公开(公告)号：US4244946A

公开(公告)日：1981-01-13

申请号：US47026

申请日：1979-06-11

申请人： Jean E. F. Rivier ,  Wylie W. Vale, Jr.

发明人： Jean E. F. Rivier ,  Wylie W. Vale, Jr.

IPC分类号： A61K38/04 ,  A61K38/00 ,  A61P5/00 ,  A61P15/00 ,  C07K7/23 ,  C07K14/575 ,  A61K37/00 ,  C07C103/52

CPC分类号： C07K7/23 ,  A61K38/00 ,  Y10S514/80 ,  Y10S930/13

摘要： [im-Bzl D-His.sup.6 ]LRF and [D-His.sup.6 (im-Bzl), Pro.sup.9 -NEt]LRF exhibit hydrophillicity comparable to that of LRF and act as superagonists exhibiting potencies, respectively, about 12 and more than 200 times that of LRF. The peptides or their nontoxic salts can be administered by intravenous subcutaneous, sublingual, oral, intravaginal, intranasal or rectal routes. The peptides can be used to regulate fertility in male and female mammals, including human beings.

摘要翻译： [im-Bzl D-His6] LRF和[D-His6（im-Bzl），Pro9-NEt] LRF表现出与LRF相当的亲水性，并且作为显示效力的超级拮抗剂分别为约12倍和超过200倍 LRF。 肽或其无毒盐可以通过静脉内皮下，舌下，口服，阴道内，鼻内或直肠途径施用。 这些肽可用于调节男性和女性哺乳动物（包括人类）的生育力。

公开(公告)号：US4215038A

公开(公告)日：1980-07-29

申请号：US950301

申请日：1978-10-16

申请人： Jean E. F. Rivier ,  Catherine L. Rivier ,  Wylie W. Vale, Jr.

发明人： Jean E. F. Rivier ,  Catherine L. Rivier ,  Wylie W. Vale, Jr.

IPC分类号： A61K38/00 ,  C07K7/16 ,  C07K7/23 ,  C07C103/52 ,  A61K37/00

CPC分类号： C07K7/23 ,  C07K7/16 ,  A61K38/00 ,  Y10S514/80 ,  Y10S930/13

摘要： Peptides which inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. The peptides have the structure:R.sub.1 --R.sub.2 --R.sub.3 --Ser--Tyr--R.sub.4 --R.sub.5 --Arg--R.sub.6wherein R.sub.1 is selected from the group consisting of D-pGlu, D-Pro, D-Trp, D-His, D-Arg, D-Leu, Formyl D-Pro, Acetyl D-Pro, Benzoyl D-Pro and .beta.-Ala; R.sub.2 is selected from the group consisting of D-Phe, Phe, N.alpha. Me-Phe, His, D-His, D-Trp, Trp and N.alpha. Me-Leu; R.sub.3 is selected from the group consisting of D-Trp, Trp; D-Phe, Phe, Pro and D-His; R.sub.4 is selected from the group consisting of Gly, D-Trp, D-Phe and D-Tyr; R.sub.5 is selected from the group consisting of Leu and N.alpha. Me Leu; and R.sub.6 is selected from the group consisting of Pro-Gly-NH.sub.2 and Pro--NH--CH.sub.2 --CH.sub.3.

摘要翻译： 抑制垂体分泌促性腺激素并抑制性腺释放类固醇的肽。 肽具有以下结构：R1-R2-R3-Ser-Tyr-R4-R5-Arg-R6，其中R1选自D-pGlu，D-Pro，D-Trp，D-His， Arg，D-Leu，甲酰基D-Pro，乙酰基D-Pro，苯甲酰基D-Pro和β-Ala; R2选自D-Phe，Phe，NαMe-Phe，His，D-His，D-Trp，Trp和NαMe-Leu; R3选自D-Trp，Trp; D-Phe，Phe，Pro和D-His; R4选自Gly，D-Trp，D-Phe和D-Tyr; R5选自Leu和NαMe Leu; 并且R 6选自Pro-Gly-NH 2和Pro-NH-CH 2 -CH 3。

公开(公告)号：US4207311A

公开(公告)日：1980-06-10

申请号：US856126

申请日：1977-11-30

申请人： Marvin R. Brown ,  Jean E. F. Rivier ,  Wylie W. Vale, Jr.

发明人： Marvin R. Brown ,  Jean E. F. Rivier ,  Wylie W. Vale, Jr.

