Structure-Activity Relationship
Research News and Information

Saturday, November 21, 2009

Role of E166 in the imine to enamine tautomerization of the clinical beta-lactamase inhibitor sulbactam.

Nov 2009 Mechanism-based inhibitors of class A beta-lactamases, such as sulbactam, undergo a complex series of chemical reactions in the enzyme active site. Formation of a trans-enamine acyl-enzyme via a hydrolysis-prone imine is responsible for transient ... Read more...

Engineering monomeric streptavidin and its ligands with infinite affinity in binding but reversibility in interaction.

30 Oct 2009 Natural tetrameric streptavidin captures and immobilizes biotinylated molecules with ultra-tight binding (K(d) approximately 10(-13) to 10(-14) M). In contrast, engineered monomeric streptavidin offers reversible binding (K(d) approximately 10(-7) ... Read more...

Modular coenzyme specificity: a domain-swopped chimera of glutamate dehydrogenase.

30 Oct 2009 Domain-swopped chimeras of the glutamate dehydrogenases from Clostridium symbiosum (CsGDH) (NAD(+)-specific) and Escherichia coli (EcGDH) (NADP(+)-specific) have been produced, with the aim of testing the localization of determinants of coenzyme ... Read more...

Latest indexed articles for 'Structure-Activity Relationship'

These are the very latest articles for this heading:

• Role of E166 in the imine to enamine tautomerization of the clinical beta-lactamase inhibitor sulbactam. Nov 2009
• Engineering monomeric streptavidin and its ligands with infinite affinity in binding but reversibility in interaction. 30 Oct 2009
• Modular coenzyme specificity: a domain-swopped chimera of glutamate dehydrogenase. 30 Oct 2009
• Hsp90 charged-linker truncation reverses the functional consequences of weakened hydrophobic contacts in the N domain. 16 Oct 2009
• Crystal structures of penicillin-binding protein 6 from Escherichia coli. 12 Oct 2009
• Effect of GC base pairs on charge transfer through DNA hairpins: the importance of electrostatic interactions. 12 Oct 2009
• The crystal structure of caspase-6, a selective effector of axonal degeneration. 10 Oct 2009
• Hydroxamic acids as a novel family of serine racemase inhibitors: mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor. 6 Oct 2009
• Development and screening of water-soluble analogues of progesterone and allopregnanolone in models of brain injury. 6 Oct 2009
• Modeling, synthesis and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene). 6 Oct 2009
• Synthesis of 1,1-[1-naphthyloxy-2-thiophenyl]-2-methylaminomethylcyclopropanes and their evaluation as inhibitors of serotonin, norepinephrine, and dopamine transporters. 6 Oct 2009
• Discovery of novel protease activated receptors 1 antagonists with potent antithrombotic activity in vivo. 6 Oct 2009
• Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. 6 Oct 2009
• Function-oriented biosynthesis of beta-lactone proteasome inhibitors in Salinispora tropica. 6 Oct 2009
• Discovery of new inhibitors of resistant Streptococcus pneumoniae penicillin binding protein (PBP) 2x by structure-based virtual screening. 6 Oct 2009
• Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain. 6 Oct 2009
• Structure-activity relationships for substrate-based inhibitors of human complement factor B. 6 Oct 2009
• Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies. 6 Oct 2009
• Synthesis and evaluation of lysophosphatidylserine analogues as inducers of mast cell degranulation. Potent activities of lysophosphatidylthreonine and its 2-deoxy derivative. 6 Oct 2009
• Discovery of novel antileishmanial agents in an attempt to synthesize pentamidine-aplysinopsin hybrid molecule. 6 Oct 2009

See a longer list of these articles.

Technical information about 'Structure-Activity Relationship'

Definition: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.

Descriptor UI: D013329

Alternative terms: Structure-Activity Relationship; Relationship, Structure-Activity; Relationships, Structure-Activity; Structure Activity Relationship; Structure-Activity Relationships;

Tree Number: G02.111.830; G07.690.830;

History Note: 72

Technical Notes: coordinate NIM with specific drug IM; DF: STRUCT ACTIV RELAT