Results 41 to 50 of about 702,558 (291)

Allosteric modulators targeting GPCRs

, 2020
The remarkable precision of the pharmacological modulation, including high degree of specificity, probe dependence, and signaling bias, confers to GPCR allosteric modulators unique advantages over orthosteric classical ligands.
María L. López-Rodríguez, Bellinda Benhamú, López Rodríguez, María Luz, Henar Vázquez-Villa, Benhamú Salama, Bellinda, Vázquez Villa, María Del Henar   +5 more
core   +1 more source

The Shewanella oneidensis Fic enzyme SoFic targets the switch‐I region of EF‐Tu for AMPylation

FEBS Letters, EarlyView.
Fic enzymes mediate diverse post‐translational modifications across all domains of life, including AMPylation. Prokaryotic EF‐Tu can be AMPylated and deAMPylated by the conserved Fic enzyme SoFic. Structural and biochemical approaches were used to characterize the effect of AMPylation on EF‐Tu, SoFic's enzymatic activities, and the enzyme‐target ...
Svenja Runge, Vivian Pogenberg, Alexander Baumgart, Bente Siebels, Hartmut Schlüter, Michael Hecht‐Bucher, Aymelt Itzen   +6 more
wiley   +1 more source

Modulation of the Erwinia ligand-gated ion channel (ELIC) and the 5-HT3 receptor via a common vestibule site

eLife, 2020
Pentameric ligand-gated ion channels (pLGICs) or Cys-loop receptors are involved in fast synaptic signaling in the nervous system. Allosteric modulators bind to sites that are remote from the neurotransmitter binding site, but modify coupling of ligand ...
Marijke Brams, Cedric Govaerts, Kumiko Kambara, Kerry L Price, Radovan Spurny, Anant Gharpure, Els Pardon, Genevieve L Evans, Daniel Bertrand, Sarah CR Lummis, Ryan E Hibbs, Jan Steyaert, Chris Ulens   +12 more
doaj   +1 more source

Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor [PDF]

Proceedings of the National Academy of Sciences, 2013
μ-Opioid receptors are among the most studied G protein-coupled receptors because of the therapeutic value of agonists, such as morphine, that are used to treat chronic pain. However, these drugs have significant side effects, such as respiratory suppression, constipation, allodynia, tolerance, and dependence, as well as abuse potential.
Neil T, Burford, Mary J, Clark, Tom S, Wehrman, Samuel W, Gerritz, Martyn, Banks, Jonathan, O'Connell, John R, Traynor, Andrew, Alt   +7 more
openaire   +2 more sources

p185(BCR/ABL) has a lower sensitivity than p210(BCR/ABL) to the allosteric inhibitor GNF-2 in Philadelphia chromosome-positive acute lymphatic leukemia [PDF]

, 2011
Background: The t(9;22) translocation leads to the formation of the chimeric breakpoint cluster region/c-abl oncogene 1 (BCR/ABL) fusion gene on der22, the Philadelphia chromosome.
Mahajna, Jamal, Y. Najajreh, Ruthardt, Martin, M. Ruthardt, Ottmann, Oliver G., J. Mahajna, Mian, Afsar Ali, Mian, Afsar A., Metodieva, Anna, Najajreh, Yousef, A. Metodieva, A. A. Mian, O. G. Ottmann   +12 more
core   +1 more source

Prospecting the protein design landscape

FEBS Letters, EarlyView.
This review outlines the current state of various protein design approaches. We discuss the current possibilities enabled by recently released tools, highlight future avenues to pursue in protein design, and underscore the crucial role of key databases and resources for successful protein design workflows.
Jakob R. Riccabona, Katharina T. Stonig, Jens Meiler, Clara T. Schoeder, Monica L. Fernández‐Quintero   +4 more
wiley   +1 more source

Molecular mechanism of allosteric modulation of opioid receptors

Signal Transduction and Targeted Therapy
Opioid analgesics provide potent pain relief but are limited by severe adverse effects, tolerance, and interindividual genetic variability in response. Poly-pharmacology and allosteric modulation of opioid receptors offer promising strategies to enhance ...
Heli Wang, Zhuang Miao, Chang Zhao, Hong Fu, Xiaowen Tian, Xinlei Liu, Lei Wang, Yuan Liu, Xingyu Liu, Xihao Yong, Lantian Su, Wei Yan, Lin Cheng, Renjie Chai, Zhenhua Shao, Bowen Ke   +15 more
doaj   +1 more source

Development of allosteric modulators of GPCRs for treatment of CNS disorders

Neurobiology of Disease, 2014
The discovery of allosteric modulators of G protein-coupled receptors (GPCRs) provides a promising new strategy with potential for developing novel treatments for a variety of central nervous system (CNS) disorders.
Hilary Highfield Nickols, P. Jeffrey Conn   +1 more
doaj   +1 more source

Allosteric crosstalk in modular proteins: Function fine-tuning and drug design

Computational and Structural Biotechnology Journal, 2023
Modular proteins are regulatory proteins that carry out more than one function. These proteins upregulate or downregulate a biochemical cascade to establish homeostasis in cells.
Suman Abhishek, Waghela Deeksha, Krishnapura Ranganatha Nethravathi, Mehdi D. Davari, Eerappa Rajakumara   +4 more
doaj   +1 more source

The heterodimeric amino acid transporters (HAT) of the SLC7/SLC3 family: A structure−function relationships and relevance to human pathology

FEBS Letters, EarlyView.
Heterodimeric amino acid transporters consist of SLC7 and SLC3 family proteins arranged in a conserved structural organization. They regulate nutrient transport across cell membranes, supporting essential cellular functions. These transporters also contribute to xenobiotic/drug uptake and distribution.
Mariafrancesca Scalise, Tiziano Mazza, Raffaella Scanga, Lara Console, Michele Galluccio, Cesare Indiveri   +5 more
wiley   +1 more source