IPC分类号： A61K38/00 ,  C07K7/08 ,  A61K37/00 ,  C07C103/52

CPC分类号： C07K7/083 ,  A61K38/00

摘要： Peptides having thermoregulative properties when administered to animals. The peptides are identified by the structure:R.sub.1 -R.sub.2 -Trp-Ala-Val-R.sub.3 -His-R.sub.4 -R.sub.5 -NH.sub.2 wherein: R.sub.1 is selected from the group consisting of hydrogen, an amino acid selected from the group consisting of p-Glu,Gln,Arg,Leu,Gly,Asn,Thr,Val, and Pro, and peptides having from 2 to 6 amino acids wherein the amino acids are selected from p-Glu,Gln,Arg,Leu,Gly,Asn,Thr,Val, and Pro, provided that when p-Glu is part of R.sub.1, p-Glu is located at the N terminus of the peptide; R.sub.2 is selected from the group consisting of D-pGlu, D-Gln and Gln; R.sub.3 is selected from the group consisting of D-Ala and Gly; R.sub.4 is selected from the group consisting of Phe and Leu and R.sub.5 is selected from Met and D-Met. Intermediates of the peptides are also provided.

摘要翻译： 当给予动物时具有温度特性的肽。 肽通过以下结构鉴定：R1-R2-Trp-Ala-Val-R3-His-R4-R5-NH2其中：R1选自氢，选自对 - Glu，Gln，Arg，Leu，Gly，Asn，Thr，Val和Pro，以及具有2至6个氨基酸的肽，其中氨基酸选自p-Glu，Gln，Arg，Leu，Gly，Asn，Thr ，Val和Pro，条件是当p-Glu是R1的一部分时，p-Glu位于肽的N末端; R2选自D-pGlu，D-Gln和Gln; R3选自D-Ala和Gly; R4选自Phe和Leu，R5选自Met和D-Met。 还提供了肽的中间体。

公开(公告)号：US20120259092A1

公开(公告)日：2012-10-11

申请号：US13444675

申请日：2012-04-11

申请人： David Chatenet ,  Jean Claude Reubi ,  Jean E. F. Rivier

发明人： David Chatenet ,  Jean Claude Reubi ,  Jean E. F. Rivier

IPC分类号： C07K17/02

CPC分类号： C07K14/57545 ,  A61K49/0002 ,  A61K51/088

摘要： Peptidic NPY antagonists selective for Y1 having an organic chelator, such as DOTA, coupled thereto which are useful for diagnostic procedures and receptor-mediated radiotherapy.

摘要翻译： 对于具有偶联有机螯合剂（例如DOTA）的Y1选择性的肽NPY拮抗剂可用于诊断程序和受体介导的放射治疗。

公开(公告)号：US07238775B2

公开(公告)日：2007-07-03

申请号：US11041676

申请日：2005-01-24

申请人： Jean E. F. Rivier ,  Jean Claude Reubi ,  Judit Erchegyi ,  Roland Riek

发明人： Jean E. F. Rivier ,  Jean Claude Reubi ,  Judit Erchegyi ,  Roland Riek

IPC分类号： A61K38/00

CPC分类号： C07K14/655 ,  A61K38/00

摘要： Analogs of SRIF which are selective for SSTR4 in contrast to the other cloned SRIF receptors are useful in determining tissue and cellular expression of the receptor SSTR4 and its biological role in regulating tumor growth. SRIF analog peptides, such as des-AA1,2,4,5,12,13[Ala7]-SRIF; des-AA1,2,4,5,12,13[Aph7]-SRIF, des-AA1,2,4,5,12,13[Aph7]Cbm-SRIF; des-AA1,2,4,5,12,13[Tyr2,Ala7]-Cbm-SRIF, and des-AA1,2,4,5,12,13[Tyr7,CβMe-L-2Nal8]-SRIF, and counterparts incorporating D-Cys3 and/or D-Trp8 and/or Ala11, bind with high affinity to the cloned human receptor SSTR4 and activate the receptor, but they do not bind with significant affinity to human SSTR1, SSTR2, SSTR3 or SSTR5. By incorporating an iodinated tyrosine in position-2 in these SSTR4-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, cytotoxins or highly radioactive elements can be N-terminally coupled or complexed thereto.

