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High-Throughput Screening Platform for Cancer Drug Discovery

Award Number: R33CA240191
ORGANIZATION: NATIONAL CANCER INSTITUTE
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 06/01/2020
PERIOD OF PERFORMANCE END DATE: 05/31/2024

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High-Throughput Screening Platform for Cancer Drug Discovery - Project Summary Targeted therapies have shown great promise in the treatment of cancer. High-throughput screening (HTS) campaigns have often relied on assays using labeled ligands or enzyme substrates. Artifacts associated with labeling have led to the erroneous identification of compounds that act in on the labeled substrate rather than the intended target. A label-free, solution-based HTS method will facilitate identification of compounds acting specifically on the intended targets. The goals of this proposed project are to advance development and validate this calorimetry platform as an accessible approach for high throughput ITC analysis, demonstrating its advantages to study a variety of cancer therapeutic targets. To achieve this goal, we will improve mixing of reagents in droplets, multiplex temperature readout from individual droplets, automate fluidic handling and data analysis, and validate the applicability of the improved technology to study: 1) SH2 domain/phosphopeptide interactions, 2) spleen tyrosine kinase (Syk) enzyme activity, and 3) Bromodomain/acetylated histone peptide interactions, further applied in small molecule screening. The realization of the spectro-optical calorimetry technology platform will enable full thermodynamic characterization of binding and enzymatic reactions at the throughput of 1536-well plate assays but with significantly reduced assay development time and larger numbers of repeats and analyte concentrations. The combination of increased throughput and reduced sample consumption will change the way researchers view calorimetry: rather than being seen as a technique for a limited number of high-value measurements, it will be viewed as a primary screening method for cancer therapeutic targets.


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 = -$5,957 )
2025	2022	PALO ALTO RESEARCH CENTER LLC	3333 COYOTE HILL ROAD	PALO ALTO	CA	94304	SANTA CLARA	USA	Cancer Detection and Diagnosis Research	000	3	12/9/2024	NON-COMPETING CONTINUATION	-$5,957
														Subtotal = -$5,957

Issue Date FY: 2022 ( Subtotal = $703,796 )
2022	2022	PALO ALTO RESEARCH CENTER INCORPORATED	3333 COYOTE HILL RD	PALO ALTO	CA	94304	SANTA CLARA	USA	Cancer Detection and Diagnosis Research	000	3	4/29/2022	NON-COMPETING CONTINUATION	$703,796
														Subtotal = $703,796

Issue Date FY: 2021 ( Subtotal = $669,017 )
2021	2021	PALO ALTO RESEARCH CENTER INCORPORATED	3333 COYOTE HILL RD	PALO ALTO	CA	94304	SANTA CLARA	USA	Cancer Detection and Diagnosis Research	000	2	6/16/2021	NON-COMPETING CONTINUATION	$669,017
														Subtotal = $669,017

Issue Date FY: 2020 ( Subtotal = $720,575 )
2020	2020	PALO ALTO RESEARCH CENTER INCORPORATED	3333 COYOTE HILL RD	PALO ALTO	CA	94304	SANTA CLARA	USA	Cancer Detection and Diagnosis Research	000	1	5/13/2020	NEW	$720,575
														Subtotal = $720,575

Grand Total All Awards = $2,087,431

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High-Throughput Screening Platform for Cancer Drug Discovery

Award Number: R33CA240191

ORGANIZATION: NATIONAL CANCER INSTITUTE

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

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

PERIOD OF PERFORMANCE START DATE: 06/01/2020

PERIOD OF PERFORMANCE END DATE: 05/31/2024

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