Evasion from programmed cell death (apoptosis) is the main hallmark of cancer and a major cause of resistance to therapy. Many tumors simply ensure survival by over-expressing the cell-protecting (anti-apoptotic) Bcl-2 membrane protein involved in apoptotic regulation. However, the molecular mechanism by which Bcl-2 protein in its mitochondrial outer membrane location protects cells remains elusive due to the absence of structural insight; and current strategies to therapeutically interfere with...
Novel functional insight in protein complex, possible new target for antibiotics - Phys.org
Novel functional insight in protein complex, possible new target for antibiotics - Phys.org
Novel functional insight in protein complex, possible new target for antibiotics Phys.orgResearchers at Utrecht University have gained new insights into the structure and function of a protein complex that maintains the outer membrane of a bacteria.
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01-07-2019 05:49 AM
[NMR paper] Solution NMR Spectroscopy in Target-Based Drug Discovery.
Solution NMR Spectroscopy in Target-Based Drug Discovery.
Related Articles Solution NMR Spectroscopy in Target-Based Drug Discovery.
Molecules. 2017 Aug 23;22(9):
Authors: Li Y, Kang C
Abstract
Solution NMR spectroscopy is a powerful tool to study protein structures and dynamics under physiological conditions. This technique is particularly useful in target-based drug discovery projects as it provides protein-ligand binding information in solution. Accumulated studies have shown that NMR will play more and more important...
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08-25-2017 04:11 AM
[NMR paper] Solution NMR structures of homeodomains from human proteins ALX4, ZHX1, and CASP8AP2 contribute to the structural coverage of the Human Cancer Protein Interaction Network.
Solution NMR structures of homeodomains from human proteins ALX4, ZHX1, and CASP8AP2 contribute to the structural coverage of the Human Cancer Protein Interaction Network.
Related Articles Solution NMR structures of homeodomains from human proteins ALX4, ZHX1, and CASP8AP2 contribute to the structural coverage of the Human Cancer Protein Interaction Network.
J Struct Funct Genomics. 2014 Jun 19;
Authors: Xu X, Pulavarti SV, Eletsky A, Huang YJ, Acton TB, Xiao R, Everett JK, Montelione GT, Szyperski T
Abstract
High-quality...
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06-20-2014 08:14 PM
[NMR paper] High-Quality NMR Structure of Human Anti-Apoptotic Protein Domain Mcl-1(171-327) for Cancer Drug Design.
High-Quality NMR Structure of Human Anti-Apoptotic Protein Domain Mcl-1(171-327) for Cancer Drug Design.
Related Articles High-Quality NMR Structure of Human Anti-Apoptotic Protein Domain Mcl-1(171-327) for Cancer Drug Design.
PLoS One. 2014;9(5):e96521
Authors: Liu G, Poppe L, Aoki K, Yamane H, Lewis J, Szyperski T
Abstract
A high-quality NMR solution structure is presented for protein hMcl-1(171-327) which comprises residues 171-327 of the human anti-apoptotic protein Mcl-1 (hMcl-1). Since this construct contains the three...
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05-03-2014 10:42 PM
[NMR paper] Drug screening strategy for human membrane proteins: from NMR protein backbone structure to in silica- and NMR-screened hits.
Drug screening strategy for human membrane proteins: from NMR protein backbone structure to in silica- and NMR-screened hits.
Related Articles Drug screening strategy for human membrane proteins: from NMR protein backbone structure to in silica- and NMR-screened hits.
Biochem Biophys Res Commun. 2014 Feb 10;
Authors: Lindert S, Maslennikov I, Chiu E, Pierce LC, Andrew McCammon J, Choe S
Abstract
About 8,000 genes encode membrane proteins in the human genome. The information about their druggability will be very useful to facilitate...
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02-15-2014 08:52 PM
Drug screening strategy for human membrane proteins: from NMR protein backbone structure to in silica- and NMR-screened hits
Drug screening strategy for human membrane proteins: from NMR protein backbone structure to in silica- and NMR-screened hits
Publication date: Available online 10 February 2014
Source:Biochemical and Biophysical Research Communications</br>
Author(s): Steffen Lindert , Innokentiy Maslennikov , Ellis Chiu , Levi C Pierce , J. Andrew McCammon , Senyon Choe</br>
About 8,000 genes encode membrane proteins in the human genome. The information about their druggability will be very useful to facilitate drug discovery and development. The main problem, however,...
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02-10-2014 08:46 PM
New Protein Evolution Insight Could Improve Drug Design - Drug Discovery & Development
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New Protein Evolution Insight Could Improve Drug Design
Drug Discovery & Development
The team used a variety of techniques to characterize the two versions of the enzyme, including X-ray crystallography and nuclear magnetic resonance, analyses of DHFR amino-acid sequences and evaluations of the enzyme's functionality in cells and in ...
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New Protein Evolution Insight Could Improve Drug Design - Drug Discovery & Development
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10-01-2013 09:43 AM
[NMR paper] Insights into the interactions between a drug and a membrane protein target by fluori
Insights into the interactions between a drug and a membrane protein target by fluorine cross-polarization magic angle spinning NMR.
Related Articles Insights into the interactions between a drug and a membrane protein target by fluorine cross-polarization magic angle spinning NMR.
Magn Reson Chem. 2004 Feb;42(2):204-11
Authors: Boland MP, Middleton DA
The fluorinated anti-psychotic drug trifluoperazine (TFP) has been shown to be a K(+)-competitive inhibitor of gastric H(+)/K(+)-ATPase, a membrane-embedded therapeutic target for peptic ulcer...