摘要翻译： 与其他克隆的SRIF受体相比，选择性SSTR4的SRIF的类似物可用于确定受体SSTR4的组织和细胞表达及其在调节肿瘤生长中的生物学作用。 SRIF类似物肽，例如des-AA 1,2,4,5,12,13，[Ala 7] -SRIF; des-AA 1,2,4,5,12,13 [Aph7] -SRIF，des-AA 1,2,4,5,12 ，13β-Cpm-SRIF; des-AA 1,2,4,5,12,13 [Tyr2]，Ala7-Cbm-SRIF，和des- AA 1,2,4,5,12,13 [Tyr 7]，C 2 H 2 Me-L-2Nal 8， SUP]] - SRIF，以及掺有D-Cys 3和/或D-Trp 8和/或Ala 11的对应物与高结合 对克隆的人受体SSTR4的亲和力并激活受体，但它们不以与人SSTR1，SSTR2，SSTR3或SSTR5的显着亲和力结合。 通过在这些SSTR4选择性SRIF类似物中加入位置2的碘化酪氨酸，可以提供用于药物筛选方法的标记化合物。 或者，为了用于治疗，细胞毒素或高度放射性元素可以是N-末端偶联或与其复合的。

公开(公告)号：US5874227A

公开(公告)日：1999-02-23

申请号：US556578

申请日：1995-11-10

申请人： Jean E. F. Rivier

发明人： Jean E. F. Rivier

IPC分类号： G01N33/15 ,  A61K38/00 ,  A61K38/04 ,  A61K45/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  C07K14/575 ,  G01N33/50 ,  G01N33/566 ,  G01N33/68 ,  G01N33/74 ,  G01N33/53 ,  A61K38/12 ,  A61K38/28 ,  C07K5/00

CPC分类号： G01N33/5008 ,  C07K14/57509 ,  G01N33/502 ,  G01N33/566 ,  G01N33/68 ,  G01N33/6842 ,  G01N33/74 ,  A61K38/00 ,  G01N2333/5751 ,  Y10S514/805 ,  Y10S930/26

摘要： Novel cyclic CRF antagonist peptides have the amino acid sequence: ##STR1## wherein Y is Ac, H, Ac-Thr or H-Thr; R.sub.30 is Glu or Cys; R.sub.32 is His or preferably a basic and/or aromatic D-amino acid such as D-His or D-Arg; R.sub.33 is Lys, Orn or Cys. The N-terminus may be extended by Leu or Asp-Leu. CML may be substituted for Leu.sup.27, and D-Tyr may be substituted for D-Phe to facilitate labelling. Lys may be substituted for Arg.sup.23, and its side chain connected by a lactam bridge to Glu.sup.20 to form a bicyclic peptide. Disclosed CRF antagonists include:(cyclo 30-33)�D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, Lys.sup.33 !r/hCRF(12-41),(cyclo 30-33)�Ac-Thr.sup.11, D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, Lys.sup.33 !r/hCRF(11-41),(cyclo 30-33)�D-Phe.sup.12, Nle.sup.21,38, Cys.sup.30,33 !r/hCRF(12-41),(bicyclo 20-23,30-33)�D-Phe.sup.12, Nle.sup.21,38, Lys.sup.23,33, Glu.sup.30 !-r/hCRF(12-41),(cyclo 30-33)�D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, D-His.sup.32, Lys.sup.33 !r/hCRF(12-41),(cyclo 30-30)�D-Phe.sup.12, Nle.sup.21,38, CML.sup.27, Glu.sup.30, D-His.sup.32, Lys.sup.33 !r/hCRF(12-41) and(cyclo 30-30)�D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, D-Arg.sup.32, Lys.sup.33 !r/hCRF(12-41).Labelled antagonists such as (cyclo 30-30)�I.sup.125 D-Tyr.sup.12, Nle.sup.21,38, Glu.sup.30, D-His.sup.32, Lys.sup.33 !r/hCRF(12-41) are useful in drug screening assays.

