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  1. Article ; Online: A Selection of Macrocyclic Peptides That Bind STING From an mRNA-Display Library With Split Degenerate Codons.

    Lin, Chi-Wang / Harner, Mary J / Douglas, Andrew E / Lafont, Virginie / Yu, Fei / Lee, Ving G / Poss, Michael A / Swain, Joanna F / Wright, Martin / Lipovšek, Daša

    Angewandte Chemie (International ed. in English)

    2021  Volume 60, Issue 42, Page(s) 22640–22645

    Abstract: Recent improvements in mRNA display have enabled the selection of peptides that incorporate non-natural amino acids, thus expanding the chemical diversity of macrocycles beyond what is accessible in nature. Such libraries have incorporated non-natural ... ...

    Abstract Recent improvements in mRNA display have enabled the selection of peptides that incorporate non-natural amino acids, thus expanding the chemical diversity of macrocycles beyond what is accessible in nature. Such libraries have incorporated non-natural amino acids at the expense of natural amino acids by reassigning their codons. Here we report an alternative approach to expanded amino-acid diversity that preserves all 19 natural amino acids (no methionine) and adds 6 non-natural amino acids, resulting in the highest sequence complexity reported to date. We have applied mRNA display to this 25-letter library to select functional macrocycles that bind human STING, a protein involved in immunoregulation. The resulting STING-binding peptides include a 9-mer macrocycle with a dissociation constant (K
    MeSH term(s) Amino Acid Sequence ; Amino Acids/chemistry ; Codon ; Cyclic AMP/chemistry ; Cyclic AMP/metabolism ; Cyclic GMP/chemistry ; Cyclic GMP/metabolism ; Dimerization ; Genetic Engineering ; Humans ; Kinetics ; Membrane Proteins/chemistry ; Membrane Proteins/metabolism ; Peptide Library ; Peptides, Cyclic/chemistry ; Peptides, Cyclic/metabolism ; RNA, Messenger/genetics ; RNA, Messenger/metabolism
    Chemical Substances Amino Acids ; Codon ; Membrane Proteins ; Peptide Library ; Peptides, Cyclic ; RNA, Messenger ; STING1 protein, human ; Cyclic AMP (E0399OZS9N) ; Cyclic GMP (H2D2X058MU)
    Language English
    Publishing date 2021-09-06
    Publishing country Germany
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.202103043
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Identification of potent 11mer glucagon-like peptide-1 receptor agonist peptides with novel C-terminal amino acids: Homohomophenylalanine analogs.

    Haque, Tasir S / Lee, Ving G / Riexinger, Douglas / Lei, Ming / Malmstrom, Sarah / Xin, Li / Han, Songping / Mapelli, Claudio / Cooper, Christopher B / Zhang, Ge / Ewing, William R / Krupinski, John

    Peptides

    2010  Volume 31, Issue 5, Page(s) 950–955

    Abstract: We report the identification of potent agonists of the Glucagon-Like Peptide-1 Receptor (GLP-1R). These compounds are short, 11 amino acid peptides containing several unnatural amino acids, including (in particular) analogs of homohomophenylalanine ( ... ...

    Abstract We report the identification of potent agonists of the Glucagon-Like Peptide-1 Receptor (GLP-1R). These compounds are short, 11 amino acid peptides containing several unnatural amino acids, including (in particular) analogs of homohomophenylalanine (hhPhe) at the C-terminal position. Typically the functional activity of the more potent peptides in this class is in the low picomolar range in an in vitro cAMP assay, with one example demonstrating excellent in vivo activity in an ob/ob mouse model of diabetes.
    MeSH term(s) Amino Acid Sequence ; Aminobutyrates/chemistry ; Animals ; Blood Glucose/drug effects ; CHO Cells ; Cricetinae ; Cricetulus ; Glucagon-Like Peptide-1 Receptor ; Hyperglycemia/blood ; Hyperglycemia/drug therapy ; Mice ; Molecular Sequence Data ; Molecular Structure ; Peptides/chemical synthesis ; Peptides/chemistry ; Peptides/pharmacokinetics ; Peptides/therapeutic use ; Receptors, Glucagon/agonists
    Chemical Substances Aminobutyrates ; Blood Glucose ; Glp1r protein, mouse ; Glucagon-Like Peptide-1 Receptor ; Peptides ; Receptors, Glucagon ; 2-amino-4-phenylbutyric acid (7636-28-4)
    Language English
    Publishing date 2010-05
    Publishing country United States
    Document type Journal Article
    ZDB-ID 769028-9
    ISSN 1873-5169 ; 0196-9781
    ISSN (online) 1873-5169
    ISSN 0196-9781
    DOI 10.1016/j.peptides.2010.01.008
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 1649: Show issues Location:
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  3. Article ; Online: Exploration of structure-activity relationships at the two C-terminal residues of potent 11mer Glucagon-Like Peptide-1 receptor agonist peptides via parallel synthesis.

