Allosteric modulation of class A GPCRs: targets, agents, and emerging concepts

EA Wold, J Chen, KA Cunningham… - Journal of medicinal …, 2018 - ACS Publications
G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with
over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR …

What can crystal structures of aminergic receptors tell us about designing subtype-selective ligands?

M Michino, T Beuming, P Donthamsetti… - Pharmacological …, 2015 - ASPET
G protein–coupled receptors (GPCRs) are integral membrane proteins that represent an
important class of drug targets. In particular, aminergic GPCRs interact with a significant …

Allosteric Modulators of Dopamine D2 Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects …

AA Kaczor, TM Wróbel, D Bartuzi - Molecules, 2022 - mdpi.com
Allosteric modulation of G protein-coupled receptors (GPCRs) is nowadays a hot topic in
medicinal chemistry. Allosteric modulators, ie, compounds which bind in a receptor site …

Allosteric modulator leads hiding in plain site: Developing peptide and peptidomimetics as GPCR allosteric modulators

KM Olson, JR Traynor, A Alt - Frontiers in Chemistry, 2021 - frontiersin.org
Allosteric modulators (AMs) of G-protein coupled receptors (GPCRs) are desirable drug
targets because they can produce fewer on-target side effects, improved selectivity, and …

Contiguous O-Galactosylation of 4(R)-Hydroxy-l-proline Residues Forms Very Stable Polyproline II Helices

NW Owens, J Stetefeld, E Lattová… - Journal of the American …, 2010 - ACS Publications
The hydroxyproline-rich glycoproteins (HRGPs) are the major structural proteins of the
extracellular matrix of algae and land plants. They are characterized by a rigid polyproline …

Non-natural 3-Arylmorpholino-β-amino Acid as a PPII Helix Inducer

F Vaghi, R Bucci, F Clerici, A Contini, ML Gelmi - Organic Letters, 2020 - ACS Publications
A new non-natural β-amino acid, named 3-Ar-β-Morph, was designed and synthesized via a
regio-and diastereoselective Pd-catalyzed C (sp3) H-arylation of the corresponding 2 S, 6 S …

Dopamine D3 Agonists in the Treatment of Parkinson&aposs Disease

B Das, G Modi, A Dutta - Current Topics in Medicinal Chemistry, 2015 - ingentaconnect.com
Parkinson&aposs disease (PD) is t he second most common form of neurodegenerative
disorders that results from the progressive loss of dopaminergic neurons in the midbrain …

Spiro-lactam nmda receptor modulators and uses thereof

JA Lowe III, MA Khan - US Patent 9,828,384, 2017 - Google Patents
Disclosed are compounds having enhanced potency in the modulation of NMD A receptor
activity. Such compounds are contemplated for use in the treatment of conditions such as …

Spiro-lactam NMDA receptor modulators and uses thereof

JA Lowe III, MA Khan - US Patent 9,758,525, 2017 - Google Patents
7, 273, 889 B2 9/2007 Mermelstein et al. 7, 884, 080 B2 2/2011 Aslanian et al. 8, 492, 340
B2 7/2013 Moskal 2002/0103335 A1 8/2002 Oldham et al. 2003/0022253 A1 1/2003 Moskal …

Spiro-lactam NMDA receptor modulators and uses thereof

JA Lowe III, MA Khan - US Patent 9,708,335, 2017 - Google Patents
Disclosed are compounds having enhanced potency in the modulation of NMDA receptor
activity. Such compounds are contemplated for use in the treatment of conditions such as …