Design and modular parallel synthesis of a MCR derived α-helix mimetic protein-protein interaction inhibitor scaffold

Walfrido Antuch; Sanjay Menon; Quin-Zene Chen; Yingchun Lu; Sukumar Sakamuri; Barbara Beck; Vesna Schauer-Vukašinović; Seema Agarwal; Sibylle Hess; Alexander Dömling

doi:10.1016/j.bmcl.2005.11.102

Design and modular parallel synthesis of a MCR derived α-helix mimetic protein-protein interaction inhibitor scaffold

Walfrido Antuch, Sanjay Menon, Quin-Zene Chen, Yingchun Lu, Sukumar Sakamuri, Barbara Beck, Vesna Schauer-Vukašinović, Seema Agarwal, Sibylle Hess, Alexander Dömling

Research output: Contribution to journal › Article › Academic › peer-review

48 Citations (Scopus)

Abstract

A terphenyl α-helix mimetic scaffold recognized to be capable of disrupting protein-protein interactions was structurally morphed into an easily amenable and versatile multicomponent reaction (MCR) backbone. The design, modular in-parallel library synthesis, initial cell based biological data, and preliminary in vitro screening for the disruption of the Bcl-w/Bak protein-protein interaction by representatives of the MCR derived scaffold are presented.

Original language	English
Pages (from-to)	1740-1743
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	6
DOIs	https://doi.org/10.1016/j.bmcl.2005.11.102
Publication status	Published - 15-Mar-2006

Keywords

Apoptosis
Bcl family
Cancer
Isocyanide
Multicomponent reaction
Protein interaction antagonist
imidazole
terphenyl derivative
alpha helix
apoptosis
article
cell proliferation
enzyme inhibition
protein protein interaction
protein structure
protein synthesis

Access to Document

10.1016/j.bmcl.2005.11.102

Cite this

Antuch, Walfrido ; Menon, Sanjay ; Chen, Quin-Zene ; Lu, Yingchun ; Sakamuri, Sukumar ; Beck, Barbara ; Schauer-Vukašinović, Vesna ; Agarwal, Seema ; Hess, Sibylle ; Dömling, Alexander. / Design and modular parallel synthesis of a MCR derived α-helix mimetic protein-protein interaction inhibitor scaffold. In: Bioorganic and Medicinal Chemistry Letters. 2006 ; Vol. 16, No. 6. pp. 1740-1743.

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abstract = "A terphenyl α-helix mimetic scaffold recognized to be capable of disrupting protein-protein interactions was structurally morphed into an easily amenable and versatile multicomponent reaction (MCR) backbone. The design, modular in-parallel library synthesis, initial cell based biological data, and preliminary in vitro screening for the disruption of the Bcl-w/Bak protein-protein interaction by representatives of the MCR derived scaffold are presented.",

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Design and modular parallel synthesis of a MCR derived α-helix mimetic protein-protein interaction inhibitor scaffold. / Antuch, Walfrido; Menon, Sanjay; Chen, Quin-Zene; Lu, Yingchun; Sakamuri, Sukumar; Beck, Barbara; Schauer-Vukašinović, Vesna; Agarwal, Seema; Hess, Sibylle; Dömling, Alexander.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 6, 15.03.2006, p. 1740-1743.

Research output: Contribution to journal › Article › Academic › peer-review

TY - JOUR

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AU - Antuch, Walfrido

AU - Menon, Sanjay

AU - Chen, Quin-Zene

AU - Lu, Yingchun

AU - Sakamuri, Sukumar

AU - Beck, Barbara

AU - Schauer-Vukašinović, Vesna

AU - Agarwal, Seema

AU - Hess, Sibylle

AU - Dömling, Alexander

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AB - A terphenyl α-helix mimetic scaffold recognized to be capable of disrupting protein-protein interactions was structurally morphed into an easily amenable and versatile multicomponent reaction (MCR) backbone. The design, modular in-parallel library synthesis, initial cell based biological data, and preliminary in vitro screening for the disruption of the Bcl-w/Bak protein-protein interaction by representatives of the MCR derived scaffold are presented.

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KW - Bcl family

KW - Cancer

KW - Isocyanide

KW - Multicomponent reaction

KW - Protein interaction antagonist

KW - imidazole

KW - terphenyl derivative

KW - alpha helix

KW - apoptosis

KW - article

KW - cell proliferation

KW - enzyme inhibition

KW - protein protein interaction

KW - protein structure

KW - protein synthesis

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DO - 10.1016/j.bmcl.2005.11.102

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EP - 1743

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

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