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  1. Article ; Online: Publisher Correction: Structural basis of GABA reuptake inhibition.

    Motiwala, Zenia / Aduri, Nanda Gowtham / Shaye, Hamidreza / Han, Gye Won / Lam, Jordy Homing / Katritch, Vsevolod / Cherezov, Vadim / Gati, Cornelius

    Nature

    2022  Volume 608, Issue 7921, Page(s) E15

    Language English
    Publishing date 2022-07-15
    Publishing country England
    Document type Published Erratum
    ZDB-ID 120714-3
    ISSN 1476-4687 ; 0028-0836
    ISSN (online) 1476-4687
    ISSN 0028-0836
    DOI 10.1038/s41586-022-05080-7
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  2. Article ; Online: Structural basis of GABA reuptake inhibition.

    Motiwala, Zenia / Aduri, Nanda Gowtham / Shaye, Hamidreza / Han, Gye Won / Lam, Jordy Homing / Katritch, Vsevolod / Cherezov, Vadim / Gati, Cornelius

    Nature

    2022  Volume 606, Issue 7915, Page(s) 820–826

    Abstract: γ-Aminobutyric acid (GABA) transporter 1 (GAT1) ...

    Abstract γ-Aminobutyric acid (GABA) transporter 1 (GAT1)
    MeSH term(s) Anticonvulsants/chemistry ; Anticonvulsants/pharmacology ; Cryoelectron Microscopy ; GABA Plasma Membrane Transport Proteins/chemistry ; GABA Plasma Membrane Transport Proteins/metabolism ; GABA Plasma Membrane Transport Proteins/ultrastructure ; GABA Uptake Inhibitors/chemistry ; GABA Uptake Inhibitors/pharmacology ; Humans ; Neurotransmitter Agents/metabolism ; Protein Conformation/drug effects ; Tiagabine/chemistry ; Tiagabine/metabolism ; Tiagabine/pharmacology ; gamma-Aminobutyric Acid/metabolism
    Chemical Substances Anticonvulsants ; GABA Plasma Membrane Transport Proteins ; GABA Uptake Inhibitors ; Neurotransmitter Agents ; SLC6A1 protein, human ; gamma-Aminobutyric Acid (56-12-2) ; Tiagabine (Z80I64HMNP)
    Language English
    Publishing date 2022-06-08
    Publishing country England
    Document type Journal Article
    ZDB-ID 120714-3
    ISSN 1476-4687 ; 0028-0836
    ISSN (online) 1476-4687
    ISSN 0028-0836
    DOI 10.1038/s41586-022-04814-x
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Novel Cocrystal Structures of Peptide Antagonists Bound to the Human Melanocortin Receptor 4 Unveil Unexplored Grounds for Structure-Based Drug Design.

    Gimenez, Luis E / Martin, Charlotte / Yu, Jing / Hollanders, Charlie / Hernandez, Ciria C / Wu, Yiran / Yao, Deqiang / Han, Gye Won / Dahir, Naima S / Wu, Lijie / Van der Poorten, Olivier / Lamouroux, Arthur / Mannes, Morgane / Zhao, Suwen / Tourwé, Dirk / Stevens, Raymond C / Cone, Roger D / Ballet, Steven

    Journal of medicinal chemistry

    2024  Volume 67, Issue 4, Page(s) 2690–2711

    Abstract: Melanocortin 4 receptor (MC4-R) antagonists are actively sought for treating cancer cachexia. We determined the structures of complexes ... ...

    Abstract Melanocortin 4 receptor (MC4-R) antagonists are actively sought for treating cancer cachexia. We determined the structures of complexes with
    MeSH term(s) Humans ; Receptor, Melanocortin, Type 4 ; Peptides/pharmacology ; Ligands ; Drug Design ; Receptor, Melanocortin, Type 3 ; Receptors, Melanocortin
    Chemical Substances Receptor, Melanocortin, Type 4 ; Peptides ; Ligands ; Receptor, Melanocortin, Type 3 ; Receptors, Melanocortin
    Language English
    Publishing date 2024-02-12
    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/acs.jmedchem.3c01822
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: A Single Reactive Noncanonical Amino Acid is Able to Dramatically Stabilize Protein Structure.

    Li, Jack C / Nasertorabi, Fariborz / Xuan, Weimin / Han, Gye Won / Stevens, Raymond C / Schultz, Peter G

    ACS chemical biology

    2020  Volume 15, Issue 10, Page(s) 2842

    Language English
    Publishing date 2020-10-02
    Publishing country United States
    Document type Published Erratum
    ISSN 1554-8937
    ISSN (online) 1554-8937
    DOI 10.1021/acschembio.0c00196
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article: The activation mechanism and antibody binding mode for orphan GPR20.

    Lin, Xi / Jiang, Shan / Wu, Yiran / Wei, Xiaohu / Han, Gye-Won / Wu, Lijie / Liu, Junlin / Chen, Bo / Zhang, Zhibin / Zhao, Suwen / Cherezov, Vadim / Xu, Fei

    Cell discovery

    2023  Volume 9, Issue 1, Page(s) 23

    Abstract: GPR20 is a class-A orphan G protein-coupled receptor (GPCR) and a potential therapeutic target for gastrointestinal stromal tumors (GIST) owing to its differentially high expression. An antibody-drug conjugate (ADC) containing a GPR20-binding antibody ( ... ...

