Abstract: Compounds of the formula ##STR1## or the alkyl (1-6C), alkenyl (1-6C), or arylalkyl (7-12C) amides or salts including the cycloamido forms thereof;whereinn is 1 or 2;whereinwhen n is 1, X is a mono- or disubstituted or unsubstituted hydrocarbyl (1-20C) moiety optionally containing 1 or 2 nonadjacent heteroatoms (O, S or N), and wherein said substitution is selected from the group consisting of halo, OR, and SR, wherein R is H or lower alkyl (1-4C); when n is 2, one X is as above defined and the other X is lower alkyl (1-4C);Y is selected from the group consisting of ##STR2## wherein m is 1 or 2; andAA.sub.C is an amino acid coupled through a peptide bond to the remainder of the compound of formula 1, are useful as affinity ligands, elution reagents, solution inhibitors, diagnostic reagents and therapeutics. These compounds and analogous tripeptide glutathione analogs can be used as members of panels to obtain specific characteristic profiles for various glutathione-S-transferases.

Abstract: Compounds of the formula ##STR1## and the esters, amides, amide/esters and salts thereof, wherein YCO is .gamma.-glu or .beta.-asp;G* is phenylglycine or glycine;Z is CH.sub.2, O or S; andX is a hydrocarbon radical selected from C.sub.6 -C.sub.8 alkyl or selected aromatic groupsare useful in modulating hematopoiesis in bone marrow, mitigating the bone-marrow-destructive effects of a chemotherapeutic agent, and in potentiating the toxicity of chemotherapeutic agents.

Abstract: Modulators of the immune system can be identified by determining the ability of candidate substances to affect the interaction of PKC-theta or a fragment thereof with its cognate. The interaction can be measured using binding of the cognate as an index, or can be measured using a physiological response.

Abstract: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula ##STR1## whereineach A is independently a proton-accepting substituent;each R is independently a noninterfering substituent;n is 0, 1, or 2; andeach linker is independently an isostere of --NHCONH-- or of --N.dbd.N-- or of --NHCO--.Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.

Abstract: Improved methods for determining interactions between peptides or proteins and small molecules are disclosed. The invention methods can be used to screen libraries of either the small molecules or the proteins. In general, the methods comprise contacting an agent/ligand complex consisting essentially of an agent to be tested for binding to a target protein coupled to a ligand capable of binding a proteinaceous ligand-binding domain with a first fusion protein comprising said target protein and a first complementary portion of a segregable protein; and a second fusion protein comprising a proteinaceous ligand-binding domain and a second complementary portion of said segregable protein; and detecting whether the first complementary portion and second complementary portion are brought into proximity.

Abstract: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula ##STR1## wherein each Ar is independently an aromatic moiety; each A is independently a proton-accepting substituent;each R is independently a noninterfering substituent;m is 0 or 1;n is 4-6; andeach linker is independently an isostere of --CH.sub.2 --, --CH.dbd.CH-- or --NCHO--. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.

Abstract: Solid phase supported synthesis of peptides and other molecules using protecting groups comprising p-nitrobenzyl is described.

Abstract: Compounds useful as affinity chromatography supports and as labeled reagents are disclosed. The compounds are peptides which can be constituted in families of positively charged, negatively charged or uncharged small peptides or the amidated forms thereof with varying characteristics as to charge, charge distribution, hydrophobicity, cyclization, and helical conformation propensity.

Abstract: Panels which consist of individual members, said members comprising proteins, wherein at least one of the members of the panel is a protein other than an immunoglobulin (Ig) or fragment thereof and wherein the presence of said non-Ig protein enriches the panel are described herein. These panels can be tested for reactivity with an analyte to create a profile. Such profiles can be used in pattern matching, analysis of samples and other analyses. Illustrated herein using such panels is a method to determine reactivity of a candidate compound with a target "receptor" which method does not require the physical presence of the receptor. By providing a formula for treating data obtained from a reference panel of this type which is predictive of reactivity with the target receptor, the compound to be tested can be physically assessed with respect to the reference panel, the formula applied, and reactivity with the actual target receptor may be predicted.

Abstract: A method to potentiate the effect of a chemotherapeutic agent in a tumor cell, which method comprises administering to said tumor cell, along with said chemotherapeutic agent, a potentiating amount of a compound of the formula: ##STR1## or an amide, ester or hybrid amide/ester thereof, wherein X is a hydrocarbon radical optionally substituted on any aromatic moiety contained therein; Y--CO is .gamma.-Glu or .beta.-Asp and AA.sub.C is an amino acid, preferably glycine, phenylglycine, .beta.-alanine, alanine or phenylalanine is disclosed.Similar compounds can also be used to selectively exert cytotoxicity versus target cells as compared to nontarget cells and also to elevate the production of GM progenitors in bone marrow of mammalian subjects.

Abstract: Methods for assessing libraries of candidate modulators of intracellular signaling transmission pathways are described. The methods assess the ability of candidates from the library to inhibit the binding of peptides which represent participants in the signaling pathways as either a signal-generating protein or its cognate partner binding at a noncatalytic site. Specific peptides useful in this regard have been identified.

Abstract: The present invention discloses that the fyn protein binds to the PKC-theta protein. Based on this observation, the present invention provides methods of identifying agents which can be used to modulate immune system activity by blocking fyn/PKC-theta binding and therapeutic methods using such agents.

Abstract: Compounds of the formula ##STR1## and the esters, amides, amide/esters and salts thereof, wherein YCO is .gamma.-glu or .beta.-asp;G* is phenyl glycine or glycine;Z is CH.sub.2, O or S; andX is a hydrocarbon radical of 1-20 C;are useful in stimulating the differentiation of bone marrow, mitigating the bone-marrow-destructive effects of a chemotherapeutic agent, and in potentiating the toxicity of chemotherapeutic agents.

