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G protein-coupled estrogen receptor GPER and breast carcinogenesis

Award Number: R01CA163890
ORGANIZATION: NATIONAL CANCER INSTITUTE
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 08/01/2012
PERIOD OF PERFORMANCE END DATE: 08/31/2025

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G protein-coupled estrogen receptor GPER and breast carcinogenesis - Selective estrogen receptor (ER) modulators and downregulators (SERMs and SERDs, also refereed to as anti-hormones) have saved the lives of millions of women with ER-positive breast cancer. Unfortunately, approximately one-third of these women display intrinsic resistance to these targeted therapies, while a similar fraction of women treated with anti-hormones will develop resistance over time, resulting in recurrences of often more aggressive cancers. SERMs and SERDs inhibit the classical nuclear estrogen receptor ERα, leading to the inhibition of cell proliferation and survival. In contrast, our results have shown that these same drugs activate the 7-transmembrane spanning G protein-coupled estrogen receptor GPER, resulting in the stimulation of the pro-survival PI3K/Akt axis. Furthermore, our recent studies have suggested that this may occur through phosphorylation and inactivation of the FOXO3 pro-apoptotic transcription factor. We have identified a collection of novel compounds that display strong selectivity for either ERα or GPER. By combining these pharmacological approaches with genetic approaches, we hypothesize that acquired resistance to anti-hormones involves their activation of GPER, resulting in the inactivation of FOXO3. We propose to test this hypothesis with the following specific aims: Aim 1 will test whether GPER mediates acquired breast cancer resistance to SERMs and SERDs. Aim 2 will test whether the inactivation of FOXO3 represents a critical step in enhancing tumor cell survival in the face of ERα inhibition. Aim 3 will employ a murine model of spontaneous breast cancer to test whether blocking GPER activity in combination with tamoxifen treatment, or alternatively selectively inhibiting ERα with novel drugs, prevents acquired resistance. Significance: Completion of these aims will significantly advance our knowledge of the role of the novel estrogen receptor GPER in acquired anti-hormone resistance in breast cancer. Identifying GPER as a novel mediator in acquired anti-hormone resistance in breast cancer in combination with the use novel highly selective ligands to be evaluated in this proposal could lead to significant improvements in outcome for the150,000 women diagnosed with ER-positive breast cancer each year.


Issue Date FY	Funding FY	Legal Entity Name	Legal Entity Address	Legal Entity City	Legal Entity State	Legal Entity Zip Code	Legal Entity COUNTY	Legal Entity COUNTRY	Assistance Listing	Award Code	Budget Year	Action Date	Action Type	Action Amount

Issue Date FY: 2026 ( Subtotal = -$90 )
2026	2023	UNIVERSITY OF NEW MEXICO	1 UNIVERSITY OF NEW MEXICO	ALBUQUERQUE	NM	87131	BERNALILLO	USA	Cancer Biology Research	000	11	12/18/2025	NON-COMPETING CONTINUATION	-$90
														Subtotal = -$90

Issue Date FY: 2023 ( Subtotal = $191,101 )
2023	2023	UNIVERSITY OF NEW MEXICO	1 UNIVERSITY OF NEW MEXICO	ALBUQUERQUE	NM	87131	BERNALILLO	USA	Cancer Biology Research	000	11	9/5/2023	NON-COMPETING CONTINUATION	$191,101
														Subtotal = $191,101

Issue Date FY: 2022 ( Subtotal = $346,862 )
2022	2022	UNIVERSITY OF NEW MEXICO	2500 MARBLE DR NE	ALBUQUERQUE	NM	87131	BERNALILLO	USA	Cancer Biology Research	000	10	8/23/2022	NON-COMPETING CONTINUATION	$346,862
														Subtotal = $346,862

Issue Date FY: 2021 ( Subtotal = $353,942 )
2021	2021	UNIVERSITY OF NEW MEXICO	2500 MARBLE DR NE	ALBUQUERQUE	NM	87131	BERNALILLO	USA	Cancer Biology Research	000	9	8/20/2021	NON-COMPETING CONTINUATION	$353,942
														Subtotal = $353,942

