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Harnessing E3 Ligases for Cancer Therapy

Award Number: R01CA240981
ORGANIZATION: NATIONAL CANCER INSTITUTE
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 07/01/2019
PERIOD OF PERFORMANCE END DATE: 06/30/2029

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Harnessing E3 Ligases for Cancer Therapy - Targeted protein degradation (TPD) has arisen as a powerful therapeutic modality for degrading and eliminating cancer-causing proteins and has enabled potential access into classically undruggable protein targets. Two main TPD approaches currently employed include heterobifunctional Proteolysis Targeting Chimeras (PROTACs) and monovalent molecular glue degraders that both use small-molecules to induce the proximity of E3 ubiquitin ligases with target proteins to ubiquitinate and degrade specific disease targets of interest. However, there are still major bottlenecks in realizing the full potential of TPD platforms. In this proposal, we will overcome bottlenecks in cancer drug discovery by developing innovative next-generation approaches for TPD using covalent chemoproteomic strategies, including expanding upon rational chemical design strategies to discover molecular glue degraders and uncover permissive E3 ligases for TPD applications and covalently targeting and destabilizing undruggable oncogenic transcription factors.


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 = $388,151 )
2025	2025	REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE	1608 4TH ST STE 201	BERKELEY	CA	94710	ALAMEDA	USA	Cancer Biology Research	002	7	7/30/2025	NON-COMPETING CONTINUATION	$388,151
2025	2024	REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE	1608 4TH ST STE 201	BERKELEY	CA	94710	ALAMEDA	USA	Cancer Biology Research	001	6	4/10/2025	COMPETING CONTINUATION	$927
2025	2023	REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE	1608 4TH ST STE 201	BERKELEY	CA	94710	ALAMEDA	USA	Cancer Biology Research	000	5	4/10/2025	NON-COMPETING CONTINUATION	-$927
														Subtotal = $388,151

Issue Date FY: 2024 ( Subtotal = $388,151 )
2024	2024	REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE	1608 4TH ST STE 201	BERKELEY	CA	94710	ALAMEDA	USA	Cancer Biology Research	000	6	7/9/2024	COMPETING CONTINUATION	$388,151
														Subtotal = $388,151

Issue Date FY: 2023 ( Subtotal = $437,813 )
2023	2023	REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE	1608 4TH ST STE 201	BERKELEY	CA	94710	ALAMEDA	USA	Cancer Biology Research	000	5	6/30/2023	NON-COMPETING CONTINUATION	$437,813
														Subtotal = $437,813

Issue Date FY: 2022 ( Subtotal = $454,038 )
2022	2022	REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE	1608 4TH ST STE 201	BERKELEY	CA	94710	ALAMEDA	USA	Cancer Biology Research	000	4	6/30/2022	NON-COMPETING CONTINUATION	$454,038
														Subtotal = $454,038

Issue Date FY: 2021 ( Subtotal = $479,360 )
2021	2021	REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE	1608 4TH ST STE 220	BERKELEY	CA	94710	ALAMEDA	USA	Cancer Biology Research	000	3	6/30/2021	NON-COMPETING CONTINUATION	$479,360
														Subtotal = $479,360

Issue Date FY: 2020 ( Subtotal = $494,377 )
2020	2020	REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE	1608 4TH ST STE 220	BERKELEY	CA	94710	ALAMEDA	USA	Cancer Biology Research	000	2	6/29/2020	NON-COMPETING CONTINUATION	$494,377
														Subtotal = $494,377

Issue Date FY: 2019 ( Subtotal = $508,677 )
2019	2019	REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE	1608 4TH ST STE 220	BERKELEY	CA	94710	ALAMEDA	USA	Cancer Biology Research	000	1	6/28/2019	NEW	$508,677
														Subtotal = $508,677

Grand Total All Awards = $3,150,567

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Harnessing E3 Ligases for Cancer Therapy

Award Number: R01CA240981

ORGANIZATION: NATIONAL CANCER INSTITUTE

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

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

PERIOD OF PERFORMANCE START DATE: 07/01/2019

PERIOD OF PERFORMANCE END DATE: 06/30/2029

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