... HGF/MET signaling is a driver of many cancers and contributes to drug resistance to several approved therapeutics targeting other RTKs, making MET itself an important drug target. In RTKs, homeostatic receptor signaling is dependent on autoinhibition in the absence of ligand binding and orchestrated...

... and validity of these approaches. This work is only the beginning of efforts to utilize these insights for the development of drugs targeting the orthosteric ligand-binding site of members of this important family. G-Protein-Coupled Receptors: from Structural Insights to Functional Mechanisms...

...Mikael Akke Protein conformational dynamics can be critical for ligand binding in two ways that relate to kinetics and thermodynamics respectively. First, conformational transitions between different substates can control access to the binding site (kinetics). Secondly, differences between free...

... ligand binding riboswitch signalling Other binding pocket nucleotides, specifically those in the J1/2 segment, are tolerant of mutation except in cases in which the sequence becomes complementary to other regions in the RNA and promotes misfolding of the riboswitch. The clearest example...

... Society 2007 G-protein-coupled receptor (GPCR) ligand binding mutagenesis photoaffinity labelling receptor activation secretin receptor Fluorescence techniques can provide complementary insights into the environment of indicators that can be situated at distinct sites throughout...

...D.R. Poyner; M. Wheatley In April 2007, the Biochemical Society held a meeting to compare and contrast ligand binding and activation of Family A and B GPCRs (G-protein-coupled receptors). Being the largest class, Family A GPCRs usually receive the most attention, although a previous Biochemical...

... intramolecular contacts between the propeller domain and the central LA repeats of the ligand-binding domain, suggesting that the receptor changes its overall shape from extended to closed, in response to pH. Here we discuss how the LDLR uses flexibility and rigidity of linkers between modules to facilitate...

... the introduction of frontal gel filtration for the study of protein self-association to the characterization of ligand binding by the biosensor variant of quantitative affinity chromatography. 1 e-mail [email protected] Intermolecular Associations in 2D and 3D, a Biochemical Society Focused...

... be addressed (e-mail [email protected] ). Intermolecular Associations in 2D and 3D, a Biochemical Society Focused Meeting held at University of Nottingham, 19–20 June 2003 18 May 2003 © 2003 Biochemical Society 2003 electron density ligand binding multiple isomorphous replacement...

...E.H. Kong; A.C.W. Pike; R.E. Hubbard We have determined the structures of the oestrogen receptor ligand-binding domain in complex with a range of ligands and with fragments of co-regulator proteins. These structures provide insights into the structural mechanisms underlying the receptor's complex...

...A. C. W. Pike; A. M. Brzozowski; J. Walton; R. E. Hubbard; T. Bonn; J-Å. Gustafsson; M. Carlquist We have determined the three-dimensional structures of both α- and β-forms of the ligand-binding domain of the oestrogen receptor (ER) in complexes with a range of receptor agonists and antagonists...