Issue Date FY: 2020 ( Subtotal = $158,942 )
2020	2020	UNIVERSITY OF NEW MEXICO	2500 MARBLE DR NE	ALBUQUERQUE	NM	87131	BERNALILLO	USA	Cancer Biology Research	000	8	9/1/2020	NON-COMPETING CONTINUATION	$158,942
														Subtotal = $158,942

Issue Date FY: 2019 ( Subtotal = $343,324 )
2019	2019	UNIVERSITY OF NEW MEXICO	2500 MARBLE DR NE	ALBUQUERQUE	NM	87131	BERNALILLO	USA	Cancer Biology Research	001	7	8/16/2019	NON-COMPETING CONTINUATION	$343,324
2019	2016	UNIVERSITY OF NEW MEXICO	2500 MARBLE DR NE	ALBUQUERQUE	NM	87131	BERNALILLO	USA	Cancer Biology Research	000	5	11/8/2018	EXTENSION WITH OR WITHOUT FUNDS	$0
														Subtotal = $343,324

Issue Date FY: 2018 ( Subtotal = $353,942 )
2018	2018	UNIVERSITY OF NEW MEXICO	2500 MARBLE DR NE	ALBUQUERQUE	NM	87131	BERNALILLO	USA	Cancer Biology Research	000	6	8/31/2018	COMPETING CONTINUATION	$353,942
														Subtotal = $353,942

Issue Date FY: 2016 ( Subtotal = $313,325 )
2016	2016	UNIVERSITY OF NEW MEXICO (THE)	1 UNIVERSITY OF NEW MEXICO	ALBUQUERQUE	NM	87131	BERNALILLO	USA	Cancer Biology Research	000	5	5/9/2016	EXTENSION WITH OR WITHOUT FUNDS	$313,325
														Subtotal = $313,325

Issue Date FY: 2015 ( Subtotal = $313,325 )
2015	2015	UNIVERSITY OF NEW MEXICO (THE)	1 UNIVERSITY OF NEW MEXICO	ALBUQUERQUE	NM	87131	BERNALILLO	USA	Cancer Biology Research	000	4	6/4/2015	NON-COMPETING CONTINUATION	$313,325
														Subtotal = $313,325

Issue Date FY: 2014 ( Subtotal = $303,925 )
2014	2014	UNIVERSITY OF NEW MEXICO (THE)	1 UNIVERSITY OF NEW MEXICO	ALBUQUERQUE	NM	87131	BERNALILLO	USA	Cancer Biology Research	000	3	5/15/2014	NON-COMPETING CONTINUATION	$303,925
														Subtotal = $303,925

Issue Date FY: 2013 ( Subtotal = $294,526 )
2013	2013	UNIVERSITY OF NEW MEXICO (THE)	1 UNIVERSITY OF NEW MEXICO	ALBUQUERQUE	NM	87131	BERNALILLO	USA	Cancer Biology Research	000	2	6/11/2013	NON-COMPETING CONTINUATION	$294,526
														Subtotal = $294,526

Issue Date FY: 2012 ( Subtotal = $313,325 )
2012	2012	UNIVERSITY OF NEW MEXICO (THE)	1 UNIVERSITY OF NEW MEXICO	ALBUQUERQUE	NM	87131	BERNALILLO	USA	Cancer Biology Research	000	1	7/26/2012	NEW	$313,325
														Subtotal = $313,325

Grand Total All Awards = $3,286,449

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G protein-coupled estrogen receptor GPER and breast carcinogenesis

Award Number: R01CA163890

ORGANIZATION: NATIONAL CANCER INSTITUTE

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

PERIOD OF PERFORMANCE START DATE: 08/01/2012

PERIOD OF PERFORMANCE END DATE: 08/31/2025

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