The identification of AF38469: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin

Tenna Juul Schrøder; Søren Christensen; Samsa Lindberg; Morten Langgård; Laurent David; Philip J Maltas; Jørgen Eskildsen; Jan Jacobsen; Lena Tagmose; Klaus Bæk Simonsen; Lars Christian Biilmann Rønn; Inge Elisabeth Maria de Jong; Ibrahim J Malik; Jens-Jakob Karlsson; Christoffer Bundgaard; Jan Egebjerg; Jeffrey B Stavenhagen; Dorthe Strandbygård; Søren Skou Thirup; Jacob Lauwring Andersen; Srinivas Uppalanchi; Sridhar Pervaram; Shiva Prasad Kasturi; Pradheep Eradi; Durga Rao Sakumudi; Stephen Paul Watson

doi:10.1016/j.bmcl.2013.11.046

The identification of AF38469: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin

Tenna Juul Schrøder, Søren Christensen, Samsa Lindberg, Morten Langgård, Laurent David, Philip J Maltas, Jørgen Eskildsen, Jan Jacobsen, Lena Tagmose, Klaus Bæk Simonsen, Lars Christian Biilmann Rønn, Inge Elisabeth Maria de Jong, Ibrahim J Malik, Jens-Jakob Karlsson, Christoffer Bundgaard, Jan Egebjerg, Jeffrey B Stavenhagen, Dorthe Strandbygård, Søren Skou Thirup, Jacob Lauwring AndersenSrinivas Uppalanchi, Sridhar Pervaram, Shiva Prasad Kasturi, Pradheep Eradi, Durga Rao Sakumudi, Stephen Paul Watson

Department of Molecular Biology and Genetics - Neurobiology

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

Abstract

The identification of the novel, selective, orally bioavailable Sortilin inhibitor AF38469 is described. Structure-activity relationships and syntheses are reported, along with an X-ray crystal structure of the sortilin-AF38469 protein-inhibitor complex.

Original language	English
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	24
Issue	1
Pages (from-to)	177-180
Number of pages	4
ISSN	0960-894X
DOIs	https://doi.org/10.1016/j.bmcl.2013.11.046
Publication status	Published - 1 Jan 2014

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Schrøder, T. J., Christensen, S., Lindberg, S., Langgård, M., David, L., Maltas, P. J., Eskildsen, J., Jacobsen, J., Tagmose, L., Simonsen, K. B., Biilmann Rønn, L. C., de Jong, I. E. M., Malik, I. J., Karlsson, J.-J., Bundgaard, C., Egebjerg, J., Stavenhagen, J. B., Strandbygård, D., Thirup, S. S., ... Watson, S. P. (2014). The identification of AF38469: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin. Bioorganic & Medicinal Chemistry Letters, 24(1), 177-180. https://doi.org/10.1016/j.bmcl.2013.11.046

@article{6779ad6696894930877f5ce944631a3e,

title = "The identification of AF38469: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin",

abstract = "The identification of the novel, selective, orally bioavailable Sortilin inhibitor AF38469 is described. Structure-activity relationships and syntheses are reported, along with an X-ray crystal structure of the sortilin-AF38469 protein-inhibitor complex.",

author = "Schr{\o}der, {Tenna Juul} and S{\o}ren Christensen and Samsa Lindberg and Morten Langg{\aa}rd and Laurent David and Maltas, {Philip J} and J{\o}rgen Eskildsen and Jan Jacobsen and Lena Tagmose and Simonsen, {Klaus B{\ae}k} and {Biilmann R{\o}nn}, {Lars Christian} and {de Jong}, {Inge Elisabeth Maria} and Malik, {Ibrahim J} and Jens-Jakob Karlsson and Christoffer Bundgaard and Jan Egebjerg and Stavenhagen, {Jeffrey B} and Dorthe Strandbyg{\aa}rd and Thirup, {S{\o}ren Skou} and Andersen, {Jacob Lauwring} and Srinivas Uppalanchi and Sridhar Pervaram and Kasturi, {Shiva Prasad} and Pradheep Eradi and Sakumudi, {Durga Rao} and Watson, {Stephen Paul}",

year = "2014",

month = jan,

day = "1",

doi = "10.1016/j.bmcl.2013.11.046",

language = "English",

volume = "24",

pages = "177--180",

journal = "Bioorganic & Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Pergamon Press",

number = "1",

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Schrøder, TJ, Christensen, S, Lindberg, S, Langgård, M, David, L, Maltas, PJ, Eskildsen, J, Jacobsen, J, Tagmose, L, Simonsen, KB, Biilmann Rønn, LC, de Jong, IEM, Malik, IJ, Karlsson, J-J, Bundgaard, C, Egebjerg, J, Stavenhagen, JB, Strandbygård, D , Thirup, SS, Andersen, JL, Uppalanchi, S, Pervaram, S, Kasturi, SP, Eradi, P, Sakumudi, DR & Watson, SP 2014, 'The identification of AF38469: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin', Bioorganic & Medicinal Chemistry Letters, vol. 24, no. 1, pp. 177-180. https://doi.org/10.1016/j.bmcl.2013.11.046

The identification of AF38469: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin. / Schrøder, Tenna Juul; Christensen, Søren; Lindberg, Samsa et al.
In: Bioorganic & Medicinal Chemistry Letters, Vol. 24, No. 1, 01.01.2014, p. 177-180.

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

TY - JOUR

T1 - The identification of AF38469: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin

T2 - An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin

AU - Schrøder, Tenna Juul

AU - Christensen, Søren

AU - Lindberg, Samsa

AU - Langgård, Morten

AU - David, Laurent

AU - Maltas, Philip J

AU - Eskildsen, Jørgen

AU - Jacobsen, Jan

AU - Tagmose, Lena

AU - Simonsen, Klaus Bæk

AU - Biilmann Rønn, Lars Christian

AU - de Jong, Inge Elisabeth Maria

AU - Malik, Ibrahim J

AU - Karlsson, Jens-Jakob

AU - Bundgaard, Christoffer

AU - Egebjerg, Jan

AU - Stavenhagen, Jeffrey B

AU - Strandbygård, Dorthe

AU - Thirup, Søren Skou

AU - Andersen, Jacob Lauwring

AU - Uppalanchi, Srinivas

AU - Pervaram, Sridhar

AU - Kasturi, Shiva Prasad

AU - Eradi, Pradheep

AU - Sakumudi, Durga Rao

AU - Watson, Stephen Paul

PY - 2014/1/1

Y1 - 2014/1/1

N2 - The identification of the novel, selective, orally bioavailable Sortilin inhibitor AF38469 is described. Structure-activity relationships and syntheses are reported, along with an X-ray crystal structure of the sortilin-AF38469 protein-inhibitor complex.

AB - The identification of the novel, selective, orally bioavailable Sortilin inhibitor AF38469 is described. Structure-activity relationships and syntheses are reported, along with an X-ray crystal structure of the sortilin-AF38469 protein-inhibitor complex.

U2 - 10.1016/j.bmcl.2013.11.046

DO - 10.1016/j.bmcl.2013.11.046

M3 - Journal article

C2 - 24355129

SN - 0960-894X

VL - 24

SP - 177

EP - 180

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 1

ER -

Schrøder TJ, Christensen S, Lindberg S, Langgård M, David L, Maltas PJ et al. The identification of AF38469: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin. Bioorganic & Medicinal Chemistry Letters. 2014 Jan 1;24(1):177-180. doi: 10.1016/j.bmcl.2013.11.046

The identification of AF38469: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin

Abstract

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