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Allosteric Modulator ORG27569 Induces CB1 Cannabinoid Receptor High Affinity Agonist Binding State, Receptor Internalization, and Gi Protein-independent ERK1/2 Kinase Activation*
Background: ORG27569 is an allosteric modulator of CB1. Results: Although ORG27569 inhibits G protein coupling, it induces CB1 high affinity agonist binding, receptor internalization, and downstreamExpand
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Distinct Roles of β-Arrestin 1 and β-Arrestin 2 in ORG27569-induced Biased Signaling and Internalization of the Cannabinoid Receptor 1 (CB1)*
Background: CB1 is activated by agonist CP55940 in a G protein-dependent manner. Results: β-Arrestin 2 plays a role in CB1 internalization, whereas β-arrestin 1 is critical for ORG27569-inducedExpand
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Valproic acid potentiates curcumin-mediated neuroprotection in lipopolysaccharide induced rats
The etiology of neuroinflammation is complex and comprises multifactorial, involving both genetic and environmental factors during which diverse genetic and epigenetic modulations are implicated.Expand
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Structure-activity relationship study of indole-2-carboxamides identifies a potent allosteric modulator for the cannabinoid receptor 1 (CB1).
The cannabinoid CB1 receptor is involved in complex physiological functions. The discovery of CB1 allosteric modulators generates new opportunities for drug discovery targeting the pharmacologicallyExpand
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Profiling two indole‐2‐carboxamides for allosteric modulation of the CB1 receptor
Allosteric modulation of G‐protein coupled receptors (GPCRs) represents a novel approach for fine‐tuning GPCR functions. The cannabinoid CB1 receptor, a GPCR associated with the CNS, has beenExpand
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The nature of the DNA substrate influences pre-catalytic conformational changes of DNA polymerase β
DNA polymerase β (Pol β) is essential for maintaining genomic integrity. During short-patch base excision repair (BER), Pol β incorporates a nucleotide into a single-gapped DNA substrate. Pol β mayExpand
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I260Q DNA polymerase β highlights precatalytic conformational rearrangements critical for fidelity
Abstract DNA polymerase β (pol β) fills single nucleotide gaps in DNA during base excision repair and non-homologous end-joining. Pol β must select the correct nucleotide from among a pool of fourExpand
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(4-(Bis(4-Fluorophenyl)Methyl)Piperazin-1-yl)(Cyclohexyl)Methanone Hydrochloride (LDK1229): A New Cannabinoid CB1 Receptor Inverse Agonist from the Class of Benzhydryl Piperazine Analogs
Some inverse agonists of cannabinoid receptor type 1 (CB1) have been demonstrated to be anorectic antiobesity drug candidates. However, the first generation of CB1 inverse agonists, represented byExpand
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Chromatin-Bound PARP1 Correlates with Upregulation of Inflammatory Genes in Response to Long-Term Treatment with Veliparib
Poly-ADP-ribose polymerase (PARP) inhibitors are active against cells and tumors with defects in homology-directed repair as a result of synthetic lethality. PARP inhibitors have been suggested toExpand