Oral bioavailability measurements in rats for over 1100 drug candidates studied at SmithKline
Beecham Pharmaceuticals (now GlaxoSmithKline) have allowed us to analyze the relative …

3-(Acylamino)-5-phenyl-2H-l, 4-benzodiazepines, antagonists of the peptide hormone
cholecystokinin (CCK), are described. Developed by reasoned modificationof the known …

In recent years chemists have become increasingly successful in the design of peptide
analogs which are resistant to metabolism while retaining high biological activity. This may be …

Conformational analysis has resulted in the design and synthesis of somatostatin analogues
which show increased duration of action 1–3 . The introduction of covalent conformational …

… DF Veber, in Peptides: Proceedings ofthe 6th American Peptide Symposium, E. Gross and
J… RM Freidinger, DA Schwenk, DF Veber, in Peptides: Proceedings of the 6th American …

The nature proteins of retroviruses originate as a result of proteolytic cleavages of polyprotein
precursors. Retroviruses encode proteases responsible for several of these processing …

General methods have been devised for the synthesis of lactam-constrained dipeptide
analogues having five-, six-, and seven-membered rings. Three different paths from protected …

THE biological activity of an organic compound represents the sum of several properties,
including solubility, absorption, transport, plasma protein binding, metabolism and receptor …

Inhibitors of human methionine aminopeptidase type 2 (hMetAP2) are of interest as potential
treatments for cancer. A new class of small molecule reversible inhibitors of hMetAP2 was …

We describe the design and synthesis of nonpeptidal antagonists of the peptide hormone
cholecystokinin. Several of these compounds have high specificity and nanomolar binding …