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18 条记录 (耗时 0.018 秒)

    Synthetic analogues of .alpha.-melanotropin
    4.
    发明授权
    Synthetic analogues of .alpha.-melanotropin 失效
    α-促黄体素的合成类似物

    公开(公告)号：US4485039A

    公开(公告)日：1984-11-27

    申请号：US387424

    申请日：1982-06-11

    申请人： Victor J. Hruby ,  Mac E. Hadley ,  Tomi K. Sawyer

    发明人： Victor J. Hruby ,  Mac E. Hadley ,  Tomi K. Sawyer

    IPC分类号： A61K38/00 ,  C07K14/695 ,  C07C103/52

    CPC分类号： C07K14/695 ,  A61K38/00 ,  Y10S930/29

    摘要： Cyclic analogues of the tridecapeptide hormone, .alpha.-melanotropin. (.alpha.-melanocyte stimulating hormone, .alpha.-MSH), wherein a physiologically stable intramolecular interaction exists (1) between the amino acid residue at position 4 and an amino acid residue at position 10 or 11, and/or (2) between the amino acid residue at position 5 and an amino acid residue at position 10 or 11. Preferred analogues, e.g., [half-Cys.sup.4, half-Cys.sup.10 ]-.alpha.-MSH display greatly increased in vitro potency, prolongation, and resistance to enzymatic degradation.

    摘要翻译： 十三肽激素，α-促黄体素的环状类似物。 （α-黑素细胞刺激激素，α-MSH），其中存在生理稳定的分子内相互作用（1）位置4的氨基酸残基与10或11位的氨基酸残基和/或（2）氨基 5位的酸残基和10或11位的氨基酸残基。优选的类似物，例如[半胱氨酸Cys4，半胱氨酸-10]-α-MSH显示出大大提高了体外效力，延长和耐酶降解。

    Method of diminishing glucose levels resulting from endogenous glucagon
    5.
    发明授权
    Method of diminishing glucose levels resulting from endogenous glucagon 失效
    降低内源胰高血糖素产生的葡萄糖水平的方法

    公开(公告)号：US4430326A

    公开(公告)日：1984-02-07

    申请号：US333376

    申请日：1981-12-22

    申请人： Victor J. Hruby ,  Marvin D. Bregman

    发明人： Victor J. Hruby ,  Marvin D. Bregman

    IPC分类号： C07K14/605 ,  A61K37/02

    CPC分类号： C07K14/605

    摘要： Effects of endogenous glucagon in mammals are diminished by administration of compositions including certain semi-synthetic analogs of glucagon. Preferred analogs include [N.sup..alpha. -TNB, HArg.sup.12 ]glucagon and [dHis.sup.1 ][N.sup..alpha. -TNB, HArg.sup.12 ]glucagon, parenterally administered at doses of from about 0.05 to about 50 mg of analog per kg of body weight.

    摘要翻译： 内源性胰高血糖素在哺乳动物中的作用通过给予包括某些胰高血糖素的半合成类似物的组合物来减少。 优选的类似物包括以每kg体重约0.05至约50mg的类似物的剂量肠胃外给药的[Nα-TNB，HArg12]胰高血糖素和[dHis1] [Nα-TNB，HArg12]胰高血糖素。

    Methods of Identifying Pancreatic Cancer Cells
    6.
    发明申请
    Methods of Identifying Pancreatic Cancer Cells 有权
    鉴定胰腺癌细胞的方法

    公开(公告)号：US20080261818A1

    公开(公告)日：2008-10-23

    申请号：US12041350

    申请日：2008-03-03

    申请人： Haiyong Han ,  Robert J. Gillies ,  Victor J. Hruby ,  David L. Morse

    发明人： Haiyong Han ,  Robert J. Gillies ,  Victor J. Hruby ,  David L. Morse

    IPC分类号： C40B30/00 ,  C12Q1/68

    CPC分类号： G01N33/57438 ,  C12Q1/6886 ,  C12Q2600/158

    摘要： Methods that identify cells as pancreatic cancer cells based on assessing the expression of combinations of target molecules expressed preferentially on pancreatic cancer cells are disclosed. Combinations were initially discovered by microarray analysis and selected based upon tumor specificity, relative lack of cross-reactivity with normal tissues, and applicability as targets of multispecific ligands. The claimed methods encompass measuring the expression of three or more specific target molecules in combination and correlating positive expression of the combination with an identification of the cell as a pancreatic cancer cell.

