Development of Peptide-Based PDZ Domain Inhibitors

Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review

Standard

Development of Peptide-Based PDZ Domain Inhibitors. / Essig, Dominik J.; Balboa, Javier R.; Strømgaard, Kristian.

Methods in Molecular Biology. ed. / Jean-Paul Borg. Humana Press, 2021. p. 157-177 (Methods in Molecular Biology, Vol. 2256).

Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review

Harvard

Essig, DJ, Balboa, JR & Strømgaard, K 2021, Development of Peptide-Based PDZ Domain Inhibitors. in J-PB (ed.), Methods in Molecular Biology. Humana Press, Methods in Molecular Biology, vol. 2256, pp. 157-177. https://doi.org/10.1007/978-1-0716-1166-1_10

APA

Essig, D. J., Balboa, J. R., & Strømgaard, K. (2021). Development of Peptide-Based PDZ Domain Inhibitors. In J-P. B. (Ed.), Methods in Molecular Biology (pp. 157-177). Humana Press. Methods in Molecular Biology Vol. 2256 https://doi.org/10.1007/978-1-0716-1166-1_10

Vancouver

Essig DJ, Balboa JR, Strømgaard K. Development of Peptide-Based PDZ Domain Inhibitors. In J-PB, editor, Methods in Molecular Biology. Humana Press. 2021. p. 157-177. (Methods in Molecular Biology, Vol. 2256). https://doi.org/10.1007/978-1-0716-1166-1_10

Author

Essig, Dominik J. ; Balboa, Javier R. ; Strømgaard, Kristian. / Development of Peptide-Based PDZ Domain Inhibitors. Methods in Molecular Biology. editor / Jean-Paul Borg. Humana Press, 2021. pp. 157-177 (Methods in Molecular Biology, Vol. 2256).

Bibtex

@inbook{b594895465d348b78ab19234a55564fd,

title = "Development of Peptide-Based PDZ Domain Inhibitors",

abstract = "Over the past decades, peptide-based drugs have gained increasing interest in a wide range of treatment applications, primarily because of high potency and selectivity, as well as good efficacy, tolerability, and safety often achieved with peptides. Attempts to target postsynaptic density protein of 95 (PSD-95) PSD-95/Discs large/Zonula occludens-1 (PDZ) domains, which mediate the formation of a ternary complex with the N-methyl-d-aspartate (NMDA) receptor and neuronal nitric oxide synthase (nNOS) responsible for excitotoxicity in ischemic stroke, by high-affinity small molecules have failed in the past. In this chapter, we focus on the discovery of peptide-based drugs targeting PSD-95, using AVLX-144 as an example, from the synthesis, over binding assays to its target, to further in vitro experiments based on the development of AVLX-144, a potential stroke treatment, which is planned to enter clinical trials in 2020.",

keywords = "AVLX-144, Inhibition, PDZ domains, Protein–protein interactions, Stroke",

author = "Essig, {Dominik J.} and Balboa, {Javier R.} and Kristian Str{\o}mgaard",

note = "Publisher Copyright: {\textcopyright} 2021, Springer Science+Business Media, LLC, part of Springer Nature.",

year = "2021",

doi = "10.1007/978-1-0716-1166-1_10",

language = "English",

isbn = "978-1-0716-1165-4",

series = "Methods in Molecular Biology",

publisher = "Humana Press",

pages = "157--177",

editor = "{Jean-Paul Borg}",

booktitle = "Methods in Molecular Biology",

address = "United States",

}

RIS

TY - CHAP

T1 - Development of Peptide-Based PDZ Domain Inhibitors

AU - Essig, Dominik J.

AU - Balboa, Javier R.

AU - Strømgaard, Kristian

PY - 2021

Y1 - 2021

N2 - Over the past decades, peptide-based drugs have gained increasing interest in a wide range of treatment applications, primarily because of high potency and selectivity, as well as good efficacy, tolerability, and safety often achieved with peptides. Attempts to target postsynaptic density protein of 95 (PSD-95) PSD-95/Discs large/Zonula occludens-1 (PDZ) domains, which mediate the formation of a ternary complex with the N-methyl-d-aspartate (NMDA) receptor and neuronal nitric oxide synthase (nNOS) responsible for excitotoxicity in ischemic stroke, by high-affinity small molecules have failed in the past. In this chapter, we focus on the discovery of peptide-based drugs targeting PSD-95, using AVLX-144 as an example, from the synthesis, over binding assays to its target, to further in vitro experiments based on the development of AVLX-144, a potential stroke treatment, which is planned to enter clinical trials in 2020.

AB - Over the past decades, peptide-based drugs have gained increasing interest in a wide range of treatment applications, primarily because of high potency and selectivity, as well as good efficacy, tolerability, and safety often achieved with peptides. Attempts to target postsynaptic density protein of 95 (PSD-95) PSD-95/Discs large/Zonula occludens-1 (PDZ) domains, which mediate the formation of a ternary complex with the N-methyl-d-aspartate (NMDA) receptor and neuronal nitric oxide synthase (nNOS) responsible for excitotoxicity in ischemic stroke, by high-affinity small molecules have failed in the past. In this chapter, we focus on the discovery of peptide-based drugs targeting PSD-95, using AVLX-144 as an example, from the synthesis, over binding assays to its target, to further in vitro experiments based on the development of AVLX-144, a potential stroke treatment, which is planned to enter clinical trials in 2020.

KW - AVLX-144

KW - Inhibition

KW - PDZ domains

KW - Protein–protein interactions

KW - Stroke

U2 - 10.1007/978-1-0716-1166-1_10

DO - 10.1007/978-1-0716-1166-1_10

M3 - Book chapter

C2 - 34014522

AN - SCOPUS:85106444970

SN - 978-1-0716-1165-4

SN - 978-1-0716-1168-5

T3 - Methods in Molecular Biology

SP - 157

EP - 177

BT - Methods in Molecular Biology

A2 - null, Jean-Paul Borg

PB - Humana Press

ER -

ID: 273635379

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