摘要翻译： 新型循环CRF拮抗剂肽具有氨基酸序列：其中Y是Ac，H，Ac-Thr或H-Thr; R30是Glu或Cys; R32是His或优选碱性和/或芳族D-氨基酸，例如D-His或D-Arg; R33是Lys，Orn或Cys。 N末端可以被Leu或Asp-Leu延伸。 CML可以代替Leu27，并且D-Tyr可以被D-Phe取代以便于标记。 Lys可以代替Arg23，其侧链通过内酰胺桥连接至Glu20以形成双环肽。 公开的CRF拮抗剂包括：（环30-33）[D-Phe12，Nle21,38，Glu30，Lys33] r / hCRF（12-41），（环30-33）[Ac-Thr11，D-Phe12，Nle21， 38，Glu30，Lys33] r / hCRF（11-41），（环30-33）[D-Phe12，Nle21,38，Cys30,33] r / hCRF（12-41），（双环20-23,30 -33）[D-Phe12，Nle21,38，Lys23,33，Glu30] -r / hCRF（12-41），（环30-33）[D-Phe12，Nle21,38，Glu30，D-His32，Lys33 ] r / hCRF（12-41），（环30-30）[D-Phe12，Nle21,38，CML27，Glu30，D-His32，Lys33] r / hCRF（12-41）和（环30-30） [D-Phe12，Nle21,38，Glu30，D-Arg32，Lys33] r / hCRF（12-41）。 标记的拮抗剂如（环30-30）[I125D-Tyr12，Nle21,38，Glu30，D-His32，Lys33] r / hCRF（12-41）可用于药物筛选测定。

公开(公告)号：US5844074A

公开(公告)日：1998-12-01

申请号：US575148

申请日：1995-12-19

申请人： Jean E. F. Rivier

发明人： Jean E. F. Rivier

IPC分类号： G01N33/15 ,  A61K38/00 ,  A61K38/04 ,  A61K45/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  C07K14/575 ,  G01N33/50 ,  G01N33/566 ,  G01N33/68 ,  G01N33/74 ,  A61K38/28 ,  A61K38/12 ,  C07K7/64 ,  C07K14/695

CPC分类号： G01N33/5008 ,  C07K14/57509 ,  G01N33/502 ,  G01N33/566 ,  G01N33/68 ,  G01N33/6842 ,  G01N33/74 ,  A61K38/00 ,  G01N2333/5751 ,  Y10S514/805 ,  Y10S930/26

摘要： Novel cyclic CRF agonist peptides have the amino acid sequence: (cyclo 30-33)Ac-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-R.sub.30 -Ala-R.sub.32 -R.sub.33 -Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH.sub.2 wherein R.sub.30 is Glu or Cys; R.sub.32 is His or a D-amino acid such as D-His, D-Arg or similar; R.sub.33 is Lys, Orn or Cys. The N-terminus may be extended by Ser-Glu-Glu. Lys may be substituted for Arg.sup.23, and its side chain connected by a lactam bridge to Glu.sup.20 to form a bicyclic peptide. Certain disclosed CRF agonists include: (cyclo 30-33)�Ac-Pro.sup.4, D-Phe.sup.12, Nle.sup.21,38, D-His.sup.32, Glu.sup.30, Lys.sup.33 !r/hCRF(4-41), (cyclo 30-33)�Ac-Pro.sup.4, D-Phe.sup.12, Nle.sup.21,38, D-His.sup.32, Glu.sup.30, Orn.sup.33 !r/hCRF(4-41), (cyclo 30-33)�Ac-Pro.sup.4, D-Phe.sup.12, Nle.sup.21,38, Cys.sup.30,33, D-His.sup.32 !r/hCRF(4-41), (bicyclo 20-23,30-33)�Ac-Pro.sup.4, D-Phe.sup.12, Nle.sup.21,38, Lys.sup.23,33, Glu.sup.30, D-His.sup.32 !-r/hCRF(4-41), (cyclo 30-33)�Ac-Pro.sup.4, D-Phe.sup.12, Nle.sup.21,38, CML.sup.27, Glu.sup.30, imBzlD-His.sup.32, Lys.sup.33 !r/hCRF(4-41) and (cyclo 30-33)�Ac-Pro.sup.4, D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, D-Arg.sup.32, Lys.sup.33 !r/hCRF(4-41). Labelled agonists such as (cyclo 30-33)�I.sup.125 Tyr.sup.o, D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, D-His.sup.32, Lys.sup.33 !r/hCRF and (cyclo 30-33)�I.sup.125 D-Tyr.sup.3, D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, D-His.sup.32, Lys.sup.33 !r/hCRF(3-41) are useful in screening for more potent agonists.

