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Sequence, structure and activity of phosphoglycerate kinase: a possible hinge-bending enzyme
The fitting of sequenced peptides to a high-resolution X-ray map of phosphoglycerate kinase has yielded the complete sequence and structure of the horse muscle enzyme. Metal ADP and ATP substratesExpand
Structural requirements for opioid activity of analogues of the enkephalins
Of the analogues described, [d-Ala2, d-Leu5]-enkephalin is the most active peptide in the three assay systems, the mouse vas deferens, the guinea pig ileum and the rat brain opiate receptor preparations. Expand
The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate.
The discovery of a potent intracellular inhibitor of human neutrophil elastase which is orally active and has a long duration of action is described. The pharmacodynamic and pharmacokineticExpand
Conformation of two 4'-thio-2'-deoxynucleoside analogs studied by 5000-MHz proton NMR spectroscopy and x-ray crystallography.
An integrated conformational study is reported on the structurally modified nucleosides 4'dhiothymidine (l), an isoelectronic analogue of natural thymidine, andExpand
Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor
The discovery of three further derivatives of pyrrolidine trans-lactams, which fulfill the criteria required for back-up candidates 28, 29, and 32, and are highly potent and selective HNE inhibitors, with a prolonged pharmacodynamic action. Expand
Synthesis and anti-herpes virus activity of 2'-deoxy-4'-thiopyrimidine nucleosides.
A series of 5-substituted 2'-deoxy-4'-thiopyrimidine nucleosides was synthesized and evaluated as potential antiviral agents and the compound with the broadest spectrum of activity was 2'- deoxy-5-ethyl- 4'-thiouridine which showed significant activity against HSV-1, HSV2, and VZV. Expand
Amino-acids and peptides. Part 42. Synthesis of a protected docosa peptide having the sequence of mast-cell degranulating peptide
Fully protected mast-cell degranulating peptide (1) has been synthesised by the picolyl ester ‘handle’ method.
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.
An explanation for the SAR observed based is presented along with a proposed docking of 38E1 into the active site of the glucocorticoid receptor. Expand
Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams.
Described are the acylation binding of trans-lactam 1 to porcine pancreatic elastase, the selection of the SO2Me activating group for the lactam N which also confers metabolic stability in hamsterExpand
Acyl carbamate directing groups in nucleoside synthesis: Applications in the synthesis of 2′-deoxy-5-ethyl-4′-thiouridine
Abstract The use of the 3- O -( N -acyl)carbamoyl directing groups in the synthesis of the potent anti-Herpes virus agent 2′-deoxy-5-ethyl-4′-thio-D-uridine is described. This includes details ofExpand