• selective
  • describe the Q pocket as subdivided into 3 parts:A saddle formed by the conserved glutamine (Q817 in PDE5A, Q443 in PDE4B and Q369 in PDE4D) and the P clamp (a hydrophopic clamp at the narrow side of the active sites pocket, formed of invariant purine-selective glutamine and a pair of conserved residues). (wikipedia.org)
  • phosphate
  • The ribose 5-phosphate binding site consists of residues Asp220-Thr228, located in the C-terminal domain of one subunit. (wikipedia.org)
  • it is suggested that phosphate and ADP compete for the same regulatory site. (wikipedia.org)
  • However, at high concentrations, phosphate is shown to have an inhibitory effect by competing with the substrate ribose 5-phosphate for binding at the active site. (wikipedia.org)
  • targets
  • I think the SPR assay is really clever and I would expect that many people will now be taking a similar approach to discovering allosteric sites in their targets. (blogspot.com)
  • Because epimerox targets the allosteric site of the bacterial 2-epimerase, low human toxicity is expected since the human 2-epimerase does not have this site. (wikipedia.org)
  • glucose
  • In addition, glucose and purines stabilize the inactive conformation of PYGL, thus inhibiting binding to its active site. (wikipedia.org)
  • mutation
  • By contrast, the D-loop of the consensus site is flexible and the aspartate to alanine mutation and conformational restriction by cross-linking strongly reduces ATP hydrolysis and substrate transport. (uzh.ch)
  • active
  • Conserved amino acids at the active site and the allosteric activity sites are also evident. (carleton.ca)
  • The active site consists of the active dithiol groups from the RNR1 as well as the diferric center and the tyrosyl radical from the RNR2 subunit. (wikipedia.org)
  • Other residues of RNR2, such as aspartate (D273), tryptophan (W48), and tyrosine (Y356) further stabilize the active-site tyrosyl radical thus allowing electron transfer. (wikipedia.org)
  • Electron transfer from RNR2 to RNR1 occurs via tyrosine (Y356 to Y731) and continues on through tyrosine (Y730) to cysteine (C439) in the active site. (wikipedia.org)
  • Site-directed mutations of the RNR primary structure indicate that all residues cited above participate in the long distance transfer of the free radical to the active site. (wikipedia.org)
  • and cysteine (C838 and C841) residues that are used in the regeneration of dithiol groups in the active site. (wikipedia.org)
  • The active site of these enzymes is in a cleft between two domains. (wikipedia.org)
  • The active sites in these dimeric proteins are well separated from each other. (wikipedia.org)
  • This may be accomplished by binding to the active site or the allosteric site. (wikipedia.org)
  • The active site is a deep pocket at the junction of the 3 subdomains and is lined with highly conserved residues between isotypes of PDE. (wikipedia.org)
  • The volume of the active site has been calculated to be between 875 and 927 Å3. (wikipedia.org)
  • The active site of PDE5 has been described as subdivided into 3 main regions based on its crystal structure in complex with sildenafil: M site: contains both a zinc and magnesium ion. (wikipedia.org)
  • Structural
  • There is little information on structural implications at allosteric sites. (blogspot.com)
  • Nucleotide binding at the degenerate site results in structural rearrangements, which are transmitted to the consensus site via two D-loops located at the NBD interface. (uzh.ch)
  • bound
  • Crystallographic analysis of a hydroxylated polychlorinated biphenyl (OH-PCB) bound to the catalytic estrogen binding site of human estrogen sulfotransferase. (thefreedictionary.com)
  • Here, we present the apo structure of the heterodimeric ABC exporter TM287/288 and compare it to the previously solved structure with adenosine 5'-(β,γ-imido)triphosphate (AMP-PNP) bound at the degenerate site. (uzh.ch)
  • Under resting conditions, it is thought that chloride is bound to allosteric sites in prestin. (wikipedia.org)
  • aspartate
  • The D-loop at the degenerate site ties the NBDs together even in the absence of nucleotides and substitution of its aspartate by alanine is well-tolerated. (uzh.ch)
  • effects
  • The models are valid in pharmacology, enzymology, transportology as well as several other fields of biology involving allosteric concentration effects. (biomedsearch.com)
  • competitive
  • To distinguish allosteric binders from competitive binders using SPR spectroscopy we perfused each fragment alone (green triangle) or in combination with the competitive antagonist d-tubocurarine (black circle). (blogspot.com)
  • C) In the case of a competitive binder, the response units for the mixture of fragment + d-tubocurarine is lower than the sum of fragment alone + d-tubocurarine alone because both compounds compete for binding at the same site. (blogspot.com)
  • Results
  • RESULTS: I show here that Hall's model for interactions between an orthoster, an alloster, and a receptive unit is the best choice of model both for simulation and analysis of allosteric concentration-responses at equilibrium or steady-state. (biomedsearch.com)