, Carlos F, Ibáñez
Rok vydání:	2018
Předmět:	Neurons Cell Death Dose-Response Relationship Drug Molecular Structure Antineoplastic Agents Nerve Tissue Proteins Neoplasms Experimental Receptors Nerve Growth Factor Small Molecule Libraries Mice Structure-Activity Relationship Animals Humans Melanoma Cell Proliferation
Zdroj:	Cell chemical biology. 25(12)
ISSN:	2451-9448
Popis:	Small molecules offer powerful ways to alter protein function. However, most proteins in the human proteome lack small-molecule probes, including the large class of non-catalytic transmembrane receptors, such as death receptors. We hypothesized that small molecules targeting the interfaces between transmembrane domains (TMDs) in receptor complexes may induce conformational changes that alter receptor function. Applying this concept in a screening assay, we identified a compound targeting the TMD of death receptor p75
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::97daacb5ee5ca829dc8a6b6e0940dc2d https://pubmed.ncbi.nlm.nih.gov/30293939 Zobrazit plný text záznamu