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2 198 (0,064s)

Výsledek výzkumu

Interactions between allosteric modulators and 4-DAMP and other antagonists at muscarinic receptors: potential significance of the distance between the N and Carboxyl C atoms in the molecules

of the allosteric binding domain(s) and the features of agonists, antagonists and modulatorsAllosteric enhancement of the affinity of muscarinic receptors clarification. We tested interactions between allosteric m...

ED - Fyziologie

  • 2001
  • Jx
Výsledek výzkumu

Identification of the molecular determinants of antagonist potency in the allosteric binding pocket of human P2X4

of vascular tone. A number of potent small-molecule P2X4 receptor antagonists have been developed, including the allosteric P2X4 receptor antagonist BX430, which that antagonists with high potency (IC50 ≤ 100 nM) ...

Computer sciences, information science, bioinformathics (hardware development to be 2.2, social aspect to be 5.8)

  • 2023
  • JSC
  • Odkaz
Výsledek výzkumu

Allosteric Antagonism of the Pregnane X Receptor (PXR): Current-State-of-the-Art and Prediction of Novel Allosteric Sites

, metabolic syndrome, and inflammatory bowel disease, and PXR antagonists have recently antagonists that can be used in a clinical setting. Nevertheless, due to the large antagonists at the orthosteric site. Alternative lig...

Pharmacology and pharmacy

  • 2022
  • Jimp
  • Odkaz
Výsledek výzkumu

Effects of an agonist, allosteric modulator, and antagonist on guanosine-gamma-(35S)thiotriphosphate binding to liposomes with varying muscarinic receptor/Go protein stoichiometry.

Annotation not available...

ED - Fyziologie

  • 1998
  • Jx
Výsledek výzkumu

Synthesis of novel and functionally selective non‐competitive muscarinic antagonists as chemical probes

Muscarinic receptors are known to play important biological roles and are drug targets for several human diseases. In a pilot study, novel muscarinic antagonists and allosteric models of drug-receptor interactions together with chem...

Physiology (including cytology)

  • 2018
  • Jimp
  • Odkaz
Výsledek výzkumu

Binding of N-methylscopolamine to the extracellular domain of muscarinic acetylcholine receptors

receptors. The orthosteric antagonists quinuclidinyl benzilate (QNB) and N of muscarinic acetylcholine receptors, suggesting allosteric binding. The affinity of NMS at the allosteric site is in the micromolar range for all...

Physiology (including cytology)

  • 2017
  • Jimp
  • Odkaz
Výsledek výzkumu

Monoterpenoid aryl hydrocarbon receptor allosteric antagonists protect against ultraviolet skin damage in female mice

. Allosteric inhibition of AhR was previously thought to be untenable. Here, we identify carvones as noncompetitive, insurmountable antagonists of AhR and characterize radiolabeled ligands from binding to AhR but instead bind al...

Other natural sciences

  • 2023
  • Jimp
  • Odkaz
Výsledek výzkumu

Allosteric modulation of muscarinic receptors: model building and proof of internal consistency

For the purposes of the work, common allosteric ligands were grouped to two gradually more even the association rate for the competitive antagonist N-methyl, this intuitive reaction scheme was proposed for the description of all...

CF - Fyzikální chemie a teoretická chemie

  • 2006
  • Jx
Výsledek výzkumu

Changes of cooperativity between N-methylscopolamine and allosteric modulators alcuronium and gallamine induced by mutations of external loops of muscarinic M(3) receptors.

To clarify the involvement of specific domains of muscarinic receptors in the action of allosteric modulators, muscarinic M3 receptors (on which allosteric (on whichallosteric interactions are strong) and expressed in COS-7 cells. A...

FH - Neurologie, neurochirurgie, neurovědy

  • 2001
  • Jx
Výsledek výzkumu

Multitargeting nature of muscarinic orthosteric agonists and antagonists

subtypes do not sufficiently differ in affinity to orthosteric antagonists or agonists ligands and they do not use allosteric ligands. Moreover, they usually rely strategy is the use of allosteric ligands, although some of...

Physiology (including cytology)

  • 2022
  • Jimp
  • Odkaz
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