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Novel artemisinin derivatives for chemogenomic profiling of Plasmodium falciparum

Award Number: SC3GM136576
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: 06/01/2020
PERIOD OF PERFORMANCE END DATE: 05/31/2024

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Novel artemisinin derivatives for chemogenomic profiling of Plasmodium falciparum - Malaria, a parasitic mosquito-borne disease, is a major concern worldwide, with 219 million cases occurring in 2017 (WHO 2018 report), causing 435,000 deaths of which 61% were children under 5. Plasmodium falciparum is the causative agent of the deadliest form of malaria and current treatment guidelines include artemisinin-based combination therapies (ACTs), combining one artemisinin derivative (artemether, artesunate or dihydroartemisinin) with one or two different drugs. Most studies have demonstrated that ACTs remain effective, but partial resistance has been reported in southeast Asia, linked to the development of the parasite’s ability to remain dormant at the ring stage long enough for clearance of artemisinin-based drugs so the parasites can re-emerge. Virtually all derivatives of artemisinin currently available are the result of chemical modifications at “C-10”, or carbon number 10 on its structure (IUPAC numbering). The fungus Cunninghamella elegans can add a hydroxyl group to carbon number 7 (C7) which, until the use of fungal transformation, was inaccessible except through extensive and costly total synthesis. The overall objective for this application is to 1) prepare C-7 derivatives of artemisinin linked with hydrophilic groups and fluorescent probes; 2) test those derivatives against a) standard P. falciparum strains (3D7, W2mef, HB3); b) at least one artemisinin-resistant phenotype (C2A) and c) test for possible anti-gametocyte action and transmission blocking activity by Standard Membrane-Feeding Assay; 3) chemogenomic profiling studies of P. falciparum piggyBac single insertion mutants seeking better understanding of the interaction of these new C7 derivatives of artemisinin with druggable targets and pathways. The central hypothesis is that derivatives of artemisinin without any steric hindrance to the peroxide group will allow full interaction with cellular targets, precisely tagging cellular structures bound to the artemisinin scaffold and enhancing inhibitory effect. These new semi-synthetic derivatives of artemisinin, built for the first time using functional groups placed structurally on the opposite side of the peroxide bridge, are expected to have enhanced antimalarial activity, present better pharmacokinetic profiles and work better as molecular probes for elucidation of mechanisms of action and drug 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: 2025 ( Subtotal = -$125,518 )
2025	2023	UNIVERSITY OF THE INCARNATE WORD	4301 BROADWAY	SAN ANTONIO	TX	78209	BEXAR	USA	Biomedical Research and Research Training	001	4	11/26/2024	SUPPLEMENT FOR EXPANSION	-$26,635
2025	2023	UNIVERSITY OF THE INCARNATE WORD	4301 BROADWAY	SAN ANTONIO	TX	78209	BEXAR	USA	Biomedical Research and Research Training	000	4	11/26/2024	NON-COMPETING CONTINUATION	-$98,884
														Subtotal = -$125,518

Issue Date FY: 2023 ( Subtotal = $134,665 )
2023	2023	UNIVERSITY OF THE INCARNATE WORD	4301 BROADWAY	SAN ANTONIO	TX	78209	BEXAR	USA	Biomedical Research and Research Training	002	4	5/31/2023	NON-COMPETING CONTINUATION	$100,749
2023	2023	UNIVERSITY OF THE INCARNATE WORD	4301 BROADWAY	SAN ANTONIO	TX	78209	BEXAR	USA	Biomedical Research and Research Training	003	4	6/6/2023	SUPPLEMENT FOR EXPANSION	$27,137
2023	2022	UNIVERSITY OF THE INCARNATE WORD	4301 BROADWAY	SAN ANTONIO	TX	78209	BEXAR	USA	Biomedical Research and Research Training	000	3	5/23/2023	NON-COMPETING CONTINUATION	$2,772
2023	2022	UNIVERSITY OF THE INCARNATE WORD	4301 BROADWAY	SAN ANTONIO	TX	78209	BEXAR	USA	Biomedical Research and Research Training	001	3	5/30/2023	SUPPLEMENT FOR EXPANSION	$4,007
														Subtotal = $134,665

Issue Date FY: 2022 ( Subtotal = $202,014 )
2022	2022	UNIVERSITY OF THE INCARNATE WORD	4301 BROADWAY	SAN ANTONIO	TX	78209	BEXAR	USA	Biomedical Research and Research Training	001	3	6/16/2022	SUPPLEMENT FOR EXPANSION	$104,542
2022	2022	UNIVERSITY OF THE INCARNATE WORD	4301 BROADWAY	SAN ANTONIO	TX	78209	BEXAR	USA	Biomedical Research and Research Training	000	3	6/14/2022	NON-COMPETING CONTINUATION	$97,472
														Subtotal = $202,014

Issue Date FY: 2021 ( Subtotal = $175,439 )
2021	2021	UNIVERSITY OF THE INCARNATE WORD	4301 BROADWAY	SAN ANTONIO	TX	78209	BEXAR	USA	Biomedical Research and Research Training	000	2	5/20/2021	NON-COMPETING CONTINUATION	$97,032
2021	2021	UNIVERSITY OF THE INCARNATE WORD	4301 BROADWAY	SAN ANTONIO	TX	78209	BEXAR	USA	Biomedical Research and Research Training	001	2	9/13/2021	SUPPLEMENT FOR EXPANSION	$78,407
														Subtotal = $175,439

Issue Date FY: 2020 ( Subtotal = $96,600 )
2020	2020	UNIVERSITY OF THE INCARNATE WORD	4301 BROADWAY	SAN ANTONIO	TX	78209	BEXAR	USA	Biomedical Research and Research Training	000	1	5/20/2020	NEW	$96,600
														Subtotal = $96,600

Grand Total All Awards = $483,200

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Novel artemisinin derivatives for chemogenomic profiling of Plasmodium falciparum

Award Number: SC3GM136576

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: 06/01/2020

PERIOD OF PERFORMANCE END DATE: 05/31/2024

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