Protein complexes including PGRMC1 and actin-associated proteins are disrupted by AG-205

Sarah Teakel; Marina Ludescher; Bashar Thejer; Gereon Poschmann; Jade Forwood; Hans Neubauer; Michael A. Cahill

doi:10.1016/j.bbrc.2019.12.108

Protein complexes including PGRMC1 and actin-associated proteins are disrupted by AG-205

Sarah Teakel, Marina Ludescher, Bashar Thejer, Gereon Poschmann, Jade Forwood, Hans Neubauer, Michael A. Cahill

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

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Abstract

PGRMC1 is a protein from the MAPR family with a range of cellular functions. PGRMC1 has been described to play a role in fertility, neuroprotection, steroidogenesis, membrane trafficking and in cancer cell biology. PGRMC1 represents a likely key regulator of cell metabolism and proliferation, as well as a potential target for anti-cancer therapies. To further understand the functions of PGRMC1 and the mechanism of the small molecule inhibitor of PGRMC1, AG-205, proteins differentially bound to PGRMC1 were identified following AG-205 treatment of MIA PaCa-2 cells. Our results suggest that AG-205 influences PGRMC1 interactions with the actin cytoskeleton. The binding of two PGRMC1-associated proteins that support this, RACK1 and alpha-Actinin-1, was reduced following AG-205 treatment. The biology associated with PGRMC1 binding partners identified here merits further investigation.

Original language	English
Pages (from-to)	64-69
Number of pages	6
Journal	Biochemical and Biophysical Research Communications
Volume	524
Issue number	1
Early online date	21 Jan 2020
DOIs	https://doi.org/10.1016/j.bbrc.2019.12.108
Publication status	Published - 26 Mar 2020

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10.1016/j.bbrc.2019.12.108

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@article{44185358dd9c41958b2b33b103a5cc3a,

title = "Protein complexes including PGRMC1 and actin-associated proteins are disrupted by AG-205",

abstract = "PGRMC1 is a protein from the MAPR family with a range of cellular functions. PGRMC1 has been described to play a role in fertility, neuroprotection, steroidogenesis, membrane trafficking and in cancer cell biology. PGRMC1 represents a likely key regulator of cell metabolism and proliferation, as well as a potential target for anti-cancer therapies. To further understand the functions of PGRMC1 and the mechanism of the small molecule inhibitor of PGRMC1, AG-205, proteins differentially bound to PGRMC1 were identified following AG-205 treatment of MIA PaCa-2 cells. Our results suggest that AG-205 influences PGRMC1 interactions with the actin cytoskeleton. The binding of two PGRMC1-associated proteins that support this, RACK1 and alpha-Actinin-1, was reduced following AG-205 treatment. The biology associated with PGRMC1 binding partners identified here merits further investigation.",

keywords = "Cytochrome b5 domain, Membrane trafficking, Actin cytoskeleton, Affinity proteomics, Membrane-associated progesterone receptor, MAPR",

author = "Sarah Teakel and Marina Ludescher and Bashar Thejer and Gereon Poschmann and Jade Forwood and Hans Neubauer and Cahill, {Michael A.}",

year = "2020",

month = mar,

day = "26",

doi = "10.1016/j.bbrc.2019.12.108",

language = "English",

volume = "524",

pages = "64--69",

journal = "Biochemical and Biophysical Research Communications",

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TY - JOUR

T1 - Protein complexes including PGRMC1 and actin-associated proteins are disrupted by AG-205

AU - Teakel, Sarah

AU - Ludescher, Marina

AU - Thejer, Bashar

AU - Poschmann, Gereon

AU - Forwood, Jade

AU - Neubauer, Hans

AU - Cahill, Michael A.

PY - 2020/3/26

Y1 - 2020/3/26

N2 - PGRMC1 is a protein from the MAPR family with a range of cellular functions. PGRMC1 has been described to play a role in fertility, neuroprotection, steroidogenesis, membrane trafficking and in cancer cell biology. PGRMC1 represents a likely key regulator of cell metabolism and proliferation, as well as a potential target for anti-cancer therapies. To further understand the functions of PGRMC1 and the mechanism of the small molecule inhibitor of PGRMC1, AG-205, proteins differentially bound to PGRMC1 were identified following AG-205 treatment of MIA PaCa-2 cells. Our results suggest that AG-205 influences PGRMC1 interactions with the actin cytoskeleton. The binding of two PGRMC1-associated proteins that support this, RACK1 and alpha-Actinin-1, was reduced following AG-205 treatment. The biology associated with PGRMC1 binding partners identified here merits further investigation.

AB - PGRMC1 is a protein from the MAPR family with a range of cellular functions. PGRMC1 has been described to play a role in fertility, neuroprotection, steroidogenesis, membrane trafficking and in cancer cell biology. PGRMC1 represents a likely key regulator of cell metabolism and proliferation, as well as a potential target for anti-cancer therapies. To further understand the functions of PGRMC1 and the mechanism of the small molecule inhibitor of PGRMC1, AG-205, proteins differentially bound to PGRMC1 were identified following AG-205 treatment of MIA PaCa-2 cells. Our results suggest that AG-205 influences PGRMC1 interactions with the actin cytoskeleton. The binding of two PGRMC1-associated proteins that support this, RACK1 and alpha-Actinin-1, was reduced following AG-205 treatment. The biology associated with PGRMC1 binding partners identified here merits further investigation.

KW - Cytochrome b5 domain

KW - Membrane trafficking

KW - Actin cytoskeleton

KW - Affinity proteomics

KW - Membrane-associated progesterone receptor

KW - MAPR

U2 - 10.1016/j.bbrc.2019.12.108

DO - 10.1016/j.bbrc.2019.12.108

M3 - Article

C2 - 31980178

VL - 524

SP - 64

EP - 69

JO - Biochemical and Biophysical Research Communications

JF - Biochemical and Biophysical Research Communications

SN - 0006-291X

IS - 1

ER -

Protein complexes including PGRMC1 and actin-associated proteins are disrupted by AG-205

Abstract

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