Thursday, June 26, 2025 6/26/2025

Late-Stage Modification of Biomolecules via Radical-Based Methods

Award Number: R01GM127778
ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 04/01/2019
PERIOD OF PERFORMANCE END DATE: 07/31/2028

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Late-Stage Modification of Biomolecules via Radical-Based Methods - Project Summary Late-stage modification of pharmaceutically relevant small molecules and biomolecules, including alcohols, peptides, and carbohydrates, is crucial in drug discovery and chemical biology research. However, achieving selectivity and specificity among the diverse functional groups present within such molecules is a primary challenge in late-stage functionalization. This proposal aims to address this challenge by leveraging the non- polar nature of radical intermediates, which exhibit orthogonal reactivity compared to the prevalent polar functional groups found in biomolecules. Specifically, a phosphoramidite reagent will selectively functionalize hydroxyl groups by enabling deoxygenative radical formation and incorporate it into various transformations, including the Giese reaction, cross-coupling, and trifluoromethylation reactions. The mild conditions and moderate electrophilicity of the phosphoramidite will offer compatibility with biomolecules rich in various reactive groups. Mechanistic studies of radical capture by nickel intermediates will inform catalyst design for stereoconvergent deoxygenative coupling of alcohols. Furthermore, understanding this fundamental step will provide insight for the design of a broader range of cross-coupling reactions involving radical intermediates generated from various means, including chemical, photoredox, and electrocatalytic activation. Finally, the proposed research aims to develop novel photoredox electron donor-acceptor coupling reactions that facilitate the synthesis of cyclic peptides, a promising strategy for drug development. These reactions will expand the chemical space accessible to drug discovery and facilitate the development of new therapeutic agents.


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 = $0 )
2025	2024	NEW YORK UNIVERSITY	70 WASHINGTON SQ S	NEW YORK	NY	10012	NEW YORK	USA	Biomedical Research and Research Training	001	6	5/7/2025	COMPETING CONTINUATION	$3,554
2025	2023	NEW YORK UNIVERSITY	70 WASHINGTON SQ S	NEW YORK	NY	10012	NEW YORK	USA	Biomedical Research and Research Training	000	5	5/7/2025	NON-COMPETING CONTINUATION	-$3,554
														Subtotal = $0

Issue Date FY: 2024 ( Subtotal = $358,367 )
2024	2024	NEW YORK UNIVERSITY	70 WASHINGTON SQ S	NEW YORK	NY	10012	NEW YORK	USA	Biomedical Research and Research Training	002	6	8/26/2024	COMPETING CONTINUATION	$358,367
2024	2023	NEW YORK UNIVERSITY	70 WASHINGTON SQ S	NEW YORK	NY	10012	NEW YORK	USA	Biomedical Research and Research Training	000	5	5/28/2024	NON-COMPETING CONTINUATION	$0
2024	2023	NEW YORK UNIVERSITY	70 WASHINGTON SQ S	NEW YORK	NY	10012	NEW YORK	USA	Biomedical Research and Research Training	001	5	8/16/2024	NON-COMPETING CONTINUATION	$0
														Subtotal = $358,367

Issue Date FY: 2023 ( Subtotal = $341,265 )
2023	2023	NEW YORK UNIVERSITY	70 WASHINGTON SQ S	NEW YORK	NY	10012	NEW YORK	USA	Biomedical Research and Research Training	000	5	3/10/2023	NON-COMPETING CONTINUATION	$341,265
														Subtotal = $341,265

Issue Date FY: 2022 ( Subtotal = $341,265 )
2022	2022	NEW YORK UNIVERSITY	70 WASHINGTON SQ S	NEW YORK	NY	10012	NEW YORK	USA	Biomedical Research and Research Training	001	4	7/21/2022	NON-COMPETING CONTINUATION	$34,127
2022	2022	NEW YORK UNIVERSITY	70 WASHINGTON SQ S	NEW YORK	NY	10012	NEW YORK	USA	Biomedical Research and Research Training	000	4	3/10/2022	NON-COMPETING CONTINUATION	$307,138
														Subtotal = $341,265

Issue Date FY: 2021 ( Subtotal = $423,529 )
2021	2021	NEW YORK UNIVERSITY	70 WASHINGTON SQ S	NEW YORK	NY	10012	NEW YORK	USA	Biomedical Research and Research Training	000	3	3/17/2021	NON-COMPETING CONTINUATION	$423,529
														Subtotal = $423,529

Issue Date FY: 2020 ( Subtotal = $556,905 )
2020	2020	NEW YORK UNIVERSITY	70 WASHINGTON SQ S	NEW YORK	NY	10012	NEW YORK	USA	Biomedical Research and Research Training	002	2	6/25/2020	SUPPLEMENT FOR EXPANSION	$52,136
2020	2020	NEW YORK UNIVERSITY	70 WASHINGTON SQ S	NEW YORK	NY	10012	NEW YORK	USA	Biomedical Research and Research Training	000	1	11/22/2019	SUPPLEMENT FOR EXPANSION	$40,945
2020	2020	NEW YORK UNIVERSITY	70 WASHINGTON SQ S	NEW YORK	NY	10012	NEW YORK	USA	Biomedical Research and Research Training	001	2	3/16/2020	NON-COMPETING CONTINUATION	$463,824
														Subtotal = $556,905

Issue Date FY: 2019 ( Subtotal = $342,004 )
2019	2019	NEW YORK UNIVERSITY	70 WASHINGTON SQ S	NEW YORK	NY	10012	NEW YORK	USA	Biomedical Research and Research Training	000	1	3/19/2019	NEW	$342,004
														Subtotal = $342,004

Grand Total All Awards = $2,363,335

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Late-Stage Modification of Biomolecules via Radical-Based Methods

Award Number: R01GM127778

ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

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

PERIOD OF PERFORMANCE START DATE: 04/01/2019

PERIOD OF PERFORMANCE END DATE: 07/31/2028

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