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Sulfur(VI) Fluoride Exchange (SuFEx): new developments and biological applications

Award Number: R35GM152118
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: 02/01/2024
PERIOD OF PERFORMANCE END DATE: 11/30/2027

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Sulfur(VI) Fluoride Exchange (SuFEx): new developments and biological applications - Project Summary/Abstract The central goal of this project is to develop new sulfur fluoride exchange (SuFEx) reactions to construct small-molecule libraries containing the SVI-F motif and to explore their in vitro and in vivo functions. SuFEx is a new family of click chemistry transformations for generating diverse chemical structures bearing the SVI-F motif, such as -OSO2F (fluorosulfate), -SO2F (sulfonyl fluoride) and iminosulfur oxydifluorides. In the last seven years, we have established three versatile SulfurVI connectors: sulfuryl fluoride (SO2F2), ethenesulfonyl fluoride (ESF), and thionyl tetrafluoride (SOF4). SO2F2 selectively reacts with the – OH group of phenols to form aryl fluorosulfates, whereas SOF4 selectively reacts with primary amines to form iminosulfur oxydifluorides. Based on the aryl fluorosulfate chemistry, we invented extremely fast fluoride exchange reactions to introduce the fluorine-18 isotope into biologically active small-molecule radiotracers for positron emission tomography. By screening aryl fluorosulfate-based libraries, we discovered small-molecule covalent modifiers for Intracellular Lipid Binding Protein(s) and a platform for the late-stage drug functionalization. Building upon the above exciting discoveries, we will develop new transformations to expand the SuFEx transformation repertory and explore the feasibility of expanding fluoride exchange reactions to stable phosphorous(V) hubs. We will apply these new chemical transformations to construct screen libraries that can be used for rapid hit-to-lead optimization and for the development of covalent inhibitors and to construct stable 18F radiotracers for PET imaging.


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 = $463,680 )
2025	2025	SCRIPPS RESEARCH INSTITUTE	10550 N TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	2	11/5/2024	NON-COMPETING CONTINUATION	$463,680
2025	2024	SCRIPPS RESEARCH INSTITUTE	10550 N TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	001	1	11/15/2024	NEW	$0
														Subtotal = $463,680

Issue Date FY: 2024 ( Subtotal = $506,800 )
2024	2024	SCRIPPS RESEARCH INSTITUTE	10550 N TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	1	1/29/2024	NEW	$506,800
														Subtotal = $506,800

Grand Total All Awards = $970,480

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Sulfur(VI) Fluoride Exchange (SuFEx): new developments and biological applications

Award Number: R35GM152118

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: 02/01/2024

PERIOD OF PERFORMANCE END DATE: 11/30/2027

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