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Design and synthesis of nucleoside-based small molecules to inhibit phosphoglycosyl transferases

Award Number: F32GM136023
ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: FELLOWSHIP/SCHOLARSHIP/STUDENT LOANS
PERIOD OF PERFORMANCE START DATE: 02/01/2020
PERIOD OF PERFORMANCE END DATE: 07/31/2023

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Design and synthesis of nucleoside-based small molecules to inhibit phosphoglycosyl transferases - Project Summary/Abstract Antibiotic resistance is becoming an increasing threat to global health. This fellowship aims to produce inhibitor libraries that target enzymes associated with bacterial survival and ultimately antibiotic resistance. Nucleoside natural products have shown biological activity towards bacterial cell wall synthesis, making them excellent scaffolds for inhibitor development. However, the complexity of these natural products makes synthesis, controlling selectivity, and minimizing toxicity a challenge. The family of enzymes that are targeted in this proposal are monotopic phosphoglycosyl transferases (PGTs). These PGTs are enzymes that catalyze the initial step in the synthesis of glycoconjugates that are linked with bacterial virulence. Once a set of inhibitors are synthesized, they will be tested with biochemical assays with various monotopic PGTs to establish their IC50 and Kd values. However, a major limitation with antibiotic development is the inability of some inhibitors to traverse the membrane and accumulate in Gram-negative bacteria. For that reason, the inhibitors will be tested for cellular uptake in Gram-negative bacteria and quantified using liquid chromatography coupled with mass spectroscopy (LC-MS). Lastly, chemoenzymatic syntheses of a UDP-sugars, will be performed and used in combination with biochemical assays to aid in the characterization of a monotopic PGT. The culmination of the work proposed in this fellowship will contribute to the development of effective inhibitors targeting monotopic PGTs, which will provide tools to study glycoconjugate biosynthesis and ultimately aid in the fight against antibiotic resistance.


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: 2024 ( Subtotal = $0 )
2024	2023	MASSACHUSETTS INSTITUTE OF TECHNOLOGY	77 MASSACHUSETTS AVE	CAMBRIDGE	MA	02139	MIDDLESEX	USA	Biomedical Research and Research Training	000	3	5/22/2024	SUPPLEMENT FOR EXPANSION	$0
														Subtotal = $0

Issue Date FY: 2023 ( Subtotal = $35,896 )
2023	2023	MASSACHUSETTS INSTITUTE OF TECHNOLOGY	77 MASSACHUSETTS AVE	CAMBRIDGE	MA	02139	MIDDLESEX	USA	Biomedical Research and Research Training	002	3	2/13/2023	SUPPLEMENT FOR EXPANSION	$995
2023	2023	MASSACHUSETTS INSTITUTE OF TECHNOLOGY	77 MASSACHUSETTS AVE	CAMBRIDGE	MA	02139	MIDDLESEX	USA	Biomedical Research and Research Training	001	3	2/1/2023	SUPPLEMENT FOR EXPANSION	$34,901
2023	2022	MASSACHUSETTS INSTITUTE OF TECHNOLOGY	77 MASSACHUSETTS AVE	CAMBRIDGE	MA	02139	MIDDLESEX	USA	Biomedical Research and Research Training	003	3	8/15/2023	NON-COMPETING CONTINUATION	$0
2023	2022	MASSACHUSETTS INSTITUTE OF TECHNOLOGY	77 MASSACHUSETTS AVE	CAMBRIDGE	MA	02139	MIDDLESEX	USA	Biomedical Research and Research Training	000	3	1/31/2023	NON-COMPETING CONTINUATION	$0
														Subtotal = $35,896

Issue Date FY: 2022 ( Subtotal = $67,582 )
2022	2022	MASSACHUSETTS INSTITUTE OF TECHNOLOGY	77 MASSACHUSETTS AVE	CAMBRIDGE	MA	02139	MIDDLESEX	USA	Biomedical Research and Research Training	002	3	6/3/2022	NON-COMPETING CONTINUATION	$1
2022	2022	MASSACHUSETTS INSTITUTE OF TECHNOLOGY	77 MASSACHUSETTS AVE	CAMBRIDGE	MA	02139	MIDDLESEX	USA	Biomedical Research and Research Training	000	3	1/7/2022	NON-COMPETING CONTINUATION	$66,390
2022	2022	MASSACHUSETTS INSTITUTE OF TECHNOLOGY	77 MASSACHUSETTS AVE	CAMBRIDGE	MA	02139	MIDDLESEX	USA	Biomedical Research and Research Training	001	3	5/10/2022	NON-COMPETING CONTINUATION	$1,191
														Subtotal = $67,582

Issue Date FY: 2021 ( Subtotal = $65,994 )
2021	2021	MASSACHUSETTS INSTITUTE OF TECHNOLOGY	77 MASSACHUSETTS AVE	CAMBRIDGE	MA	02139	MIDDLESEX	USA	Biomedical Research and Research Training	001	2	2/3/2021	NON-COMPETING CONTINUATION	$1,068
2021	2021	MASSACHUSETTS INSTITUTE OF TECHNOLOGY	77 MASSACHUSETTS AVE	CAMBRIDGE	MA	02139	MIDDLESEX	USA	Biomedical Research and Research Training	000	2	1/14/2021	NON-COMPETING CONTINUATION	$64,926
														Subtotal = $65,994

Issue Date FY: 2020 ( Subtotal = $64,554 )
2020	2020	MASSACHUSETTS INSTITUTE OF TECHNOLOGY	77 MASSACHUSETTS AVE	CAMBRIDGE	MA	02139	MIDDLESEX	USA	Biomedical Research and Research Training	001	1	12/24/2019	NEW	$0
2020	2020	MASSACHUSETTS INSTITUTE OF TECHNOLOGY	77 MASSACHUSETTS AVE	CAMBRIDGE	MA	02139	MIDDLESEX	USA	Biomedical Research and Research Training	000	1	12/24/2019	NEW	$60,854
2020	2020	MASSACHUSETTS INSTITUTE OF TECHNOLOGY	77 MASSACHUSETTS AVE	CAMBRIDGE	MA	02139	MIDDLESEX	USA	Biomedical Research and Research Training	002	1	2/21/2020	NEW	$3,700
														Subtotal = $64,554

Grand Total All Awards = $234,026

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Design and synthesis of nucleoside-based small molecules to inhibit phosphoglycosyl transferases

Award Number: F32GM136023

ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: FELLOWSHIP/SCHOLARSHIP/STUDENT LOANS

PERIOD OF PERFORMANCE START DATE: 02/01/2020

PERIOD OF PERFORMANCE END DATE: 07/31/2023

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