摘要翻译： 新型循环CRF激动剂肽具有氨基酸序列：（环30-33）Ac-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val -Leu-Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-R30-Ala-R32-R33-Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH2 是Glu或Cys; R32是His或D-氨基酸，例如D-His，D-Arg或类似物; R33是Lys，Orn或Cys。 N末端可以被Ser-Glu-Glu延伸。 Lys可以代替Arg23，其侧链通过内酰胺桥连接至Glu20以形成双环肽。 某些公开的CRF激动剂包括：（环30-33）[Ac-Pro4，D-Phe12，Nle21,38，D-H​​is32，Glu30，Lys33] r / hCRF（4-41），（环30-33）[Ac -Pro4，D-Phe12，Nle21,38，D-H​​is32，Glu30，Orn33] r / hCRF（4-41），（环30-33）[Ac-Pro4，D-Phe12，Nle21,38，Cys30,33 ，D-His32] r / hCRF（4-41），（双环20-23,30-33）[Ac-Pro4，D-Phe12，Nle21,38，Lys23,33，Glu30，D-His32] -r / hCRF（4-41），（环30-33）[Ac-Pro4，D-Phe12，Nle21,38，CML27，Glu30，imBzlD-His32，Lys33] r / hCRF（4-41）和（环30-33 ）[Ac-Pro4，D-Phe12，Nle21,38，Glu30，D-Arg32，Lys33] r / hCRF（4-41）。 标记的激动剂如（环30-33）[I125Tyro，D-Phe12，Nle21,38，Glu30，D-His32，Lys33] r / hCRF和（环30-33）[I125D-Tyr3，D-Phe12，Nle21， 38，Glu30，D-His32，Lys33] r / hCRF（3-41）可用于筛选更有效的激动剂。

公开(公告)号：US5530095A

公开(公告)日：1996-06-25

申请号：US447613

申请日：1995-05-23

申请人： Joan Vaughn ,  Wolfgang H. Fischer ,  Jean E. F. Rivier ,  Jean-Louis M. Nahon ,  Francoise G. Presse ,  Wylie W. Vale, Jr.

发明人： Joan Vaughn ,  Wolfgang H. Fischer ,  Jean E. F. Rivier ,  Jean-Louis M. Nahon ,  Francoise G. Presse ,  Wylie W. Vale, Jr.

IPC分类号： C12N15/09 ,  A61K38/00 ,  A61K38/04 ,  A61P35/00 ,  C07K7/06 ,  C07K7/08 ,  C07K7/64 ,  C07K14/00 ,  C07K14/575 ,  C12N15/12 ,  C12N15/16 ,  C12P21/02

CPC分类号： C07K7/08 ,  C07K7/64 ,  A61K38/00 ,  Y10S530/827 ,  Y10S530/854

摘要： Mammalian melanin-concentrating hormone (MCH) is isolated from rat tissue, purified and characterized. These MCH peptides are useful for treating skin disorders, for suppressing the proliferation of skin tumor cells, such as melanomas in mammals, and for modulating the secretion of ACTH. Generally, peptides are provided which have the following formula: ##STR1## or which are naturally occurring homologs of the peptide with said formula. The peptides which are the naturally occurring MCH homologs of mammalian species other than rat can also be obtained using the materials disclosed, as demonstrated specifically with human MCH, which is found to have the same structure as rat MCH. Also disclosed are the amino acid sequences of, and the nucleotide sequences of the cDNAs which encode, the putative precursors of rat MCH and human MCH. These precursors may also include one or more biologically active peptides N-terminally of the mature MCH's. Among these peptides, which are thought to be formed from the MCH precursors, are the peptide with the sequence H-Glu-Ile-Gly-Asp-Glu-Glu-Asn-Ser-Ala-Lys-Phe-Pro-Ile-NH.sub.2, which is cross-reactive with antibodies against alpha-MSH and CRF, and the peptide with the sequence H-Gly-X.sub.NGE -Phe-Pro-Ala-Glu-Asn-Gly-Val-Gln-Asn-Thr-Glu-Ser-Thr-Gln-Glu-OH, wherein X.sub.NGE is Pro-Ala-Val or Ser-Val-Ala, which is cross-reactive with antibodies against GRF.

