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    CYCLIC PEPTIDES
    1.
    发明申请
    CYCLIC PEPTIDES 有权
    循环肽

    公开(公告)号：US20070207502A1

    公开(公告)日：2007-09-06

    申请号：US11670112

    申请日：2007-02-01

    申请人： Stephen Benkovic ,  Charles Scott ,  Ernesto Abel-Santos

    发明人： Stephen Benkovic ,  Charles Scott ,  Ernesto Abel-Santos

    IPC分类号： C40B30/06 ,  C40B40/08 ,  C40B40/10 ,  C07K14/005 ,  C07K14/47 ,  C07K14/195

    CPC分类号： C12N15/10 ,  C07K7/52 ,  C07K7/64 ,  C12N15/1055 ,  G01N2500/00

    摘要： Methods of producing cyclic peptides and splicing intermediates of peptides in a looped conformation are disclosed. The methods utilize the trans-splicing ability of split inteins to catalyze cyclization of peptides from a precursor peptide having a target peptide interposed between two portions of a split intein. The interaction of the two portions of the split intein creates a catalytically-active intein and also forces the target peptide into a loop configuration that stabilizes the ester isomer of the amino acid at the junction between one of the intein portions and the target peptide. A heteroatom from the other intein portion then reacts with the ester to form a cyclic ester intermediate. The active intein catalyzes the formation of an aminosuccinimide that liberates a cyclized form of the target peptide, which spontaneously rearranges to form the thermodynamically favored backbone cyclic peptide product. Also disclosed are nucleic acid molecules, polypeptides, methods for making cyclic peptides, methods of making libraries, and methods of screening peptides.

    摘要翻译： 公开了以循环构象形成肽的环肽和剪接中间体的方法。 所述方法利用分裂内蛋白的转拼能力来催化来自前导肽的肽的环化，所述肽的前导肽插入分裂的内含肽的两部分之间。 分裂内含肽的两部分的相互作用产生催化活性内含肽，并且还将目标肽强制成使得在内含肽部分和目标肽之间的连接处稳定氨基酸的酯异构体的环构型。 来自另一个内含肽部分的杂原子然后与酯反应以形成环状酯中间体。 活性内含肽催化氨基琥珀酰亚胺的形成，其释放环化形式的靶肽，其自发重排以形成热力学上有利的主链环肽产物。 还公开了核酸分子，多肽，制备环肽的方法，制备文库的方法和筛选肽的方法。

    Boronic and borinic acid compound as inhibitors of sulfenic acid-containing proteins
    2.
    发明授权
    Boronic and borinic acid compound as inhibitors of sulfenic acid-containing proteins 有权
    硼酸和硼酸化合物作为含亚磺酸蛋白质的抑制剂

    公开(公告)号：US09309508B2

    公开(公告)日：2016-04-12

    申请号：US14576613

    申请日：2014-12-19

    申请人： Stephen Benkovic ,  Chunyu Liu ,  John W. Tomsho

    发明人： Stephen Benkovic ,  Chunyu Liu ,  John W. Tomsho

    IPC分类号： C12N9/99 ,  C12N9/88

    CPC分类号： C12N9/99 ,  C12N9/88 ,  C12Y402/01084

    摘要： A boronic or borinic acid compound is used to inhibit the activity of a sulfenic acid-containing protein. Thus, a biologically-active sulfenic acid-containing protein is contacted with an activity-inhibiting effective amount of a boronic or borinic acid compound of Formula I or a salt, hydrate or solvate thereof, whose components are disclosed within, and that contact is maintained for a time sufficient to inhibit the biological activity of the protein.

    摘要翻译： 使用硼酸或硼酸化合物抑制含亚磺酸的蛋白质的活性。 因此，含有生物活性的含亚磺酸的蛋白质与活性抑制有效量的式I的硼酸或硼酸化合物或其盐，水合物或溶剂合物接触，其组分在其中公开，并且保持接触 足以抑制蛋白质的生物活性。

    Antibody combining sites that exhibit amide or ester synthase activity
    9.
    发明授权
    Antibody combining sites that exhibit amide or ester synthase activity 失效
    表现出酰胺或酯合成酶活性的抗体结合位点

    公开(公告)号：US4900674A

    公开(公告)日：1990-02-13

    申请号：US55177

    申请日：1987-05-28

    申请人： Stephen Benkovic ,  Richard A. Lerner ,  Alfonso Tramontano ,  Andrew D. Napper

    发明人： Stephen Benkovic ,  Richard A. Lerner ,  Alfonso Tramontano ,  Andrew D. Napper

    IPC分类号： C12N9/00

    CPC分类号： C12N9/0002

    摘要： A phosphorous-containing analog-ligand having a conformation that substantially corresponds to the conformation of an amide- or ester-forming transition state is used to induce production of receptor molecules whose antibody combining sites have amide or ester synthase catalytic activity when reacted with a ligand containing (i) a carbonyl carbon atom and (ii) an amine or alcohol group that are structurally capable of forming a preselected carboxylic amide or ester bond.

    摘要翻译： 具有基本上对应于形成酰胺或酯形成过渡态的构象的构象的含磷类似物配体被用于诱导当与配体反应时其抗体结合位点具有酰胺或酯合成酶催化活性的受体分子的产生 含有（i）羰基碳原子和（ii）结构上能够形成预选择的羧酰胺或酯键的胺或醇基团。

    SYNERGISTIC BENZOXABOROLE-CONTAINING ANTI-FUNGICIDAL COMPOSITION
    10.
    发明申请
    SYNERGISTIC BENZOXABOROLE-CONTAINING ANTI-FUNGICIDAL COMPOSITION 有权
    合成含苯甲酸的抗真菌组合物

    公开(公告)号：US20160324160A1

    公开(公告)日：2016-11-10

    申请号：US15093331

    申请日：2016-04-07

    申请人： Stephen Benkovic ,  Chunyu Liu

    发明人： Stephen Benkovic ,  Chunyu Liu

    IPC分类号： A01N55/08 ,  A01N25/08 ,  A01N25/02

    CPC分类号： A01N55/08 ,  A01N25/02 ,  A01N25/08 ,  A01N61/00 ,  A61K31/69 ,  A01N2300/00

    摘要： An anti-fungal composition for the control of one or more target fungi (or a similar heterotrophic, hyphae-producing organism) that infect plant materials and are (is) separately controllable by a benzoxaborole and an anti-fungal compound of a preselected FRAC Target Site Code is disclosed, as is a method of its use. A composition contains a diluent medium having dissolved or dispersed therein a synergistic effective amount of each of a first and a second anti-fungal compound. The first anti-fungal compound is a benzoxaborole of Formula I. The second anti-fungal compound is other than a benzoxaborole and is known to control said one or more target species of fungus when utilized as the sole anti-fungal compound at a concentration greater than the synergistic effective amount and has a preselected FRAC Target Site Code of B, C, D, E, G, H, or M.

    摘要翻译： 用于控制感染植物材料的一种或多种目标真菌（或类似的异养，菌丝产生生物体）的抗真菌组合物，其可分别由预选的FRAC靶标的苯并恶唑和抗真菌化合物控制 公开了现场代码，以及其使用方法。 组合物含有溶解或分散有协同有效量的第一和第二抗真菌化合物的稀释介质。 第一种抗真菌化合物是式I的苯并恶唑。第二种抗真菌化合物是除苯并恶唑之外的化合物，当用作唯一的抗真菌化合物时，已知可以控制所述一种或多种目标物种的真菌浓度 具有协同有效量，并具有B，C，D，E，G，H或M的预先选定的FRAC目标位点代码。