Elham Khajehali

Restoring Agonist Function at a Chemogenetically Modified M-1 Muscarinic Acetylcholine Receptor

Elham Khajehali, Sophie Bradley, Emma T van der Westhuizen, Colin Molloy, Celine Valant, Lisa Finlayson, Craig W Lindsley, Patrick M Sexton, Andrew B Tobin, Arthur Christopoulos

Journal article  |  2020  |  ACS CHEMICAL NEUROSCIENCE

Designer receptors exclusively activated by designer drugs (DREADDs) have been successfully employed to activate signaling pathway..

Development of Novel 4-Arylpyridin-2-one and 6-Arylpyrimidin-4-one Positive Allosteric Modulators of the M(1)Muscarinic Acetylcholine Receptor

Manuela Jorg, Elham Khajehali, Emma T van der Westhuizen, KH C. Choy, David M Shackleford, Andrew B Tobin, Patrick M Sexton, Celine Valant, Ben Capuano, Arthur Christopoulos, Peter J Scammells

Journal article  |  2020  |  CHEMMEDCHEM

This study investigated the structure-activity relationships of 4-phenylpyridin-2-one and 6-phenylpyrimidin-4-one M1 muscarinic ac..

Negative allosteric modulators of the human calcium-sensing receptor bind to overlapping and distinct sites within the 7-transmembrane domain

Tracy M Josephs, Andrew N Keller, Elham Khajehali, Aaron DeBono, Christopher J Langmead, Arthur D Conigrave, Capuano Ben, Irina Kufareva, Karen J Gregory, Katie Leach

Journal article  |  2020  |  BRITISH JOURNAL OF PHARMACOLOGY

BACKGROUND AND PURPOSE: Negative allosteric modulators (NAMs) that target the calcium-sensing receptor (CaS receptor) were origina..

The in vitro characterisation of DREADD agonist 21, a novel ligand for muscarinic DREADD receptors

KJ Thompson, E Khajehali, C Molloy, C Valant, SJ Bradley, PM Sexton, A Christopoulos, AB Tobin

Conference Proceedings  |  2019  |  BRITISH JOURNAL OF PHARMACOLOGY

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M-1 mAChR: The Determinants of Allosteric Activity

Manuela Jorg, Emma T van der Westhuizen, Elham Khajehali, Wessel AC Burger, Jonathan M White, Kwok HC Choy, Andrew B Tobin, Patrick M Sexton, Celine Valant, Ben Capuano, Arthur Christopoulos, Peter J Scammells

Journal article  |  2019  |  ACS CHEMICAL NEUROSCIENCE

Targeting allosteric sites of the M1 muscarinic acetylcholine receptor (mAChR) is an enticing approach to overcome the lack of rec..

Dual Action Calcium-Sensing Receptor Modulator Unmasks Novel Mode-Switching Mechanism

Karen J Gregory, Irina Kufareva, Andrew N Keller, Elham Khajehali, Hee-Chang Mun, Mahvash A Goolam, Rebecca S Mason, Ben Capuano, Arthur D Conigrave, Arthur Christopoulos, Katie Leach

Journal article  |  2018  |  ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE

Negative allosteric modulators (NAMs) of the human calcium-sensing receptor (CaSR) have previously failed to show efficacy in huma..

DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo

Karen J Thompson, Elham Khajehali, Sophie J Bradley, Jovana S Navarrete, Xi Ping Huang, Samuel Slocum, Jian Jin, Jing Liu, Yan Xiong, Reid HJ Olsen, Jeffrey F Diberto, Kristen M Boyt, Melanie M Pina, Dipanwita Pati, Colin Molloy, Christoffer Bundgaard, Patrick M Sexton, Thomas L Kash, Michael J Krashes, Arthur Christopoulos, et al.

Journal article  |  2018  |  ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE

Chemogenetic tools such as designer receptors exclusively activated by designer drugs (DREADDs) are routinely used to modulate neu..

Probing the binding site of novel selective positive allosteric modulators at the M-1 muscarinic acetylcholine receptor

Elham Khajehali, Celine Valant, Manuela Jorg, Andrew B Tobin, P Jeffrey Conn, Craig W Lindsley, Patrick M Sexton, Peter J Scammells, Arthur Christopoulos

Journal article  |  2018  |  BIOCHEMICAL PHARMACOLOGY

Subtype-selective allosteric modulation of the M1 muscarinic acetylcholine (ACh) receptor (M1 mAChR) is an attractive approach for..

Assessment of the Molecular Mechanisms of Action of Novel 4-Phenylpyridine-2-One and 6-Phenylpyrimidin-4-One Allosteric Modulators at the M-1 Muscarinic Acetylcholine Receptors

Emma T van der Westhuizen, Arthur Spathis, Elham Khajehali, Manuela Jorg, Shailesh N Mistry, Ben Capuano, Andrew B Tobin, Patrick M Sexton, Peter J Scammells, Celine Valant, Arthur Christopoulos

Journal article  |  2018  |  MOLECULAR PHARMACOLOGY

Positive allosteric modulators (PAMs) that target the M1 muscarinic acetylcholine (ACh) receptor (M1 mAChR) are potential treatmen..

Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M-1 Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles

Juliana CC Dallagnol, Elham Khajehali, Emma T van der Westhuizen, Manuela Jorg, Celine Valant, Alan G Goncalves, Ben Capuano, Arthur Christopoulos, Peter J Scammells

Journal article  |  2018  |  JOURNAL OF MEDICINAL CHEMISTRY

Targeting allosteric sites at M1 muscarinic acetylcholine receptors is a promising strategy for the treatment of Alzheimer's disea..