The Significance of Chirality in Drug Design and Synthesis of Bitopic Ligands as D3 Receptor (D3R) Selective Agonists.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00702
Abstract: Because of the large degree of homology among dopamine D2-like receptors, discovering ligands capable of discriminating between the D2, D3, and D4 receptor subtypes remains a significant challenge. Previous work has exemplified the use of… read more here.
Keywords: chirality drug; significance chirality; d3r; bitopic ligands ... See more keywords
FRET Studies of Quinolone-Based Bitopic Ligands and Their Structural Analogues at the Muscarinic M1 Receptor.
Sign Up to like & getrecommendations! Published in 2017 at "ACS chemical biology"
DOI: 10.1021/acschembio.6b00828
Abstract: Aiming to design partial agonists as well as allosteric modulators for the M1 muscarinic acetylcholine (M1AChR) receptor, two different series of bipharmacophoric ligands and their structural analogues were designed and synthesized. The hybrids were composed… read more here.
Keywords: structural analogues; bitopic ligands; linker; receptor ... See more keywords
The Role of Orthosteric Building Blocks of Bitopic Ligands for Muscarinic M1 Receptors
Sign Up to like & getrecommendations! Published in 2020 at "ACS Omega"
DOI: 10.1021/acsomega.0c04220
Abstract: The muscarinic M1 acetylcholine receptor is an important drug target for the treatment of various neurological disorders. Designing M1 receptor-selective drugs has proven challenging, mainly due to the high conservation of the acetylcholine binding site… read more here.
Keywords: receptor; bitopic ligands; arrestin recruitment;