The identification of novel acid isostere based inhibitors of the VPS10P family sorting receptor Sortilin

Jacob Lauwring Andersen; Samsa Lindberg; Morten Langgård; Philip J Maltas; Lars Christian Biilmann Rønn; Christoffer Bundgaard; Dorthe Strandbygaard; Søren Thirup; Stephen Paul Watson

doi:10.1016/j.bmcl.2017.02.028

The identification of novel acid isostere based inhibitors of the VPS10P family sorting receptor Sortilin

Jacob Lauwring Andersen, Samsa Lindberg, Morten Langgård, Philip J Maltas, Lars Christian Biilmann Rønn, Christoffer Bundgaard, Dorthe Strandbygaard, Søren Thirup, Stephen Paul Watson

Research output: Contribution to journal/Conference contribution in journal/Contribution to newspaper › Journal article › Research › peer-review

Abstract

Using fragment based and structure based drug discovery strategies a series of novel Sortilin inhibitors has been identified. The inhibitors are based on the N-substituted 1,2,3-triazol-4-one/ol heterocyclic template. X-ray crystallography shows that the 1,2,3-triazol-4-one/ol acts as a carboxylic acid isostere, making a bi-dentate interaction with an arginine residue of Sortilin, an interaction which has not been previously characterised for this heterocycle.

Original language	English
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	27
Issue	11
Pages (from-to)	2629-2633
Number of pages	5
ISSN	0960-894X
DOIs	https://doi.org/10.1016/j.bmcl.2017.02.028
Publication status	Published - 1 Jun 2017

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Journal Article

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10.1016/j.bmcl.2017.02.028

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title = "The identification of novel acid isostere based inhibitors of the VPS10P family sorting receptor Sortilin",

abstract = "Using fragment based and structure based drug discovery strategies a series of novel Sortilin inhibitors has been identified. The inhibitors are based on the N-substituted 1,2,3-triazol-4-one/ol heterocyclic template. X-ray crystallography shows that the 1,2,3-triazol-4-one/ol acts as a carboxylic acid isostere, making a bi-dentate interaction with an arginine residue of Sortilin, an interaction which has not been previously characterised for this heterocycle.",

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doi = "10.1016/j.bmcl.2017.02.028",

language = "English",

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journal = "Bioorganic & Medicinal Chemistry Letters",

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The identification of novel acid isostere based inhibitors of the VPS10P family sorting receptor Sortilin. / Andersen, Jacob Lauwring; Lindberg, Samsa; Langgård, Morten et al.
In: Bioorganic & Medicinal Chemistry Letters, Vol. 27, No. 11, 01.06.2017, p. 2629-2633.

Research output: Contribution to journal/Conference contribution in journal/Contribution to newspaper › Journal article › Research › peer-review

TY - JOUR

T1 - The identification of novel acid isostere based inhibitors of the VPS10P family sorting receptor Sortilin

AU - Andersen, Jacob Lauwring

AU - Lindberg, Samsa

AU - Langgård, Morten

AU - Maltas, Philip J

AU - Rønn, Lars Christian Biilmann

AU - Bundgaard, Christoffer

AU - Strandbygaard, Dorthe

AU - Thirup, Søren

AU - Watson, Stephen Paul

PY - 2017/6/1

Y1 - 2017/6/1

N2 - Using fragment based and structure based drug discovery strategies a series of novel Sortilin inhibitors has been identified. The inhibitors are based on the N-substituted 1,2,3-triazol-4-one/ol heterocyclic template. X-ray crystallography shows that the 1,2,3-triazol-4-one/ol acts as a carboxylic acid isostere, making a bi-dentate interaction with an arginine residue of Sortilin, an interaction which has not been previously characterised for this heterocycle.

AB - Using fragment based and structure based drug discovery strategies a series of novel Sortilin inhibitors has been identified. The inhibitors are based on the N-substituted 1,2,3-triazol-4-one/ol heterocyclic template. X-ray crystallography shows that the 1,2,3-triazol-4-one/ol acts as a carboxylic acid isostere, making a bi-dentate interaction with an arginine residue of Sortilin, an interaction which has not been previously characterised for this heterocycle.

KW - Journal Article

U2 - 10.1016/j.bmcl.2017.02.028

DO - 10.1016/j.bmcl.2017.02.028

M3 - Journal article

C2 - 28462834

SN - 0960-894X

VL - 27

SP - 2629

EP - 2633

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 11

ER -

The identification of novel acid isostere based inhibitors of the VPS10P family sorting receptor Sortilin

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