    Abstract GPR20 is a class-A orphan G protein-coupled receptor (GPCR) and a potential therapeutic target for gastrointestinal stromal tumors (GIST) owing to its differentially high expression. An antibody-drug conjugate (ADC) containing a GPR20-binding antibody (Ab046) was recently developed in clinical trials for GIST treatment. GPR20 constitutively activates Gi proteins in the absence of any known ligand, but it remains obscure how this high basal activity is achieved. Here we report three cryo-EM structures of human GPR20 complexes including Gi-coupled GPR20 in the absence or presence of the Fab fragment of Ab046 and Gi-free GPR20. Remarkably, the structures demonstrate a uniquely folded N-terminal helix capping onto the transmembrane domain and our mutagenesis study suggests a key role of this cap region in stimulating the basal activity of GPR20. We also uncover the molecular interactions between GPR20 and Ab046, which may enable the design of tool antibodies with enhanced affinity or new functionality for GPR20. Furthermore, we report the orthosteric pocket occupied by an unassigned density which might be essential for exploring opportunities for deorphanization.
    Language English
    Publishing date 2023-02-28
    Publishing country England
    Document type Journal Article
    ISSN 2056-5968
    ISSN 2056-5968
    DOI 10.1038/s41421-023-00520-8
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: A Single Reactive Noncanonical Amino Acid Is Able to Dramatically Stabilize Protein Structure.

    Li, Jack C / Nastertorabi, Fariborz / Xuan, Weimin / Han, Gye Won / Stevens, Raymond C / Schultz, Peter G

    ACS chemical biology

    2019  Volume 14, Issue 6, Page(s) 1150–1153

    Abstract: A p-isothiocyanate phenylalanine mutant of the homodimeric protein homoserine o-succinyltransferase (MetA) was isolated in a temperature dependent selection from a library of metA mutants containing noncanonical amino acids. This mutant protein has a ... ...

    Abstract A p-isothiocyanate phenylalanine mutant of the homodimeric protein homoserine o-succinyltransferase (MetA) was isolated in a temperature dependent selection from a library of metA mutants containing noncanonical amino acids. This mutant protein has a dramatic increase of 24 °C in thermal stability compared to the wild type protein. Peptide mapping experiments revealed that the isothiocyanate group forms a thiourea cross-link to the N terminal proline of the other monomer, despite the two positions being >30 Å apart in the X-ray crystal structure of the wild type protein. These results show that an expanded set of building blocks beyond the canonical 20 amino acids can lead to significant changes in the properties of proteins.
    MeSH term(s) Crystallography, X-Ray ; Escherichia coli/enzymology ; Escherichia coli Proteins/chemistry ; Escherichia coli Proteins/genetics ; Homoserine O-Succinyltransferase/chemistry ; Homoserine O-Succinyltransferase/genetics ; Mutation ; Phenylalanine/chemistry ; Protein Conformation ; Protein Stability ; Temperature
    Chemical Substances Escherichia coli Proteins ; Phenylalanine (47E5O17Y3R) ; Homoserine O-Succinyltransferase (EC 2.3.1.46)
    Language English
    Publishing date 2019-06-04
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ISSN 1554-8937
    ISSN (online) 1554-8937
    DOI 10.1021/acschembio.9b00002
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article ; Online: High ligand efficiency quinazoline compounds as novel A

    Bolteau, Raphaël / Duroux, Romain / Laversin, Amélie / Vreulz, Brandon / Shiriaeva, Anna / Stauch, Benjamin / Han, Gye Won / Cherezov, Vadim / Renault, Nicolas / Barczyk, Amélie / Ravez, Séverine / Coevoet, Mathilde / Melnyk, Patricia / Liberelle, Maxime / Yous, Saïd

    European journal of medicinal chemistry

    2022  Volume 241, Page(s) 114620

    Abstract: The past fifty years have been marked by the surge of neurodegenerative diseases. Unfortunately, current treatments are only symptomatic. Hence, the search for new and innovative therapeutic targets for curative treatments becomes a major challenge. ... ...

    Abstract The past fifty years have been marked by the surge of neurodegenerative diseases. Unfortunately, current treatments are only symptomatic. Hence, the search for new and innovative therapeutic targets for curative treatments becomes a major challenge. Among these targets, the adenosine A
    MeSH term(s) Adenosine A2 Receptor Antagonists/chemistry ; Adenosine A2 Receptor Antagonists/pharmacology ; Ligands ; Molecular Docking Simulation ; Purinergic P1 Receptor Antagonists/pharmacology ; Quinazolines/pharmacology ; Receptor, Adenosine A2A/chemistry ; Structure-Activity Relationship
    Chemical Substances Adenosine A2 Receptor Antagonists ; Ligands ; Purinergic P1 Receptor Antagonists ; Quinazolines ; Receptor, Adenosine A2A
    Language English
    Publishing date 2022-07-22
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2022.114620
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article ; Online: An orthogonal seryl-tRNA synthetase/tRNA pair for noncanonical amino acid mutagenesis in Escherichia coli.

