Application of encoded library technology (ELT) to a protein–protein interaction target: Discovery of a potent class of integrin lymphocyte function-associated antigen 1 (LFA-1) antagonists
Encoded library technology (ELT) was utilized to identify a class of compounds that disrupt the interaction between lymphocyte function-associated antigen-1 (LFA-1) and its ligand intercellular adhesion molecule-1 (ICAM-1) at submicromolar potency in both ELISA and cell adhesion assays. The inhibiti...
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Published in | Bioorganic & medicinal chemistry Vol. 22; no. 7; pp. 2353 - 2365 |
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Main Authors | , , , , , , , , , , , , , , |
Format | Journal Article |
Language | English |
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01.04.2014
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Abstract | Encoded library technology (ELT) was utilized to identify a class of compounds that disrupt the interaction between lymphocyte function-associated antigen-1 (LFA-1) and its ligand intercellular adhesion molecule-1 (ICAM-1) at submicromolar potency in both ELISA and cell adhesion assays.
The inhibition of protein–protein interactions remains a challenge for traditional small molecule drug discovery. Here we describe the use of DNA-encoded library technology for the discovery of small molecules that are potent inhibitors of the interaction between lymphocyte function-associated antigen 1 and its ligand intercellular adhesion molecule 1. A DNA-encoded library with a potential complexity of 4.1 billion compounds was exposed to the I-domain of the target protein and the bound ligands were affinity selected, yielding an enriched small-molecule hit family. Compounds representing this family were synthesized without their DNA encoding moiety and found to inhibit the lymphocyte function-associated antigen 1/intercellular adhesion molecule-1 interaction with submicromolar potency in both ELISA and cell adhesion assays. Re-synthesized compounds conjugated to DNA or a fluorophore were demonstrated to bind to cells expressing the target protein. |
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AbstractList | The inhibition of protein-protein interactions remains a challenge for traditional small molecule drug discovery. Here we describe the use of DNA-encoded library technology for the discovery of small molecules that are potent inhibitors of the interaction between lymphocyte function-associated antigen 1 and its ligand intercellular adhesion molecule 1. A DNA-encoded library with a potential complexity of 4.1 billion compounds was exposed to the I-domain of the target protein and the bound ligands were affinity selected, yielding an enriched small-molecule hit family. Compounds representing this family were synthesized without their DNA encoding moiety and found to inhibit the lymphocyte function-associated antigen 1/intercellular adhesion molecule-1 interaction with submicromolar potency in both ELISA and cell adhesion assays. Re-synthesized compounds conjugated to DNA or a fluorophore were demonstrated to bind to cells expressing the target protein. The inhibition of protein-protein interactions remains a challenge for traditional small molecule drug discovery. Here we describe the use of DNA-encoded library technology for the discovery of small molecules that are potent inhibitors of the interaction between lymphocyte function-associated antigen 1 and its ligand intercellular adhesion molecule 1. A DNA-encoded library with a potential complexity of 4.1 billion compounds was exposed to the I-domain of the target protein and the bound ligands were affinity selected, yielding an enriched small-molecule hit family. Compounds representing this family were synthesized without their DNA encoding moiety and found to inhibit the lymphocyte function-associated antigen 1/intercellular adhesion molecule-1 interaction with submicromolar potency in both ELISA and cell adhesion assays. Re-synthesized compounds conjugated to DNA or a fluorophore were demonstrated to bind to cells expressing the target protein. (c) 2014 Elsevier Ltd. All rights reserved. Encoded library technology (ELT) was utilized to identify a class of compounds that disrupt the interaction between lymphocyte function-associated antigen-1 (LFA-1) and its ligand intercellular adhesion molecule-1 (ICAM-1) at submicromolar potency in both ELISA and cell adhesion assays. The inhibition of protein–protein interactions remains a challenge for traditional small molecule drug discovery. Here we describe the use of DNA-encoded library technology for the discovery of small molecules that are potent inhibitors of the interaction between lymphocyte function-associated antigen 1 and its ligand intercellular adhesion molecule 1. A DNA-encoded library with a potential complexity of 4.1 billion compounds was exposed to the I-domain of the target protein and the bound ligands were affinity selected, yielding an enriched small-molecule hit family. Compounds representing this family were synthesized without their DNA encoding moiety and found to inhibit the lymphocyte function-associated antigen 1/intercellular adhesion molecule-1 interaction with submicromolar potency in both ELISA and cell adhesion assays. Re-synthesized compounds conjugated to DNA or a fluorophore were demonstrated to bind to cells expressing the target protein. |
