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Mechanistic studies of corepressor-mediated PPARγ transcriptional repression

Award Number: R01DK124870
ORGANIZATION: NATIONAL INSTITUTE OF DIABETES & DIGESTIVE & KIDNEY DISEASES
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 03/01/2023
PERIOD OF PERFORMANCE END DATE: 12/31/2024

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Mechanistic studies of corepressor-mediated PPARγ transcriptional repression - Peroxisome proliferator-activated receptor gamma (PPARγ) is a nuclear receptor transcription factor that regulates cellular differentiation, adipogenesis, and insulin resistance by recruiting transcriptional coregulator proteins (corepressor and coactivator proteins) to target gene promoters in a ligand-dependent manner. Structure-function approaches have defined how the transcriptionally active structural conformation and coactivator-selective functions of PPARγ are influenced by agonist ligands. However, little is known about the transcriptionally repressive conformation and corepressor-selective functions of PPARγ. Our long-term goal is to close this knowledge gap by defining how different pharmacological PPARγ ligands influence the structure and function of PPARγ between transcriptionally active and repressive states. In preliminary studies, we solved crystal structures of the PPARγ ligand-binding domain (LBD) in a transcriptionally repressive state using a unique corepressor-selective ligand, revealing a unique structural conformation that we have started to validate using solution NMR methods. In this project, we will use mechanistic studies to define how small molecule ligands impact PPARγ activation and repression on the molecular, structural, and cellular levels. Successful outcomes from our studies will define the activity-dependent conformational ensemble of the PPARγ LBD, develop ligands with enhanced corepressor-selective activity, and determine the molecular mechanisms by which corepressor-selective repressive ligands modulate PPARγ cellular functions.


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: 2025 ( Subtotal = -$763 )
2025	2023	VANDERBILT UNIVERSITY	110 21ST AVE S	NASHVILLE	TN	37203	DAVIDSON	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	000	6	4/14/2025	CHANGE OF GRANTEE / TRAINING INSTITUTION / AWARDING INSTITUTION	-$763
														Subtotal = -$763

Issue Date FY: 2024 ( Subtotal = -$158,953 )
2024	2023	UNIVERSITY OF FLORIDA	1523 UNION RD RM 207	GAINESVILLE	FL	32611	ALACHUA	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	000	5	12/4/2023	NON-COMPETING CONTINUATION	-$527,570
2024	2023	UNIVERSITY OF FLORIDA	1523 UNION RD RM 207	GAINESVILLE	FL	32611	ALACHUA	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	002	5	4/4/2024	NON-COMPETING CONTINUATION	-$1
2024	2023	VANDERBILT UNIVERSITY	110 21ST AVE S	NASHVILLE	TN	37203	DAVIDSON	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	001	6	12/5/2023	CHANGE OF GRANTEE / TRAINING INSTITUTION / AWARDING INSTITUTION	$368,617
2024	2023	VANDERBILT UNIVERSITY	110 21ST AVE S	NASHVILLE	TN	37203	DAVIDSON	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	004	6	4/4/2024	CHANGE OF GRANTEE / TRAINING INSTITUTION / AWARDING INSTITUTION	$149,132
2024	2022	UNIVERSITY OF FLORIDA	1523 UNION RD RM 207	GAINESVILLE	FL	32611	ALACHUA	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	003	4	4/4/2024	CHANGE OF GRANTEE / TRAINING INSTITUTION / AWARDING INSTITUTION	-$149,131
														Subtotal = -$158,953

Issue Date FY: 2023 ( Subtotal = $527,571 )
2023	2023	UNIVERSITY OF FLORIDA	1523 UNION RD RM 207	GAINESVILLE	FL	32611	ALACHUA	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	000	5	12/16/2022	NON-COMPETING CONTINUATION	$474,814
2023	2023	UNIVERSITY OF FLORIDA	1523 UNION RD RM 207	GAINESVILLE	FL	32611	ALACHUA	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	001	5	1/5/2023	NON-COMPETING CONTINUATION	$52,757
														Subtotal = $527,571

Issue Date FY: 2022 ( Subtotal = $527,570 )
2022	2022	SCRIPPS RESEARCH INSTITUTE, THE	130 SCRIPPS WAY	JUPITER	FL	33458	PALM BEACH	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	004	3	7/22/2022	NON-COMPETING CONTINUATION	-$1
2022	2022	SCRIPPS RESEARCH INSTITUTE, THE	130 SCRIPPS WAY	JUPITER	FL	33458	PALM BEACH	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	001	3	4/18/2022	NON-COMPETING CONTINUATION	-$454,660
2022	2022	UNIVERSITY OF FLORIDA	1523 UNION RD RM 207	GAINESVILLE	FL	32611	ALACHUA	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	005	4	7/22/2022	CHANGE OF GRANTEE / TRAINING INSTITUTION / AWARDING INSTITUTION	$94,366
2022	2022	SCRIPPS RESEARCH INSTITUTE, THE	130 SCRIPPS WAY	JUPITER	FL	33458	PALM BEACH	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	000	3	1/28/2022	NON-COMPETING CONTINUATION	$454,661
2022	2022	UNIVERSITY OF FLORIDA	1523 UNION RD RM 207	GAINESVILLE	FL	32611	ALACHUA	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	002	4	4/18/2022	CHANGE OF GRANTEE / TRAINING INSTITUTION / AWARDING INSTITUTION	$527,569
2022	2021	SCRIPPS RESEARCH INSTITUTE, THE	130 SCRIPPS WAY	JUPITER	FL	33458	PALM BEACH	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	003	2	7/22/2022	NON-COMPETING CONTINUATION	-$94,365
														Subtotal = $527,570

Issue Date FY: 2021 ( Subtotal = $505,180 )
2021	2021	SCRIPPS RESEARCH INSTITUTE, THE	130 SCRIPPS WAY	JUPITER	FL	33458	PALM BEACH	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	001	2	2/8/2021	NON-COMPETING CONTINUATION	$50,519
2021	2021	SCRIPPS RESEARCH INSTITUTE, THE	130 SCRIPPS WAY	JUPITER	FL	33458	PALM BEACH	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	000	2	12/17/2020	NON-COMPETING CONTINUATION	$454,661
														Subtotal = $505,180

Issue Date FY: 2020 ( Subtotal = $505,180 )
2020	2020	SCRIPPS RESEARCH INSTITUTE, THE	130 SCRIPPS WAY	JUPITER	FL	33458	PALM BEACH	USA	Diabetes, Digestive, and Kidney Diseases Extramural Research	000	1	2/28/2020	NEW	$505,180
														Subtotal = $505,180

Grand Total All Awards = $1,905,785

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Mechanistic studies of corepressor-mediated PPARγ transcriptional repression

Award Number: R01DK124870

ORGANIZATION: NATIONAL INSTITUTE OF DIABETES & DIGESTIVE & KIDNEY DISEASES

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

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

PERIOD OF PERFORMANCE START DATE: 03/01/2023

PERIOD OF PERFORMANCE END DATE: 12/31/2024

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