The University of North Carolina at Chapel Hill

University of California

Leland Stanford Junior University

University of Illinois

Friedrich-Alexander-Universitat Erlangen-Nürnberg

University of Florida Research Foundation, Incorporated

Duke University

University of Southern California

Memorial Sloan Kettering Cancer Center

University of Kansas

University of Health Sciences & Pharmacy in St. Louis

Bryan Leo Roth

Alan P Kozikowski

Brian K Kobilka

Jian Jin

Aashish Manglik

Brian K Shoichet

Sung Jin Cho

Peter Gmeiner

Daniela Gisela Dengler

John Arthur Allen

Hsien-Sung Huang

Mark John Zylka

Andreas Svennebring

Benjamin David Philpot

Henry Lin

Jeffrey Aube

Gavril W Pasternak

Stephen Frye

Kevin Frankowski

Jay McLaughlin

Susruta Majumdar

Rajendra Uprety

Justin Gregory English

Ryan Strachan

Reid Olsen

Jeffrey Frederick Diberto

Partha Ghosh

Saheem Zaidi

Vsevolod Katritch

Hyeong-min Lee

Yuna Kim

Yong-hui Jiang

Gang Chen

Disclosed herein is a G protein-coupled receptor (GPCR) assay platform comprised of two complementary systems that equate dynamic intermolecular interactions between a receptor and transducer with more complex stimulus-response cascades in living cells. In the disclosed in vitro ADSoRB method, the forced dissociation of transducers like G protein heterotrimers from receptors alters receptor conformations and ligand interactions to simulate pathway activation in a cell. In the disclosed TRUPATH method, measuring the extent of engineered G protein heterotrimer complex dissociation provides single transducer resolution in a cell.

G protein-coupled receptor screening systems

In some aspects, the present disclosure provides compounds of the formula: wherein the variables are as defined herein. In some embodiments, these compounds may be used to reduce the pain of a patient. These compounds may be used in pain relief and show an improved pharmaceutical profile relative to other commonly used opiates and opioid derivatives.

G-protein biased opioid receptor agonist/analgesics with reduced arrestin recruitment

Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.

Mu opioid receptor modulators

The invention provides pharmaceutical compositions and methods of use thereof for treating Prader-Willi syndrome. More specifically, the invention provides pharmaceutical compositions that when administered inhibit the G9a driven methylation of histone H3 lysine 9.

Compositions and methods for the treatment of Prader-Willi syndrome

MU opioid receptor modulators

The present invention provides methods and compositions for inducing expression of Ube3a in a cell by contacting the cell with a topoisomerase inhibitor. Particular embodiments include a method of treating a genomic imprinting disorder, such as Angelman syndrome, in a subject by administering to the subject an effective amount of a topoisomerase inhibitor.

Methods and compositions for unsilencing imprinted genes

The present invention relates to novel functionally selective ligands of dopamine Dreceptors, including agonists, antagonists, and inverse agonists. The invention further relates to the use of these compounds for treating central nervous system disorders related to Dreceptors.

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Highly selective 5-HT(2C) receptor agonists receptors are disclosed. The 5-HT(2C) receptor agonists are used in the treatments of disease and conditions wherein modulation of 5-HT(2C) receptors provides a benefit, such as obesity and psychiatric disorders.

Highly selective 5-HT(2C) receptor agonists that show anti-psychotic effects with antagonist activity at the 5-HT(2B) receptor

A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.

Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxamides, octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods

Growing community of inventors

Durham, NC, United States of America

Bryan Leo Roth