摘要翻译： 从大鼠组织中分离哺乳动物黑色素浓缩激素（MCH），进行纯化和表征。 这些MCH肽可用于治疗皮肤病症，抑制皮肤肿瘤细胞增殖，如哺乳动物的黑素瘤，以及调节ACTH的分泌。 通常，提供具有下式的肽：＆lt; IMAGE＆gt;或具有所述式的肽的天然存在同系物。 作为除大鼠之外的哺乳动物物种的天然存在的MCH同源物的肽也可以使用公开的材料获得，如用人MCH特异性证实的，其被发现具有与大鼠MCH相同的结构。 还公开了编码大鼠MCH和人MCH的推定前体的cDNA的氨基酸序列和cDNA的核苷酸序列。 这些前体还可以包括成熟MCH的N-末端的一种或多种生物活性肽。 在这些被认为由MCH前体形成的肽中，具有序列H-Glu-Ile-Gly-Asp-Glu-Glu-Asn-Ser-Ala-Lys-Phe-Pro-Ile-NH 2的肽 ，其与抗α-MSH和CRF的抗体具有交叉反应性，并且具有序列H-Gly-XNGE-Phe-Pro-Ala-Glu-Asn-Gly-Val-Gln-Asn-Thr-Glu-Ser -Thr-Gln-Glu-OH，其中XNGE是Pro-Ala-Val或Ser-Val-Ala，其与抗GRF的抗体交叉反应。

公开(公告)号：US5432155A

公开(公告)日：1995-07-11

申请号：US84848

申请日：1993-06-29

申请人： Baldomero M. Olivera ,  Jean E. F. Rivier ,  Lourdes J. Cruz ,  Fe Abogadie ,  Chris E. Hopkins ,  John Dykert ,  Josep L. Torres

发明人： Baldomero M. Olivera ,  Jean E. F. Rivier ,  Lourdes J. Cruz ,  Fe Abogadie ,  Chris E. Hopkins ,  John Dykert ,  Josep L. Torres

IPC分类号： A61K38/00 ,  A61K39/00 ,  A61P21/00 ,  C07K14/435 ,  C12N15/12 ,  C07K7/08 ,  A61K38/10 ,  A61K38/17

CPC分类号： C07K14/43504 ,  C07K14/435 ,  A61K38/00 ,  A61K39/00

摘要： Substantially pure conotoxins are provided which inhibit synaptic transmissions at the neuromuscular junctions and which are useful both in vivo and in assays because they specifically target particular receptors, such as the acetylcholine receptor, and ion channels. The peptides are of such length that they can be made by chemical synthesis. They also may be made using recombinant DNA techniques, and the DNA encoding such conotoxins having pesticidal properties can be incorporated as plant defense genes into plant species of interest.

摘要翻译： 提供基本上纯的芋螺毒素，其抑制神经肌肉接头处的突触传递，并且其在体内和分析中都是有用的，因为它们特异性靶向特定受体，例如乙酰胆碱受体和离子通道。 肽的长度可以通过化学合成制成。 它们也可以使用重组DNA技术制备，并且编码具有杀虫性质的这种芋螺毒素的DNA可以作为植物防御基因并入感兴趣的植物物种中。

公开(公告)号：US5328899A

公开(公告)日：1994-07-12

申请号：US882923

申请日：1992-05-12

申请人： Jaroslav H. Boublik ,  Jean E. F. Rivier ,  Marvin R. Brown ,  Neal A. Scott

发明人： Jaroslav H. Boublik ,  Jean E. F. Rivier ,  Marvin R. Brown ,  Neal A. Scott

IPC分类号： A61K38/00 ,  C07K14/575 ,  A61K37/02 ,  C07K7/08 ,  C07K7/10

CPC分类号： C07K14/57545 ,  A61K38/00

摘要： Human Neuropeptide Y (NPY) has the formula: H-Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala-Pro- Ala-Glu-Asp-Met-Ala-Arg-Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu-Ile- Thr-Arg-Gln-Arg -Tyr-NH.sub.2. Porcine and rat NPY have the same sequence except for Leu instead of Met in the 17-position. Porcine PYY is homologous having 11 different residues. NPY analogs and N-terminally-shortened fragments, e.g. NPY(18-36), which contain one or more specific D-isomer substitutions for the naturally occurring residues (as well as pharmaceutically acceptable salts thereof), dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals, including humans, to substantially lower blood pressure over an extended period of time or to counteract hypertension.

摘要翻译： 人神经肽Y（NPY）具有下式：H-Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala-Pro-Ala-Glu-Asp-Met-Ala-Arg- Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu-Ile-Thr-Arg-Gln-Arg-Tyr-NH2。 猪和大鼠NPY具有相同的序列，除了Leu而不是17位的Met。 猪PYY具有11个不同残基的同源物。 NPY类似物和N-末端缩短的片段，例如 对于分散在药学上可接受的液体或固体载体中的天然存在的残基（以及其药学上可接受的盐）含有一个或多个特异性D-异构体取代的NPY（18-36）可以施用于包括人在内的哺乳动物 ，以在更长的时间内大幅降低血压或抵抗高血压。