    摘要翻译： 公开了基于评估胰腺癌细胞优先表达的靶分子的组合的表达来鉴定细胞作为胰腺癌细胞的方法。 组合最初通过微阵列分析发现，并且基于肿瘤特异性，与正常组织的相对缺乏交叉反应性和作为多特异性配体的靶标的适用性来选择。 要求保护的方法包括组合测量三种或更多种特异性靶分子的表达，并将组合的阳性表达与作为胰腺癌细胞的细胞鉴定相关联。

    Peptides having potent antagonist and agonist bioactivities at melanocortin receptors
    7.
    发明授权
    Peptides having potent antagonist and agonist bioactivities at melanocortin receptors 失效
    肽在黑皮质素受体中具有有效的拮抗剂和激动剂生物活性

    公开(公告)号：US5731408A

    公开(公告)日：1998-03-24

    申请号：US420972

    申请日：1995-04-10

    申请人： Mac E. Hadley ,  Victor J. Hruby ,  Shubh D. Sharma

    发明人： Mac E. Hadley ,  Victor J. Hruby ,  Shubh D. Sharma

    IPC分类号： C07K14/685 ,  C07K7/00

    CPC分类号： C07K14/685 ,  Y10S930/27

    摘要： Cyclic lactam peptides, seven amino acids in length, having D-2'-naphthylalanine (D-2'-Nal) or D-para-iodo-phenylalanine D-(p-I)Phe at position 4 of the peptide provided potent and specific antagonists of the two neural melanocortin receptors and of the peripheral receptor. In particular, the peptide ##STR1## was found to be a potent antagonist of the MC3 and MC4 receptors with partial agonist activity, and a full agonist of the MC1 and MC5 receptors; the peptide ##STR2## was found to be a potent antagonist of the MC3 and MC4 receptors with partial agonist activity. Both peptides have antagonist activities in the classical frog skin bioassay for pigmentation at the MC1 receptor.

    摘要翻译： 肽的位置4处具有D-2'-萘基丙氨酸（D-2'-Nal）或D-对 - 碘 - 苯丙氨酸D-（pI）Phe的长度为7个氨基酸的环内酰胺肽提供了有效的和特异性的拮抗剂 的两种神经黑皮质素受体和外周受体。 特别地，发现肽“IMAGE”是具有部分激动剂活性的MC3和MC4受体的有效拮抗剂，以及MC1和MC5受体的完全激动剂; 发现肽“IMAGE”是具有部分激动剂活性的MC3和MC4受体的有效拮抗剂。 两种肽在经典青蛙皮肤生物测定中具有拮抗剂活性，用于MC1受体的色素沉着。

    Conformationally constrained alpha-melanotropin analogs with specific central nervous system activity
    10.
    发明授权
    Conformationally constrained alpha-melanotropin analogs with specific central nervous system activity 失效
    具有特定中枢神经系统活性的构象约束的α-黑素素类似物

    公开(公告)号：US4649191A

    公开(公告)日：1987-03-10

    申请号：US608708

    申请日：1984-05-10

    申请人： Victor J. Hruby

    发明人： Victor J. Hruby

    IPC分类号： A61K38/00 ,  C07K14/685 ,  C07K7/06

    CPC分类号： C07K14/685 ,  A61K38/00 ,  Y10S930/26 ,  Y10S930/27

    摘要： Novel compounds which are analogs of .alpha.-melanotropin and which exhibit reactivity for the central nervous system receptors without exhibiting substantial reactivity for the peripheral receptors are disclosed. The compounds of the present invention are polypeptides of the formula: ##STR1## wherein R.sup.1 is a substituted or unsubstituted aromatic radical;R.sup.2 is hydrogen or a methyl group;R.sup.3 is carboxylate, carboxamide, hydroxymethyl, or aldehyde group or a peptide residue;R.sup.4 is a simple amino acid residue;R.sup.5 is a simple amino acid residue;R.sup.6 and R.sup.7, which may be the same or different, are hydrogen, methyl or lower alkyl having one to five carbon atoms;R.sup.8 and R.sup.9, which may be the same or different, are hydrogen, methyl or lower alkyl having one to five carbon atoms;X and Y are sulfur, methylene, SO, or SO.sub.2 ;Z is --NH.sub.2, ##STR2## and n is an integer greater than or equal to 2.The noval compounds may be used in humans and lower animals to facilitate memory and behavior, improve fetal growth and development, enhance attention, improve socialization, stimulate sexual activity, reverse morphine analgesia, act as an antidepressant, act as an antipyretic and centrally direct effects on visceral functions.

    摘要翻译： 公开了作为α-促黄体激素类似物并且对中枢神经系统受体表现出反应性而不对外周受体表现出显着反应性的新型化合物。 本发明的化合物是下式的多肽：其中R 1是取代或未取代的芳族基团; R2是氢或甲基; R 3是羧酸酯，甲酰胺，羟甲基或醛基或肽残基; R4是简单的氨基酸残基; R5是简单的氨基酸残基; R 6和R 7可以相同或不同，是氢，甲基或具有1-5个碳原子的低级烷基; R8和R9可以相同或不同，是氢，甲基或具有1-5个碳原子的低级烷基; X和Y是硫，亚甲基，SO或SO 2; Z是-NH2，，n是大于或等于2的整数。该化合物可用于人类和低等动物，以促进记忆和行为，改善胎儿生长发育，增强注意力，改善社会化，刺激 性活动，反向吗啡镇痛作为抗抑郁药，作为对内脏功能的解热和中心直接作用。