Author | Xie, Can Kollmann, Christopher S. Cuozzo, John W. Skinner, Steven R. Israel, David I. Shimaoka, Motomu Evindar, Ghotas Bai, Xiaopeng Lind, Kenneth E. Yang, Hongfang Tsai, Ching-Hsuan Springer, Timothy A. Morgan, Barry A. Yuki, Koichi Zhu, Zhengrong |
Author_xml | – sequence: 1 givenname: Christopher S. surname: Kollmann fullname: Kollmann, Christopher S. organization: GlaxoSmithKline, Platform Technology & Science, MDR Boston, 830 Winter Street, Waltham, MA 02451, USA – sequence: 2 givenname: Xiaopeng surname: Bai fullname: Bai, Xiaopeng organization: GlaxoSmithKline, Platform Technology & Science, MDR Boston, 830 Winter Street, Waltham, MA 02451, USA – sequence: 3 givenname: Ching-Hsuan surname: Tsai fullname: Tsai, Ching-Hsuan organization: GlaxoSmithKline, Platform Technology & Science, MDR Boston, 830 Winter Street, Waltham, MA 02451, USA – sequence: 4 givenname: Hongfang surname: Yang fullname: Yang, Hongfang organization: GlaxoSmithKline, Platform Technology & Science, MDR Boston, 830 Winter Street, Waltham, MA 02451, USA – sequence: 5 givenname: Kenneth E. surname: Lind fullname: Lind, Kenneth E. organization: GlaxoSmithKline, Platform Technology & Science, MDR Boston, 830 Winter Street, Waltham, MA 02451, USA – sequence: 6 givenname: Steven R. surname: Skinner fullname: Skinner, Steven R. organization: GlaxoSmithKline, Platform Technology & Science, MDR Boston, 830 Winter Street, Waltham, MA 02451, USA – sequence: 7 givenname: Zhengrong surname: Zhu fullname: Zhu, Zhengrong organization: GlaxoSmithKline, Platform Technology & Science, MDR Boston, 830 Winter Street, Waltham, MA 02451, USA – sequence: 8 givenname: David I. surname: Israel fullname: Israel, David I. organization: GlaxoSmithKline, Platform Technology & Science, MDR Boston, 830 Winter Street, Waltham, MA 02451, USA – sequence: 9 givenname: John W. surname: Cuozzo fullname: Cuozzo, John W. organization: GlaxoSmithKline, Platform Technology & Science, MDR Boston, 830 Winter Street, Waltham, MA 02451, USA – sequence: 10 givenname: Barry A. surname: Morgan fullname: Morgan, Barry A. organization: GlaxoSmithKline, Platform Technology & Science, MDR Boston, 830 Winter Street, Waltham, MA 02451, USA – sequence: 11 givenname: Koichi surname: Yuki fullname: Yuki, Koichi organization: Immune Disease Institute, Children’s Hospital Boston, Harvard Medical School, Program in Cellular and Molecular Medicine, Department of Biological Chemistry and Molecular Pharmacology, 3 Blackfan Circle, Rm. 3100, Boston, MA 02115, USA – sequence: 12 givenname: Can surname: Xie fullname: Xie, Can organization: Immune Disease Institute, Children’s Hospital Boston, Harvard Medical School, Program in Cellular and Molecular Medicine, Department of Biological Chemistry and Molecular Pharmacology, 3 Blackfan Circle, Rm. 3100, Boston, MA 02115, USA – sequence: 13 givenname: Timothy A. surname: Springer fullname: Springer, Timothy A. organization: Immune Disease Institute, Children’s Hospital Boston, Harvard Medical School, Program in Cellular and Molecular Medicine, Department of Biological Chemistry and Molecular Pharmacology, 3 Blackfan Circle, Rm. 3100, Boston, MA 02115, USA – sequence: 14 givenname: Motomu surname: Shimaoka fullname: Shimaoka, Motomu organization: Immune Disease Institute, Children’s Hospital Boston, Harvard Medical School, Program in Cellular and Molecular Medicine, Department of Biological Chemistry and Molecular Pharmacology, 3 Blackfan Circle, Rm. 3100, Boston, MA 02115, USA – sequence: 15 givenname: Ghotas surname: Evindar fullname: Evindar, Ghotas email: ghotas.x.evindar@gsk.com organization: GlaxoSmithKline, Platform Technology & Science, MDR Boston, 830 Winter Street, Waltham, MA 02451, USA |
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Keywords | Affinity-based selections Lymphocyte Function-associated Antigen 1 LFA-1 PPI Encoded Library Technology DNA-encoded libraries ICAM-1 Intercellular Adhesion Molecule 1 ELT Protein-Protein Interactions SITE DESIGN MOLECULE CHEMICAL LIBRARY PEPTIDE CONFORMATIONAL REGULATION INHIBITORS I-DOMAIN BINDING SUBUNIT |
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Snippet | Encoded library technology (ELT) was utilized to identify a class of compounds that disrupt the interaction between lymphocyte function-associated antigen-1... The inhibition of protein-protein interactions remains a challenge for traditional small molecule drug discovery. Here we describe the use of DNA-encoded... |
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SubjectTerms | Affinity-based selections Biochemistry & Molecular Biology Cell Adhesion - drug effects Chemistry Chemistry, Medicinal Chemistry, Organic DNA-encoded libraries Dose-Response Relationship, Drug Drug Discovery Encoded Library Technology Humans Intercellular Adhesion Molecule 1 Jurkat Cells Life Sciences & Biomedicine Ligands Lymphocyte Function-associated Antigen 1 Lymphocyte Function-Associated Antigen-1 - metabolism Molecular Structure Pharmacology & Pharmacy Physical Sciences Protein Binding - drug effects Protein-Protein Interactions Science & Technology Small Molecule Libraries - chemical synthesis Small Molecule Libraries - chemistry Small Molecule Libraries - pharmacology Structure-Activity Relationship |
Title | Application of encoded library technology (ELT) to a protein–protein interaction target: Discovery of a potent class of integrin lymphocyte function-associated antigen 1 (LFA-1) antagonists |
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