Journal ArticleDOI
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions
David Buttar,Nicola Colclough,Stefan Gerhardt,Philip A. MacFaul,Scott D. Phillips,Alleyn T. Plowright,Paul Robert Owen Whittamore,Kin Yip Tam,Klaus Maskos,Stefan Steinbacher,Holger Steuber +10 more
TLDR
The crystallography results support the findings from the fluorescence displacement assay and indicate that drug binding to subdomain IB might also be important location for certain compounds.About:
This article is published in Bioorganic & Medicinal Chemistry.The article was published on 2010-11-01. It has received 83 citations till now. The article focuses on the topics: Human serum albumin & Fluorescence spectrometry.read more
Citations
More filters
Journal ArticleDOI
Human serum albumin: from bench to bedside.
TL;DR: HSA is a valuable biomarker of many diseases, including cancer, rheumatoid arthritis, ischemia, post-menopausal obesity, severe acute graft-versus-host disease, and diseases that need monitoring of the glycemic control.
Journal ArticleDOI
Subdomain IB is the third major drug binding region of human serum albumin: toward the three-sites model.
TL;DR: It is shown that biliverdin is the specific CD label of an additional drug binding area in subdomain IB, which implies that sub domain IB can be considered as the third major drug binding region of HSA featured with promiscuous ligand recognition ability.
Journal ArticleDOI
Interactive Association of Drugs Binding to Human Serum Albumin
Feng Yang,Yao Zhang,Hong Liang +2 more
TL;DR: This review will succinctly outline the properties of binding site of drugs in IIA subdomain within the structure of HSA to give an overview on the binding characterization of interactive association of drugs to human serum albumin that may potentially lead to significant clinical applications.
Journal ArticleDOI
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014
Kurt Gordon Pike,Karine Malagu,Marc Geoffrey Hummersone,Keith Allan Menear,Heather Mary Ellen Duggan,Sylvie Gomez,Niall M. B. Martin,Linette Ruston,Sarah L. Pass,Martin Pass +9 more
TL;DR: The optimization of a potent and highly selective series of dual m TORC1 and mTORC2 inhibitors is described, particularly aimed at reducing the rate of metabolism in human hepatocyte incubations, resulted in the discovery of the clinical candidate AZD2014.
Journal ArticleDOI
The role of albumin receptors in regulation of albumin homeostasis: Implications for drug delivery
Malin C. Bern,Kine Marita Knudsen Sand,Kine Marita Knudsen Sand,Jeannette Nilsen,Inger Sandlie,Inger Sandlie,Jan Terje Andersen +6 more
TL;DR: The current understanding of albumin homeostasis is reviewed with a particular focus on the impact of the cellular receptors, namely the neonatal Fc receptor (FcRn) and the cubilin-megalin complex, and their importance on uses ofalbumin in drug delivery is discussed.
References
More filters
Journal ArticleDOI
Coot: model-building tools for molecular graphics.
Paul Emsley,Kevin Cowtan +1 more
TL;DR: CCP4mg is a project that aims to provide a general-purpose tool for structural biologists, providing tools for X-ray structure solution, structure comparison and analysis, and publication-quality graphics.
Journal ArticleDOI
PROCHECK: a program to check the stereochemical quality of protein structures
TL;DR: The PROCHECK suite of programs as mentioned in this paper provides a detailed check on the stereochemistry of a protein structure and provides an assessment of the overall quality of the structure as compared with well refined structures of the same resolution.
Journal ArticleDOI
Refinement of macromolecular structures by the maximum-likelihood method.
TL;DR: The likelihood function for macromolecular structures is extended to include prior phase information and experimental standard uncertainties and the results derived are consistently better than those obtained from least-squares refinement.
Journal ArticleDOI
Atomic structure and chemistry of human serum albumin.
Xiao Min He,Daniel C. Carter +1 more
TL;DR: The three-dimensional structure of human serum albumin has been determined crystallographically to a resolution of 2.8 Å and should provide insight into future pharmacokinetic and genetically engineered therapeutic applications of serumalbumin.
Journal ArticleDOI
Use of TLS parameters to model anisotropic displacements in macromolecular refinement
TL;DR: The implementation of the TLS parameterization in the macromolecular refinement program REFMAC is described, which gives improved refinement statistics and in particular an improvement in R and free R values of several percent.