Abstract: The invention relates to methods of preparing peptide hydrazides useful in as intermediates in preparing derivatized peptides and amenable to conversion to reactive azide comprising species. The invention relates to chemical methods of preparing such species from protected peptide-resins containing the aspartyl or glutamyl residues with orthogonal side-chain carboxylic acid protecting groups ester of Asp and Glu.

Abstract: A solution phase synthetic method for preparing basic tripeptides of the formula Gly-Xaa-Gly-X which have in various biological properties such as stimulating protein production when used as additives in a bioreactor. The basic tripeptides of the invention may be produced on gram or kilogram scale.

Abstract: This invention describes a method for removing unreacted activated lipid moieties using a bifunctional ligand containing a first functional group reactive with the activating group of the lipid and a second functional group capable of binding to an affinity reagent or support. These reagents can be used to quench reactions between peptides/proteins and other moieties such as activated PEGs or lipids. Once the reaction has been quenched, the reaction mixture can be passed over an affinity column that will bind the peptide, biotin or other ligand attached to the “quenched” reagent and thereby remove it from the reaction mixture.

Abstract: Peptides derived from three regions of the lectin domain of GMP-140 (P-selectin) and the related selectins, ELAM-1 (E-selectin) and the lymphocyte homing receptor (L-selectin), have been found to inhibit neutrophil adhesion to GMP-140. These and additional peptides have been synthesized, having as their core region portions of the 74-76 amino acid sequence of GMP-140, with residue 1 defined as the N-terminus of the mature protein after the cleavage of the signal peptide. Examples demonstrate the inhibition of the binding of neutrophils to GMP-140 of peptides in concentrations ranging from 30 to 1500 .mu.mol. It has been found that alterations within the core sequence, as well as N-terminal and C-terminal flanking regions, do not result in loss of biological activity. The peptides are useful as diagnostics and, in combination with a suitable pharmaceutical carrier, for clinical applications in the modulation or inhibition of coagulation processes or inflammatory processes.

Abstract: Peptides which consist of six to eight, predominately D-amino acids and which bind to tumor necrosis factor-alpha, prevent tumor necrosis factor-alpha from binding to its receptors and inhibit tumor necrosis factor-alpha activity are disclosed. Methods of inhibiting tumor necrosis factor-alpha activity and of treating individuals suffering from tumor necrosis factor-alpha-mediated diseases and disorders are disclosed.

Abstract: Novel cyclic peptides of the selectin 54-63 sequence exhibit unexpected and desired properties. Specific points of cyclization or conformational restriction in conjunction with specific substitutions have been identified that not only unexpectedly enhance the biological activity of these compounds, but also significantly increase their resistance to enzymatic degradation. Formulae of the active compounds and representative examples of preferred peptides are presented herein.

Abstract: The present invention provides novel peptides having as their core region portions of the 109-118 amino acid sequence of P-selectin, E-selectin or L-selectin. The invention also provides pharmaceutical compositions comprising the peptides of the invention, and diagnostic and therapeutic methods utilizing the peptides and pharmaceutical compositions of the invention.

Abstract: The present invention provides novel peptides constructed to mimic the topology of the surface exposed segements of the 23-30 sequence and Tyr.sup.118 in the lectin domain of P-selectin. The invention also provides pharmaceutical compositions comprising the peptides of the invention, and diagnostic and therapeutic methods utilizing the peptides and pharmaceutical compositions of the invention.

Abstract: The present invention provides novel peptides derived from portions of the sequence of amino acids 23-26 and 27-30 of P-selectin. The invention also provides pharmaceutical compositions comprising the peptides of the invention, and diagnostic and therapeutic methods utilizing the peptides and pharmaceutical compositions of the invention. The peptides of this invention can be used in the modulation or inhibition of coagulation processes or inflammatory processes.

Abstract: Peptides which consist of 4-25 amino acids and which bind to tumor necrosis factor-alpha, prevent tumor necrosis factor-alpha from binding to its receptors and inhibit tumor necrosis factor-alpha activity are disclosed. Methods of inhibiting tumor necrosis factor-alpha activity and of treating individuals suffering from tumor necrosis factor-alpha-mediated diseases and disorders are disclosed.