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Biomedical Applications of Expanded Porphyrins: Development of Gold-Texaphyrin Conjugates

Award Number: R01CA068682
ORGANIZATION: NATIONAL CANCER INSTITUTE
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 08/01/1990
PERIOD OF PERFORMANCE END DATE: 02/29/2024

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Biomedical Applications of Expanded Porphyrins: Development of Gold-Texaphyrin Conjugates - This is a year -25 renewal request that addresses a recognized challenge in medicinal inorganic chemistry, namely moving beyond platinum in oncology. To do this, a set of texaphyrin-gold conjugates is proposed. These systems will help overwhelm the antioxidant defense network essential to tumor growth via two overlapping mechanisms. They will also build on progress made in recent years under this grant that has led to very promising texaphyrin-platinum conjugates that display improved efficacy and reduced toxicity relative to FDA-approved agents, such as oxaliplatin. However, this proposal addresses a new challenge, namely using texaphyrins to deliver gold(I) N-heterocyclic carbene complexes to tumors. There is a strong mechanistic rationale for doing so. We have recently shown that uniquely designed, N-hetrocyclic carbene Au(I) complexes give rise to enhanced inhibition of antioxidant activity in cancer models as a result of thioredoxin reductase (TrxR) inhibition. On the other hand, texaphyrins are known to increase oxidative stress through redox cycling. This complementarity is unique and exciting. It should allow us to target the antioxidant protective network from two different directions and do so in a tumor-selective manner. To test the promise inherent in this hypothesis, we will pursue the following specific aims: Aim 1. Synthesize texaphyrin-Au(I) conjugates containing both labile and non-labile linkages. Use N- heterocyclic carbenes to control gold complexation. Aim 2. Assess the ability of the texaphyrin-Au conjugates to affect the antioxidant network. Use MTT assays to assess anti-proliferation activity in well-studied cancer cell lines and use flow cytometry to screen for oxidative stress response. Aim 3. Study texaphyrin-Au conjugate cellular uptake and compartmentalization in vitro. Use analyses of metal content (Gd, Au) and LCMS measurements of texaphyrin concentration in cellular and organ digests to confirm whole cell uptake and subcellular localization. Aim 4. Begin studies of toxicity and efficacy in vivo. Use murine models to determine the tolerability and biodistribution of the most promising texaphyrin-Au conjugates and their ability to localize to solid tumors and inhibit tumor growth in vivo.


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: 2026 ( Subtotal = $385,691 )
2026	2026	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	32	5/5/2026	NON-COMPETING CONTINUATION	$385,691
														Subtotal = $385,691

Issue Date FY: 2025 ( Subtotal = $384,959 )
2025	2025	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	001	31	7/2/2025	NON-COMPETING CONTINUATION	$384,959
2025	2021	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	29	2/24/2025	NON-COMPETING CONTINUATION	$0
														Subtotal = $384,959

Issue Date FY: 2024 ( Subtotal = $384,208 )
2024	2024	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	30	4/30/2024	COMPETING CONTINUATION	$384,208
														Subtotal = $384,208

Issue Date FY: 2023 ( Subtotal = $0 )
2023	2021	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	29	3/6/2023	NON-COMPETING CONTINUATION	$0
														Subtotal = $0

Issue Date FY: 2021 ( Subtotal = $360,416 )
2021	2021	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR MN 13	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	001	29	2/9/2021	NON-COMPETING CONTINUATION	$360,416
2021	2020	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR MN 13	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	28	11/11/2020	NON-COMPETING CONTINUATION	$0
														Subtotal = $360,416

Issue Date FY: 2020 ( Subtotal = $360,416 )
2020	2020	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR MN 13	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	28	4/10/2020	NON-COMPETING CONTINUATION	$360,416
														Subtotal = $360,416

Issue Date FY: 2019 ( Subtotal = $349,603 )
2019	2019	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR, MN 13	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	27	2/26/2019	NON-COMPETING CONTINUATION	$349,603
														Subtotal = $349,603

Issue Date FY: 2018 ( Subtotal = $360,416 )
2018	2018	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR, MN 13	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	001	26	5/23/2018	NON-COMPETING CONTINUATION	$36,042
2018	2018	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR, MN 13	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	26	2/22/2018	NON-COMPETING CONTINUATION	$324,374
														Subtotal = $360,416

Issue Date FY: 2017 ( Subtotal = $360,416 )
2017	2017	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR, MN 13	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	003	25	6/15/2017	COMPETING CONTINUATION	$17,188
2017	2017	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR, MN 13	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	001	25	3/8/2017	COMPETING CONTINUATION	$360,416
2017	2015	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR, MN 13	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	002	24	6/15/2017	NON-COMPETING CONTINUATION	-$17,188
2017	2015	UNIVERSITY OF TEXAS AT AUSTIN	110 INNER CAMPUS DR, MN 13	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	24	3/8/2017	NON-COMPETING CONTINUATION	$0
														Subtotal = $360,416

