Design and Synthesis of Small Molecule Agonists Targeting Type I Interferon and Vitamin D Receptors
Year: 2014
Type: dissertation
Abstract: Small molecule agonists were designed and synthesized for two receptor systems: (i) type I interferon-α/β-receptor (IFNAR), a heterodimeric cell-surface transmembrane receptor; and (ii) the vitamin D receptor (VDR), a nuclear membrane bound receptor. As part of the first project, 18 compounds were designed, carrying specific functionalities, and were synthesized targeting IFNAR. A candidate compound exhibited antiviral activities and induced interferon-inducible genes, implying their agonist-like interactions at the receptor. As part of the second project, synthetic strategies were investigated for the synthesis of three hit compounds as potential agonists of VDR to enable accessibility to target compounds. Three hit molecules belonging to the class of pyrimidines were synthesized. This thesis outlines the functional group modifications for exploring agonist activities using rational approaches.
Source: TSpace (University of Toronto)
Author: Joseph M. Keca
Language: English
Subfield: Immunology
Field: Immunology and Microbiology
Domain: Life Sciences
Open Access status: green
OpenAlex ID: W2617981360