G protein

Crinetics’ Once-Daily Oral Paltusotine Achieved the Primary and All Secondary Endpoints in the Phase 3 PATHFNDR-1 Study Evaluating Treatment of Patients with Acromegaly

Retrieved on: 
Sunday, September 10, 2023

The frequency of participants with at least one treatment emergent adverse event (TEAE) was comparable in the paltusotine (PAL) treatment arm vs placebo (PBO) arm (80% vs. 100% respectively).

Key Points: 
  • The frequency of participants with at least one treatment emergent adverse event (TEAE) was comparable in the paltusotine (PAL) treatment arm vs placebo (PBO) arm (80% vs. 100% respectively).
  • The frequency of adverse events considered related to acromegaly was notably lower in paltusotine treated participants compared to placebo treated participants (30% vs. 86% respectively).
  • “We designed paltusotine to be the preferred therapeutic option for people living with acromegaly.
  • The Company is also conducting an open-label Phase 2 study to evaluate paltusotine in patients with carcinoid syndrome and intends to report preliminary results later this year.

PerkinElmer Launches Industry-First GPCR TR-FRET Binding Assay and Beta-Arrestin Kits to Help Advance Therapeutics Discovery

Retrieved on: 
Tuesday, January 26, 2021

PerkinElmer , a global leader committed to innovating for a healthier world, today announced the addition of new assay kits to help further GPCR (G Protein-Coupled Receptor) therapeutic discovery .

Key Points: 
  • PerkinElmer , a global leader committed to innovating for a healthier world, today announced the addition of new assay kits to help further GPCR (G Protein-Coupled Receptor) therapeutic discovery .
  • These assays will help scientists continue to better understand the important role GPCRs play in disease by studying the interaction, expression and potential modulation of intracellular proteins involved in GPCR signaling mechanisms.
  • For more information on the new kits and PerkinElmers extensive line up of GPCR offerings please visit: https://www.perkinelmer.com/category/gpcr-research-reagents and https://horizondiscovery.com/en/screening/screening-libraries .
  • We strategically partner with customers to enable earlier and more accurate insights supported by deep market knowledge and technical expertise.

Gigadocking™ in Orion™ Molecular Design Platform Rapidly Identifies Novel Chemical Entities for GPCR Targets

Retrieved on: 
Thursday, October 15, 2020

SANTA FE, N.M., & SAN DIEGO, Oct. 15, 2020 /PRNewswire/ -- OpenEye Scientific and Beacon Discovery today announced the rapid identification of two novel chemical entities and more than 30 potent hits for known G-Protein Coupled Receptor (GPCR) targets using Gigadocking in OpenEye's Orion molecular design cloud platform.

Key Points: 
  • SANTA FE, N.M., & SAN DIEGO, Oct. 15, 2020 /PRNewswire/ -- OpenEye Scientific and Beacon Discovery today announced the rapid identification of two novel chemical entities and more than 30 potent hits for known G-Protein Coupled Receptor (GPCR) targets using Gigadocking in OpenEye's Orion molecular design cloud platform.
  • "OpenEye's novel technology seamlessly implemented on the Amazon cloud has been a game-changer for our computational approaches to drug discovery," said Sunny Al-Shamma, CEO of Beacon Discovery.
  • "We have leveraged these tools to make significant progress on multiple targets."
  • "We built our cloud platform to help rapidly advance small molecule discovery, and to see Beacon's success is sensational.

Glucagon Receptor Structures Reveal G protein Specificity Mechanism

Retrieved on: 
Thursday, March 19, 2020

This study offers valuable insights into pleiotropic GPCR-G protein coupling and G protein specificity.

Key Points: 
  • This study offers valuable insights into pleiotropic GPCR-G protein coupling and G protein specificity.
  • Although GCGR couples to both G proteins through the common pocket, it does so with different interaction patterns, which account for G protein specificity.
  • Based on the structures of GCGR-G protein complexes, the researchers performed extensive functional studies using techniques such as mutagenesis, G protein activation and cell signaling to investigate the roles of key residues in the receptor-G protein binding interface in Gs and Gi activation.
  • The results show that conformational differences of intracellular loops and residue side chains in the receptor are sufficient to guide G protein selectivity.

Glucagon Receptor Structures Reveal G protein Specificity Mechanism

Retrieved on: 
Thursday, March 19, 2020

This study offers valuable insights into pleiotropic GPCR-G protein coupling and G protein specificity.

Key Points: 
  • This study offers valuable insights into pleiotropic GPCR-G protein coupling and G protein specificity.
  • Although GCGR couples to both G proteins through the common pocket, it does so with different interaction patterns, which account for G protein specificity.
  • Based on the structures of GCGR-G protein complexes, the researchers performed extensive functional studies using techniques such as mutagenesis, G protein activation and cell signaling to investigate the roles of key residues in the receptor-G protein binding interface in Gs and Gi activation.
  • The results show that conformational differences of intracellular loops and residue side chains in the receptor are sufficient to guide G protein selectivity.

Global Outlook on Cancer Therapies 2018-2030: Transcription Factors, GTPases, Phosphatases and GPCRs

Retrieved on: 
Wednesday, July 4, 2018

The "New Frontiers in Cancer Therapies: Focus on Transcription Factors, GTPases, Phosphatases and GPCRs, 2018-2030" report has been added to ResearchAndMarkets.com's offering.

Key Points: 
  • The "New Frontiers in Cancer Therapies: Focus on Transcription Factors, GTPases, Phosphatases and GPCRs, 2018-2030" report has been added to ResearchAndMarkets.com's offering.
  • It features an elaborate discussion on the future potential of this evolving domain, focusing on phosphatases, transcription factors, small GTPases (specifically Ras family) and undruggable G-protein coupled receptors (GPCRs).
  • Of these, pancreatic cancer (23%) is the most common; other popular indications include breast cancer (21%), lung cancer (19%) and colorectal cancer (16%).
  • The focus of the report is on difficult-to-modulate phosphatases, transcription factors, small GTPases (specifically Ras family) and GPCRs.