Abstract: Compounds of the formula ##STR1## or the alkyl (1-6C), alkenyl (1-6C), or arylalkyl (7-12C) amides or salts including the cycloamido forms thereof;wherein n is 1 or 2;wherein when n is 1, X is a mono- or disubstituted or unsubstituted hydrocarbyl (1-20C) moiety optionally containing 1 or 2 nonadjacent heteroatoms (O, S or N), and wherein said substitution is selected from the group consisting of halo, OR, and SR, wherein R is H or lower alkyl (1-4C); when n is 2, one X is as above defined and the other X is lower alkyl (1-4C);Y is selected from the group consisting of ##STR2## wherein m is 1 or 2; and AA.sub.C is an amino acid coupled through a peptide bond to the remainder of the compound of formula 1, are useful as affinity ligands, elution reagents, solution inhibitors, diagnostic reagents and therapeutics. These compounds and analogous tripeptide glutathione analogs can be used as members of panels to obtain specific characteristic profiles for various glutathione-S-transferases.

Abstract: Panels which consist of individual members, said members comprising proteins, wherein at least one of the members of the panel is a protein other than an immunoglobulin (Ig) or fragment thereof and wherein the presence of said non-Ig protein enriches the panel are described herein. These panels can be tested for reactivity with an analyte to create a profile. Such profiles can be used in pattern matching, analysis of samples and other analyses. Illustrated herein using such panels is a method to determine reactivity of a candidate compound with a target "receptor" which method does not require the physical presence of the receptor. By providing a formula for treating data obtained from a reference panel of this type which is predictive of reactivity with the target receptor, the compound to be tested can be physically assessed with respect to the reference panel, the formula applied, and reactivity with the actual target receptor may be predicted.

Abstract: A process for preparing a trinucleotide phosphoramidite comprising reacting a 3',5'-dihydroxy dinucleoside with a nucleoside 5'-phosphoramidite; oxidizing this trinucleotide phosphite to produce the 3'-hydroxyl trinucleotide; and finally converting the 3'-hydroxy trinucleotide to the 3'-phosphoramidite derivative. Such trinucleotide phosphoramidites provide a convenient route for synthesizing oligonucleotides with randomized codons at specified positions.

Abstract: Compounds of the formula: ##STR1## or a salt thereof, wherein n is 1 or 2;wherein when n is 1, X is a mono- or disubstituted or unsubstituted C.sub.1-20 hydrocarbon radical wherein any substitution is selected from the group consisting of halo, OR, and SR, wherein R is H or C.sub.1-4 alkyl;and wherein, when n is 2, one X is defined as for n=1 and the other X is lower C.sub.1-4 alkyl; ##STR2## wherein m is 1 or 2; AA.sub.C is an amino acid coupled through a peptide bond to the remainder of the compound of Formula (1) selected from the group consisting of glycine, valine, alanine, 4-aminobutyric acid, aspartic acid, phenylglycine, histidine, tryptophan, tyrosine, and phenylalanine, wherein the phenyl group of phenylalanine or phenylglycine may optionally contain a single substitution selected from the group consisting of halo, OR, and SR, wherein R is H or C.sub.1-4 alkyl;with the proviso that if Y is ##STR3## AA.sub.C is not Gly; and if Y is ##STR4## and X is benzyl, AA.sub.

Abstract: The precision of identification of analyte composition in a sample, where the possible analytes each provide a series of values for characteristic parameters; in particular where the parameters are generated by cross-reaction with specific binding reagents, is enhanced by applying pattern recognition techniques. Samples to be tested are evaluated with respect to each survey parameter to obtain a pattern of parameter values with respect to each analyte at a given concentration. In the case of the use of a panel of specific binding reagents, the samples to be tested are reacted with this panel and the affinities at various analyte concentrations are determined. This results in a databank of "SC profiles" for known concentrations of each analyte. This databank is stored in a computationally accessible form, which then can be matched against SC profiles obtained by testing unknown samples.

Abstract: A method for determining the amount of analyte in a sample utilizes a series of test regions with systematically varied, preferably monotonically increasing, affinity for a specific binding partner for an analyte or for the analyte itself. By determining the portion of test regions which are capable of binding specific binding partner in competition with the analyte in the sample, or which bind the analyte, the amount of analyte may be estimated. Thus, titration of affinity replaces titration of concentration, allowing assays to be performed without the need for serial dilution steps.

Abstract: Compounds of the formula ##STR1## or the alkyl (1-6 C), alkenyl (1-6 C), or arylalkyl (7-12 C) amides or salts including the cycloamido forms thereof;wherein n is 1 or 2;wherein when n is 1, X is a mono- or disubstituted or unsubstituted hydrocarbyl (1-20 C) moiety optionally containing 1 or 2 nonadjacent heteroatoms (O, S or N), and wherein said substitution is selected from the group consisting of halo, OR, and SR, wherein R is H or lower alkyl (1-4 C); when n is 2, one X is as above defined and the other X is lower alkyl (1-4 C);Y is selected from the group consisting of ##STR2## wherein m is 1 or 2; and AA.sub.C is an amino acid coupled through a peptide bond to the remainder of the compound of formula 1, are useful as affinity ligands, elution reagents, solution inhibitors, diagnostic reagents and therapeutics. These compounds and analogous tripeptide glutathione analogs can be used as members of panels to obtain specific characteristic profiles for various glutathione-S-transferases.