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Development of an oral drug targeting SUMOylation

Award Number: R43CA217349
ORGANIZATION: NATIONAL CANCER INSTITUTE
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 09/18/2018
PERIOD OF PERFORMANCE END DATE: 08/31/2020

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Development of an oral drug targeting SUMOylation - c-Myc- and KRas-dependent cancers, such as colorectal cancer, represent major unmet medical needs that currently lack targeted therapy. Recent scientific advances revealed that these “undruggable” oncogenes critically depend on post-translational modification with the small ubiquitin-like modifier (SUMO) family of proteins, and inhibiting SUMOylation inhibits c-Myc and KRas. Furthermore, SUMOylation inhibition can activate anti-tumor immune responses. Genome- wide gene expression analysis has demonstrated that the SUMO activating enzyme (E1) is the most overexpressed SUMOylation-related protein in colorectal cancers tissues. SUMO E1 overexpression is also associated with cancer cell stemness and poor patient survival. This evidence makes SUMO E1 an attractive target. Therefore, we propose to develop highly selective, potent, and orally available SUMO E1 inhibitors as targeted therapies for colorectal cancer. Using a high-throughput screening campaign, we have identified a class of potent and specific SUMO E1 inhibitors suitable for development into orally available drugs, which could represent a new class of therapeutic agents. We will conduct lead optimization of these compounds and validate the resulting candidates in cellular assays of colorectal cancer, followed by pharmacokinetic and toxicity studies. In addition to colorectal cancer, which is the focus of our proposal, inhibiting SUMOylation will likely inhibit other c-Myc and KRas-dependent cancers. Thus, the potent SUMO E1 inhibitors developed in the proposed studies are expected to have a major impact on cancer research and targeted therapy.


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: 2021 ( Subtotal = $0 )
2021	2018	SUVALENT THERAPEUTICS INC.	1290 RANCHO CONEJO BLVD, STE 101F	THOUSAND OAKS	CA	91320	VENTURA	USA	Cancer Treatment Research	000	1	12/9/2020	NEW	$0
														Subtotal = $0

Issue Date FY: 2020 ( Subtotal = $0 )
2020	2018	SUMO BIOSCIENCES INC.	2265 E FOOTHILL BLVD	PASADENA	CA	91107	LOS ANGELES	USA	Cancer Treatment Research	001	1	7/6/2020	NEW	$0
2020	2018	SUMO BIOSCIENCES INC.	2265 E FOOTHILL BLVD	PASADENA	CA	91107	LOS ANGELES	USA	Cancer Treatment Research	000	1	11/7/2019	NEW	$0
														Subtotal = $0

Issue Date FY: 2018 ( Subtotal = $232,759 )
2018	2018	SUMO BIOSCIENCES INC.	2265 E FOOTHILL BLVD	PASADENA	CA	91107	LOS ANGELES	USA	Cancer Treatment Research	000	1	9/18/2018	NEW	$232,759
														Subtotal = $232,759

Grand Total All Awards = $232,759

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Development of an oral drug targeting SUMOylation

Award Number: R43CA217349

ORGANIZATION: NATIONAL CANCER INSTITUTE

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

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

PERIOD OF PERFORMANCE START DATE: 09/18/2018

PERIOD OF PERFORMANCE END DATE: 08/31/2020

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