A methodology for creating mutants of G‐protein coupled receptors stabilized in active state by combining statistical thermodynamics and evolutionary molecular engineering
Sign Up to like & getrecommendations! Published in 2022 at "Protein Science"
DOI: 10.1002/pro.4425
Abstract: We challenged the stabilization of a G‐protein coupled receptor (GPCR) in the active state solely by multiple amino‐acid mutations without the agonist binding. For many GPCRs, the free energy of the active state is higher… read more here.
Keywords: statistical thermodynamics; state; methodology; active state ... See more keywords
Active state structures of G protein-coupled receptors highlight the similarities and differences in the G protein and arrestin coupling interfaces.
Sign Up to like & getrecommendations! Published in 2017 at "Current opinion in structural biology"
DOI: 10.1016/j.sbi.2017.04.010
Abstract: G protein-coupled receptors (GPCRs) regulate cellular signalling through heterotrimeric G proteins and arrestins in response to an array of extracellular stimuli. Structure determination of GPCRs in an active conformation bound to intracellular signalling proteins has… read more here.
Keywords: protein coupled; active state; state structures; coupled receptors ... See more keywords
G-Protein Peptidomimetics Stabilize GPCR Active State Conformations.
Sign Up to like & getrecommendations! Published in 2021 at "Trends in pharmacological sciences"
DOI: 10.1016/j.tips.2021.03.009
Abstract: Technologies stabilizing the active state of G protein-coupled receptors (GPCRs) represent potential breakthroughs for interrogating G protein activation. Camelid nanobodies have been used as a 'one tool, one receptor' paradigm. However, the development of G… read more here.
Keywords: peptidomimetics stabilize; protein peptidomimetics; active state; gpcr active ... See more keywords
Theoretical Investigation of the Structural Characteristics in the Active State of Akt1 Kinase
Sign Up to like & getrecommendations! Published in 2019 at "Journal of chemical information and modeling"
DOI: 10.1021/acs.jcim.8b00506
Abstract: Akt (known as protein kinase B or PKB) is a serine/threonine kinase that regulates multiple biological processes, including cell growth, survival, and differentiation. Akt plays a critical role in the intracellular signaling network through conformational… read more here.
Keywords: state; structural characteristics; kinase; water ... See more keywords
Active State Organization of Spontaneous Behavioral Patterns
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/s41598-017-18276-z
Abstract: We report the development and validation of a principled analytical approach to reveal the manner in which diverse mouse home cage behaviors are organized. We define and automate detection of two mutually-exclusive low-dimensional spatiotemporal units… read more here.
Keywords: active state; organization spontaneous; patterns active; state organization ... See more keywords
Structural determinants of a permeation barrier of the SecYEG translocon in the active state
Sign Up to like & getrecommendations! Published in 2021 at "Physical Chemistry Chemical Physics"
DOI: 10.1039/d1cp02702f
Abstract: The SecYEG translocon is a channel in bacteria, which provides a passage for secretory proteins across as well as integration of membrane proteins into the plasma membrane. The molecular mechanism, by which SecYEG manages protein… read more here.
Keywords: structural determinants; translocon active; active state; secyeg translocon ... See more keywords
The non‐biphenyl‐tetrazole angiotensin AT1 receptor antagonist eprosartan is a unique and robust inverse agonist of the active state of the AT1 receptor
Sign Up to like & getrecommendations! Published in 2018 at "British Journal of Pharmacology"
DOI: 10.1111/bph.14213
Abstract: Conditions such as hypertension and renal allograft rejection are accompanied by chronic, agonist‐independent, signalling by angiotensin II AT1 receptors. The current treatment paradigm for these diseases entails the preferred use of inverse agonist AT1 receptor… read more here.
Keywords: at1 receptor; at1; inverse agonist; active state ... See more keywords
Stability Control of Quadruped Robot Based on Active State Adjustment
Sign Up to like & getrecommendations! Published in 2023 at "Biomimetics"
DOI: 10.3390/biomimetics8010112
Abstract: The quadruped robot has a strong motion performance and broad application prospects in practical applications. However, during the movement of the quadruped robot, it is easy to be affected by external disturbance and environmental changes,… read more here.
Keywords: disturbance; state; movement; state adjustment ... See more keywords