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Thermodynamic profiling of conformationally constrained cyclic ligands for the PDZ domain.

Publication ,  Journal Article
Li, T; Saro, D; Spaller, MR
Published in: Bioorganic & Medicinal Chemistry Letters
March 2004

Inspired by structure-based design and tailored for combinatorial preparation, a series of novel cyclic peptides has been developed to yield binding ligands for the third PDZ domain (PDZ3) of PSD-95. These side chain-side chain bridged peptides permit the systematic expansion or contraction of ring size, which is intended to maximize the conformational diversity of the ensemble. Isothermal titration calorimetry (ITC) was used to measure the dissociation constants (K(d)) and associated thermodynamic binding parameters.

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Published In

Bioorganic & Medicinal Chemistry Letters

DOI

EISSN

1464-3405

ISSN

0960-894X

Publication Date

March 2004

Volume

14

Issue

6

Start / End Page

1385 / 1388

Related Subject Headings

  • Thermodynamics
  • Protein Conformation
  • Nerve Tissue Proteins
  • Neoplasm Proteins
  • Medicinal & Biomolecular Chemistry
  • Ligands
  • Cell Adhesion Molecules
  • Binding Sites
  • Adaptor Proteins, Signal Transducing
  • 1115 Pharmacology and Pharmaceutical Sciences
 

Citation

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MLA
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Li, T., Saro, D., & Spaller, M. R. (2004). Thermodynamic profiling of conformationally constrained cyclic ligands for the PDZ domain. Bioorganic & Medicinal Chemistry Letters, 14(6), 1385–1388. https://doi.org/10.1016/j.bmcl.2003.09.103
Li, Tao, Dorina Saro, and Mark R. Spaller. “Thermodynamic profiling of conformationally constrained cyclic ligands for the PDZ domain.Bioorganic & Medicinal Chemistry Letters 14, no. 6 (March 2004): 1385–88. https://doi.org/10.1016/j.bmcl.2003.09.103.
Li T, Saro D, Spaller MR. Thermodynamic profiling of conformationally constrained cyclic ligands for the PDZ domain. Bioorganic & Medicinal Chemistry Letters. 2004 Mar;14(6):1385–8.
Li, Tao, et al. “Thermodynamic profiling of conformationally constrained cyclic ligands for the PDZ domain.Bioorganic & Medicinal Chemistry Letters, vol. 14, no. 6, Mar. 2004, pp. 1385–88. Epmc, doi:10.1016/j.bmcl.2003.09.103.
Li T, Saro D, Spaller MR. Thermodynamic profiling of conformationally constrained cyclic ligands for the PDZ domain. Bioorganic & Medicinal Chemistry Letters. 2004 Mar;14(6):1385–1388.
Journal cover image

Published In

Bioorganic & Medicinal Chemistry Letters

DOI

EISSN

1464-3405

ISSN

0960-894X

Publication Date

March 2004

Volume

14

Issue

6

Start / End Page

1385 / 1388

Related Subject Headings

  • Thermodynamics
  • Protein Conformation
  • Nerve Tissue Proteins
  • Neoplasm Proteins
  • Medicinal & Biomolecular Chemistry
  • Ligands
  • Cell Adhesion Molecules
  • Binding Sites
  • Adaptor Proteins, Signal Transducing
  • 1115 Pharmacology and Pharmaceutical Sciences