    Haque, Tasir S / Martinez, Rogelio L / Lee, Ving G / Riexinger, Douglas G / Lei, Ming / Feng, Ming / Koplowitz, Barry / Mapelli, Claudio / Cooper, Christopher B / Zhang, Ge / Huang, Christine / Ewing, William R / Krupinski, John

    Peptides

    2010  Volume 31, Issue 7, Page(s) 1353–1360

    Abstract: We report the identification of potent agonists of the Glucagon-Like Peptide-1 receptor (GLP-1R) via evaluation of two positional scanning libraries and a two-dimensional focused library, synthesized in part on SynPhase Lanterns. These compounds are 11 ... ...

    Abstract We report the identification of potent agonists of the Glucagon-Like Peptide-1 receptor (GLP-1R) via evaluation of two positional scanning libraries and a two-dimensional focused library, synthesized in part on SynPhase Lanterns. These compounds are 11 amino acid peptides containing several unnatural amino acids, including (in particular) analogs of biphenylalanine (Bip) at the two C-terminal positions. Typical activities of the most potent peptides in this class are in the picomolar range in an in vitro functional assay using human GLP-1 receptor.
    MeSH term(s) Amino Acid Sequence ; Animals ; CHO Cells ; Cricetinae ; Cricetulus ; Dogs ; Glucagon-Like Peptide-1 Receptor ; Humans ; Models, Molecular ; Molecular Sequence Data ; Peptide Library ; Peptides/chemistry ; Peptides/metabolism ; Peptides/pharmacology ; Receptors, Glucagon/agonists ; Structure-Activity Relationship
    Chemical Substances GLP1R protein, human ; Glucagon-Like Peptide-1 Receptor ; Peptide Library ; Peptides ; Receptors, Glucagon
    Language English
    Publishing date 2010-07
    Publishing country United States
    Document type Journal Article
    ZDB-ID 769028-9
    ISSN 1873-5169 ; 0196-9781
    ISSN (online) 1873-5169
    ISSN 0196-9781
    DOI 10.1016/j.peptides.2010.04.013
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article: An inhibitor binding pocket distinct from the catalytic active site on human beta-APP cleaving enzyme.

    Kornacker, Michael G / Lai, Zhihong / Witmer, Mark / Ma, Jianghong / Hendrick, Joseph / Lee, Ving G / Riexinger, Douglas J / Mapelli, Claudio / Metzler, William / Copeland, Robert A

    Biochemistry

    2005  Volume 44, Issue 34, Page(s) 11567–11573

    Abstract: Beta-APP cleaving enzyme (BACE) is responsible for the first of two proteolytic cleavages of the APP protein that together lead to the generation of the Alzheimer's disease-associated Abeta peptide. It is widely believed that halting the production of ... ...

