Now showing items 41-50 of 71
Development of a model for the δ-opioid receptor pharmacophore. 4. Residue 3 dehydrophenylalanine analogues of Tyr-c[ D -Cys-Phe- D -Pen]OH (JOM-13) confirm required gauche orientation of aromatic side chain
(Wiley Subscription Services, Inc., A Wiley Company, 1996-09)
We have previously proposed a model for the δ-opioid receptor binding conformation of the high affinity tetrapeptide Tyr-c[ D -Cys-Phe- D -Pen] OH (JOM-13) based on experimental and theoretical conformational analysis of ...
Characterization of the intestinal transport parameters for small peptide drugs
(Elsevier, 1990-08)
Several laboratories have recently shown that many peptides and peptide-similar drugs are well absorbed in the mammalian intestine via the peptide transport system for nutrient small peptide (dipeptides and tripeptides) ...
Voronoi binding site models: Calculation of binding modes and influence of drug binding data accuracy
(John Wiley & Sons, Inc., 1989-07)
A new and accurate method for calculating the geometrically allowed modes of binding of a ligand molecule to a Voronoi site model is reported. It is shown that the feasibility of the binding of a group of atoms to a Voronoi ...
Some observations on classical QSAR
(Kluwer Academic Publishers; ESCOM Science Publishers B.V. ; Springer Science+Business Media, 1993-12)
Classical QSAR began almost 30 years ago. This article briefly traces its development, use and impact in relation to drug design and medicinal chemistry. Particular aspects discussed include hydrophobicity, relative potency ...
Design, synthesis and activity against human cytomegalovirus of non-phosphorylatable analogs of toyocamycin, sangivamycin and thiosangivamycin
(Elsevier, 1992-12)
A number of 7-alkyl 4-aminopyrrolo[2,3-pyrimidine derivatives related to toyocamycin, sangivamycin and thiosangivamycin have been prepared and tested for their activity against human cytomegalovirus (HCMV). Only the thioamide ...
Structural organization of G-protein-coupled receptors
(Kluwer Academic Publishers; Springer Science+Business Media, 1999-07)
Atomic-resolution structures of the transmembrane 7-α-helical domains of 26 G-protein-coupled receptors (GPCRs) (including opsins, cationic amine, melatonin, purine, chemokine, opioid, and glycoprotein hormone receptors ...
Atomic Physicochemical Parameters for Three-Dimensional Structure-Directed Quantitative Structure-Activity Relationships I. Partition Coefficients as a Measure of Hydrophobicity
(John Wiley & Sons, Inc., 1986-08)
Earlier we showed (A. K. Ghose and G. M. Crippen, J. Med. Chem. , 28, 333, 1985) the necessity of atomic physicochemical parameters in three-dimensional receptor mapping. Here we derive more refined and widely applicable ...
Alternate substrates and inhibitors of 1-aminocyclopropane-1-carboxylic acid synthase
(Elsevier, 1987-06)
Structural analogs of (-)-S-adenosyl--methionine (SAM), in which the heterocyclic base was modified, were used to initiate studies to elucidate the active site conformation of the enzyme 1-aminocyclopropane-1-carboxylic ...