摘要:
Pharmaceutical compositions and methods of using them. Lipid formulations of a glutathione analog and methods of manufacturing them. Their use to stimulate hematopoiesis, protect hematopoietic cells from damage caused by radiation or chemotherapy, or potentiate the stimulatory action of one or a combination of cytokines on colony formation by hematopoietic progenitor cells, protect a subject from a destructive effect of a chemotherapeutic agent or irradiation, or to potentiate the effect of a chemotherapeutic agent.
摘要:
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 wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; m is 0 or 1; n is 0, 1, or 2; and each linker is independently —NHCNHNH—, —NHCOO—, OCOO—,—CH═CH—, —CH═N—, —CH2CH2—, —NHCH2—, —OCO— or —COO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
摘要:
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 A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each 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.
摘要:
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; and each 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.
摘要:
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.
摘要:
A method to determine reactivity of a candidate compound with a target receptor which method does not require the physical presence of the receptor is disclosed. By providing a formula for treating data obtained from a reference set of receptors which is predictive of reactivity with the target receptor, the compound to be tested can be physically assessed with respect to the reference receptors, the formula applied, and reactivity with the actual target receptor may be predicted.
摘要:
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 wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of —NHCONH— or of —N═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.
摘要:
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.
摘要:
Compounds of the formula ##STR1## or of the formula ##STR2## or the amides, esters or salts thereof, wherein: S.sup.x is S.dbd.O, O.dbd.S.dbd.O, S.dbd.NH, HN.dbd.S.dbd.O, Se.dbd.O, O.dbd.Se.dbd.O, Se.dbd.NH, HN.dbd.Se.dbd.O, S.sup.+ R.sup.3 wherein R.sup.3 is alkyl (1-6C) or O--C.dbd.O or HN--C.dbd.O;each R of R.sup.1, and R.sup.2 is independently H or a noninterfering substituent;wherein (conj) represents a conjugated system capable of transmitting electrons;n is 0 or 1;YCO is selected from the group consisting of .gamma.-Glu, .gamma.-Glu-Gly, Glu, Glu-Gly, .beta.Asp, .beta.-Asp-Gly, Asp and Asp-Gly;AA.sub.C is an amino acid linked through a peptide bond to the remainder of said compound of Formula 1; andN(Z) represents a reduced nitrogen-containing leaving group and L represents an electron-withdrawing leaving group,are useful as prodrugs and to generate active components released by the activity of glutathione S-transferase.
摘要翻译:式或式的化合物或其酰胺,酯或盐,其中:Sx为S = O,O = S = O,S = NH,HN = S = O,Se = O,O = Se = O ,Se = NH,HN = Se = O,S + R3,其中R3是烷基(1-6C)或OC = O或HN-C = O; R 1的每个R和R 2独立地为H或非干扰取代基; 其中(conj)表示能够传输电子的共轭系统; n为0或1; YCO选自γ-Glu,γ-Glu-Gly,Glu,Glu-Gly,β-Asp,β-Asp-Gly,Asp和Asp-Gly; AAC是通过肽键与所述式1化合物的剩余部分连接的氨基酸; 并且N(Z)表示还原的含氮离去基团,L表示吸电子离去基团,可用作前药并产生通过谷胱甘肽S-转移酶活性释放的活性成分。
摘要:
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.