    Abstract Beta-APP cleaving enzyme (BACE) is responsible for the first of two proteolytic cleavages of the APP protein that together lead to the generation of the Alzheimer's disease-associated Abeta peptide. It is widely believed that halting the production of Abeta peptide, by inhibition of BACE, is an attractive therapeutic modality for the treatment of Alzheimer's disease. BACE is an aspartyl protease, and there is significant effort in the pharmaceutical community to apply traditional design methods to the development of active site-directed inhibitors of this enzyme. We report here the discovery of a ligand binding pocket within the catalytic domain of BACE that is distinct from the enzymatic active site (i.e., an exosite). Peptides, initially identified from combinatorial phage peptide libraries, contain the sequence YPYF(I/L)P(L/I) and bind specifically to this exosite, even in the presence of saturating concentrations of active site-directed inhibitors. Binding of peptides to the BACE exosite leads to a concentration-dependent inhibition of proteolysis for APP-related, protein-based substrates of BACE. The discovery of this exosite opens new opportunities for the identification and development of novel and potentially selective small molecule inhibitors of BACE that act through exosite, rather than active site, binding interactions.
    MeSH term(s) Amino Acid Sequence ; Amyloid Precursor Protein Secretases ; Aspartic Acid Endopeptidases/chemistry ; Aspartic Acid Endopeptidases/metabolism ; Binding Sites ; Binding, Competitive ; Catalytic Domain ; Endopeptidases ; Fluorescence Polarization ; Humans ; Kinetics ; Peptide Fragments/chemistry
    Chemical Substances Peptide Fragments ; Amyloid Precursor Protein Secretases (EC 3.4.-) ; Endopeptidases (EC 3.4.-) ; Aspartic Acid Endopeptidases (EC 3.4.23.-) ; BACE1 protein, human (EC 3.4.23.46)
    Language English
    Publishing date 2005-08-30
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1108-3
    ISSN 1520-4995 ; 0006-2960
    ISSN (online) 1520-4995
    ISSN 0006-2960
    DOI 10.1021/bi050932l
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 217: Show issues Location:
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  5. Article ; Online: Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity.

    Mapelli, Claudio / Natarajan, Sesha I / Meyer, Jean-Philippe / Bastos, Margarita M / Bernatowicz, Michael S / Lee, Ving G / Pluscec, Jelka / Riexinger, Douglas J / Sieber-McMaster, Ellen S / Constantine, Keith L / Smith-Monroy, Constance A / Golla, Rajasree / Ma, Zhengping / Longhi, Daniel A / Shi, Dan / Xin, Li / Taylor, Joseph R / Koplowitz, Barry / Chi, Cecilia L /
    Khanna, Ashish / Robinson, Gordon W / Seethala, Ramakrishna / Antal-Zimanyi, Ildiko A / Stoffel, Robert H / Han, Songping / Whaley, Jean M / Huang, Christine S / Krupinski, John / Ewing, William R

    Journal of medicinal chemistry

    2009  Volume 52, Issue 23, Page(s) 7788–7799

    Abstract: Glucagon-like peptide 1 (GLP-1) is a 30 or 31 amino acid peptide hormone that contributes to the physiological regulation of glucose homeostasis and food intake. Herein, we report the discovery of a novel class of 11 amino acid GLP-1 receptor agonists. ... ...

    Abstract Glucagon-like peptide 1 (GLP-1) is a 30 or 31 amino acid peptide hormone that contributes to the physiological regulation of glucose homeostasis and food intake. Herein, we report the discovery of a novel class of 11 amino acid GLP-1 receptor agonists. These peptides consist of a structurally optimized 9-mer, which is closely related to the N-terminal 9 amino acids of GLP-1, linked to a substituted C-terminal biphenylalanine (BIP) dipeptide. SAR studies resulted in 11-mer GLP-1R agonists with similar in vitro potency to the native 30-mer. Peptides 21 and 22 acutely reduced plasma glucose excursions and increased plasma insulin concentrations in a mouse model of diabetes. These peptides also showed sustained exposures over several hours in mouse and dog models. The described 11-mer GLP-1 receptor agonists represent a new tool in further understanding GLP-1 receptor pharmacology that may lead to novel antidiabetic agents.
    MeSH term(s) Amino Acid Sequence ; Animals ; CHO Cells ; Cricetinae ; Cricetulus ; Dogs ; Dose-Response Relationship, Drug ; Glucagon-Like Peptide-1 Receptor ; Humans ; Hypoglycemic Agents/chemical synthesis ; Hypoglycemic Agents/chemistry ; Hypoglycemic Agents/pharmacokinetics ; Hypoglycemic Agents/pharmacology ; Male ; Mice ; Models, Molecular ; Molecular Sequence Data ; Oligopeptides/chemical synthesis ; Oligopeptides/chemistry ; Oligopeptides/pharmacokinetics ; Oligopeptides/pharmacology ; Protein Conformation ; Receptors, Glucagon/agonists
    Chemical Substances GLP1R protein, human ; Glp1r protein, mouse ; Glucagon-Like Peptide-1 Receptor ; Hypoglycemic Agents ; Oligopeptides ; Receptors, Glucagon
    Language English
    Publishing date 2009-12-10
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/jm900752a
    Database MEDical Literature Analysis and Retrieval System OnLINE

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