    Zambaldo, Claudio / Koh, Minseob / Nasertorabi, Fariborz / Han, Gye Won / Chatterjee, Abhishek / Stevens, Raymond C / Schultz, Peter G

    Bioorganic & medicinal chemistry

    2020  Volume 28, Issue 20, Page(s) 115662

    Abstract: We report the development of the orthogonal amber-suppressor pair Archaeoglobus fulgidus seryl-tRNA (Af- ... ...

    Abstract We report the development of the orthogonal amber-suppressor pair Archaeoglobus fulgidus seryl-tRNA (Af-tRNA
    MeSH term(s) Amino Acids/genetics ; Amino Acids/metabolism ; Archaeoglobus fulgidus/enzymology ; Escherichia coli/metabolism ; Methanosarcina/enzymology ; Protein Engineering ; RNA, Transfer/chemistry ; RNA, Transfer/metabolism ; Serine-tRNA Ligase/chemistry ; Serine-tRNA Ligase/metabolism
    Chemical Substances Amino Acids ; RNA, Transfer (9014-25-9) ; Serine-tRNA Ligase (EC 6.1.1.11)
    Language English
    Publishing date 2020-07-28
    Publishing country England
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 1161284-8
    ISSN 1464-3391 ; 0968-0896
    ISSN (online) 1464-3391
    ISSN 0968-0896
    DOI 10.1016/j.bmc.2020.115662
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  9. Article: Generation of an Orthogonal Protein–Protein Interface with a Noncanonical Amino Acid

    Koh, Minseob / Han Gye Won / Nasertorabi Fariborz / Schultz Peter G / Stevens Raymond C

    Journal of the American Chemical Society. 2017 Apr. 26, v. 139, no. 16

    2017  

    Abstract: We have engineered the protein interface of the Escherichia coli chorismate mutase (EcCM) homodimer to be dependent on incorporation of a noncanonical amino acid (ncAA) at residue 72. The large hydrophobic amino acid p-benzoyl phenylalanine (pBzF) was ... ...

    Abstract We have engineered the protein interface of the Escherichia coli chorismate mutase (EcCM) homodimer to be dependent on incorporation of a noncanonical amino acid (ncAA) at residue 72. The large hydrophobic amino acid p-benzoyl phenylalanine (pBzF) was substituted for Tyr72, which led to a catalytically inactive protein. A library of five residues (Leu25′, Arg29′, Leu76, Ile80′ and Asp83′) surrounding pBzF72 was generated and subjected to a growth based selection in a chorismate mutase deficient strain. An EcCM variant (Phe25′, pBzF72, Thr76, Gly80′ and Tyr83′) forms a stable homodimer, has catalytic activity similar to the wild type enzyme, and unfolds with a Tₘ of 53 °C. The X-ray crystal structure reveals a pi–pi stacking and hydrogen bonding interactions that stabilize the new protein interface. The strategy described here should be useful for generating organisms that are dependent on the presence of a ncAA for growth.
    Keywords catalytic activity ; chorismic acid ; Escherichia coli ; hydrogen bonding ; hydrophobicity ; phenylalanine ; protein-protein interactions ; X-ray diffraction
    Language English
    Dates of publication 2017-0426
    Size p. 5728-5731.
    Publishing place American Chemical Society
    Document type Article
    ZDB-ID 3155-0
    ISSN 1520-5126 ; 0002-7863
    ISSN (online) 1520-5126
    ISSN 0002-7863
    DOI 10.1021%2Fjacs.7b02273
    Database NAL-Catalogue (AGRICOLA)

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  10. Article ; Online: GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A

    Shiriaeva, Anna / Park, Daejin / Kim, Gyudong / Lee, Yoonji / Hou, Xiyan / Jarhad, Dnyandev B / Kim, Gibae / Yu, Jinha / Hyun, Young Eum / Kim, Woomi / Gao, Zhan-Guo / Jacobson, Kenneth A / Han, Gye Won / Stevens, Raymond C / Jeong, Lak Shin / Choi, Sun / Cherezov, Vadim

    Journal of medicinal chemistry

    2022  Volume 65, Issue 17, Page(s) 11648–11657

    Abstract: Modulators of the G protein-coupled ... ...

    Abstract Modulators of the G protein-coupled A
    MeSH term(s) Adenosine A2 Receptor Antagonists/chemistry ; Adenosine A2 Receptor Antagonists/pharmacology ; Crystallography, X-Ray ; Molecular Conformation ; Nucleosides ; Receptor, Adenosine A2A/chemistry ; Thiophenes
    Chemical Substances Adenosine A2 Receptor Antagonists ; Nucleosides ; Receptor, Adenosine A2A ; Thiophenes
    Language English
    Publishing date 2022-08-17
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, Non-P.H.S. ; Research Support, N.I.H., Intramural
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.2c00462
    Database MEDical Literature Analysis and Retrieval System OnLINE

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