Issue Date FY: 2015 ( Subtotal = $320,588 )
2015	2015	UNIVERSITY OF TEXAS AT AUSTIN	P.O. BOX 7159	AUSTIN	TX	78713	TRAVIS	USA	Cancer Treatment Research	000	24	9/14/2015	NON-COMPETING CONTINUATION	$320,588
														Subtotal = $320,588

Issue Date FY: 2014 ( Subtotal = $310,970 )
2014	2014	UNIVERSITY OF TEXAS AT AUSTIN	P.O. BOX 7159	AUSTIN	TX	78713	TRAVIS	USA	Cancer Treatment Research	000	23	5/22/2014	NON-COMPETING CONTINUATION	$310,970
														Subtotal = $310,970

Issue Date FY: 2013 ( Subtotal = $301,027 )
2013	2013	UNIVERSITY OF TEXAS AT AUSTIN	P.O. BOX 7159	AUSTIN	TX	78713	TRAVIS	USA	Cancer Treatment Research	000	22	6/11/2013	NON-COMPETING CONTINUATION	$301,027
														Subtotal = $301,027

Issue Date FY: 2012 ( Subtotal = $319,550 )
2012	2012	UNIVERSITY OF TEXAS AT AUSTIN	P.O. BOX 7159	AUSTIN	TX	78713	TRAVIS	USA	Cancer Treatment Research	000	21	8/13/2012	COMPETING CONTINUATION	$319,550
														Subtotal = $319,550

Issue Date FY: 2010 ( Subtotal = $305,354 )
2010	2010	UNIVERSITY OF TEXAS AT AUSTIN	P.O. BOX 7159	AUSTIN	TX	78713	TRAVIS	USA	Cancer Treatment Research	000	20	5/25/2010	NON-COMPETING CONTINUATION	$305,354
														Subtotal = $305,354

Issue Date FY: 2009 ( Subtotal = $305,354 )
2009	2009	UNIVERSITY OF TEXAS AT AUSTIN	P.O. BOX 7159	AUSTIN	TX	78713	TRAVIS	USA	Cancer Treatment Research	000	19	5/1/2009	NON-COMPETING CONTINUATION	$305,354
														Subtotal = $305,354

Issue Date FY: 2008 ( Subtotal = $305,354 )
2008	2008	UNIVERSITY OF TEXAS AT AUSTIN	PO BOX 7159	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	18	5/2/2008	NON-COMPETING CONTINUATION	$305,354
														Subtotal = $305,354

Issue Date FY: 2007 ( Subtotal = $311,400 )
2007	2007	UNIVERSITY OF TEXAS AT AUSTIN	PO BOX 7159	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	17	6/4/2007	NON-COMPETING CONTINUATION	$311,400
														Subtotal = $311,400

Issue Date FY: 2006 ( Subtotal = $327,075 )
2006	2006	UNIVERSITY OF TEXAS AT AUSTIN	PO BOX 7159	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	16	8/25/2006	COMPETING CONTINUATION	$327,075
														Subtotal = $327,075

Issue Date FY: 2004 ( Subtotal = $328,185 )
2004	2004	UNIVERSITY OF TEXAS AT AUSTIN	PO BOX 7159	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	15	6/16/2004	NON-COMPETING CONTINUATION	$328,185
														Subtotal = $328,185

Issue Date FY: 2003 ( Subtotal = $328,185 )
2003	2003	UNIVERSITY OF TEXAS AT AUSTIN	PO BOX 7159	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	14		NON-COMPETING CONTINUATION	$328,185
														Subtotal = $328,185

Issue Date FY: 2002 ( Subtotal = $328,185 )
2002	2002	UNIVERSITY OF TEXAS AT AUSTIN	PO BOX 7159	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	13	8/9/2002	NON-COMPETING CONTINUATION	$328,185
														Subtotal = $328,185

Issue Date FY: 2001 ( Subtotal = $328,185 )
2001	2001	UNIVERSITY OF TEXAS AT AUSTIN	PO BOX 7159	AUSTIN	TX	78712	TRAVIS	USA	Cancer Treatment Research	000	12	7/16/2001	NON-COMPETING CONTINUATION	$328,185
														Subtotal = $328,185

Grand Total All Awards = $7,885,832

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Biomedical Applications of Expanded Porphyrins: Development of Gold-Texaphyrin Conjugates

Award Number: R01CA068682

ORGANIZATION: NATIONAL CANCER INSTITUTE

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

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

PERIOD OF PERFORMANCE START DATE: 08/01/1990

PERIOD OF PERFORMANCE END DATE: 02/29/2024

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