Full Text Journal Articles by
Author David J Austin


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Bifunctional inhibition of HIV-1 reverse transcriptase: a first step in designing a bifunctional triphosphate.

Dongyuan Piao, Aravind Basavapathruni, Pinar Iyidogan, Guangxiu Dai, Wolfgang Hinz, Adrian S Ray, Eisuke Murakami, Joy Y Feng, Fei You, Ginger E Dutschman, David J Austin, Kathlyn A Parker, Karen S Anderson,

The onset of resistance to approved anti-AIDS drugs by HIV necessitates the search for novel inhibitors of HIV-1 reverse transcriptase (RT). Developing single molecular agents concurrently occupying the nucleoside and nonnucleoside binding sites in RT is an intriguing idea but the proof of concept has so far been elusive. As ... Read more >>

Bioorg. Med. Chem. Lett. (Bioorganic & medicinal chemistry letters)
[2013, 23(5):1511-1518]

Cited: 3 times

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Novel compounds with antiproliferative activity against imatinib-resistant cell lines.

Enrica I Lerma, Viet-Anh Nguyen, Tao Wang, Alex Tipping, Junia V Melo, Donald Kufe, David J Austin, Albert Deisseroth,

Chronic myelogenous leukemia is caused by the Bcr-Abl hybrid gene that encodes the p210Bcr-Abl chimeric oncoprotein. Although it reduces the total body burden of leukemia cells, the use of imatinib mesylate as a single agent may be accompanied by the evolution of resistance due mainly to the acquisition of point ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2007, 6(2):655-666]

Cited: 3 times

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EBP, a program for protein identification using multiple tandem mass spectrometry datasets.

Thomas S Price, Margaret B Lucitt, Weichen Wu, David J Austin, Angel Pizarro, Anastasia K Yocum, Ian A Blair, Garret A FitzGerald, Tilo Grosser,

MS/MS combined with database search methods can identify the proteins present in complex mixtures. High throughput methods that infer probable peptide sequences from enzymatically digested protein samples create a challenge in how best to aggregate the evidence for candidate proteins. Typically the results of multiple technical and/or biological replicate experiments ... Read more >>

Mol. Cell Proteomics (Molecular & cellular proteomics : MCP)
[2007, 6(3):527-536]

Cited: 33 times

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Identification of a molecular recognition role for the activation loop phosphotyrosine of the SRC tyrosine kinase.

Elizabeth J Videlock, Victor K Chung, Justin M Hall, John Hines, Christina M Agapakis, David J Austin,

A human cDNA phage display library screen, using a phosphopeptide designed to mimic the activation loop phosphotyrosine of the Src tyrosine kinase, has identified the N-terminal SH2 domain of the p85 regulatory subunit of phosphatidyl inositol-3 kinase (PI3K) as an interacting recognition domain. Activation loop phosphorylation is known to play ... Read more >>

J. Am. Chem. Soc. (Journal of the American Chemical Society)
[2005, 127(6):1600-1601]

Cited: 2 times

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Two-dimensional diversity: screening human cDNA phage display libraries with a random diversity probe for the display cloning of phosphotyrosine binding domains.

Elizabeth J Videlock, Victor K Chung, Michael A Mohan, Timothy M Strok, David J Austin,

A random phosphopeptide probe (bio-pYZZZ) has been used for the isolation and identification of multiple SH2 domains from human cDNA-displaying phage libraries. In addition, on-phage analysis and quantification of binding affinities for these phage-displayed proteins has shown them to be functional domains, retaining the same characteristics as in their native ... Read more >>

J. Am. Chem. Soc. (Journal of the American Chemical Society)
[2004, 126(12):3730-3731]

Cited: 5 times

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Right ventricle-sparing heart transplantation effective against iatrogenic pulmonary hypertension.

Constantinos Lovoulos, Shawn Tittle, Lee Goldstein, David J Austin, Simran Singh, Edward Rocco, James Keane, Ping Tang, Gary S Kopf, John A Elefteriades,

BACKGROUND: Right heart failure is the predominant cause of death following heart transplantation, occurring with disturbingly high frequency in patients with severe antecedent pulmonary hypertension. We have recently reported a novel technique of heart transplantation that spares the recipient right ventricle, excising only the recipient left ventricle. The resulting model ... Read more >>

J. Heart Lung Transplant. (The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation)
[2004, 23(2):236-241]

Cited: 4 times

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Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring.

Yashang Lee, Hosup Yeo, Shwu-Huey Liu, Zaoli Jiang, Ruben M Savizky, David J Austin, Yung-chi Cheng,

The aqueous extract of Scutellariae baicalensis Georgi has inhibitory activity against P-gp 170, a multiple drug resistant gene product. Baicalein, one of the major flavones, was found to be responsible for this activity. The hydroxyl groups of the A ring of baicalein were systematically alkylated in order to assess the ... Read more >>

J. Med. Chem. (Journal of medicinal chemistry)
[2004, 47(22):5555-5566]

Cited: 17 times

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Hypervalent iodine-mediated vicinal syn diazidation: application to the total synthesis of (+/-)-dibromophakellstatin.

Raymond Chung, Eunsun Yu, Christopher D Incarvito, David J Austin,

[reaction: see text] The total synthesis of (+/-)-dibromophakellstatin is described. The molecule is constructed from a key syn-diazide, formed by a hypervalent iodine-mediated diazidation of a dihydrodipyrrolopyrazinone ring structure. ... Read more >>

Org. Lett. (Organic letters)
[2004, 6(22):3881-3884]

Cited: 40 times

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Adenosine-anchored triphosphate subsite probing: distinguishing between HER-2 and HER-4 tyrosine protein kinases.

Fei Liu, Eric F Johnson, David J Austin, Karen S Anderson,

A strategy of full-site occupancy and stereospecific recognition in the triphosphate subsite was used to specifically inhibit two protein kinases HER-2 and HER-4 from the EGFR family. The SAR profiles of a panel of adenosine-anchored bicyclic heterocycles against HER-2 and HER-4 indicated that specificity can be derived for highly homologous ... Read more >>

Bioorg. Med. Chem. Lett. (Bioorganic & Medicinal Chemistry Letters)
[2003, 13(20):3587-3592]

Cited: 4 times

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Simultaneous identification of multiple protein targets by using complementary-DNA phage display and a natural-product-mimetic probe.

Kathleen M McKenzie, Elizabeth J Videlock, Ute Splittgerber, David J Austin,

Angew. Chem. Int. Ed. Engl. (Angewandte Chemie (International ed. in English))
[2004, 43(31):4052-4055]

Cited: 9 times

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A transient N-O-linked Pauson-Khand strategy for the synthesis of the deschloro carbocyclic core of the palau'amines and styloguanidines.

Stefan G Koenig, Stefan M Miller, Kristi A Leonard, Ralf S Löwe, Betty C Chen, David J Austin,

A stereocontrolled route to the deschloro cyclopentyl core of the palau'amines and styloguanidines has been developed. This strategy makes use of the intramolecular Pauson-Khand cyclization of an enyne with a "transient N-O tether" to construct a five-membered carbocycle in a diastereoselective fashion. [reaction: see text] ... Read more >>

Org. Lett. (Organic letters)
[2003, 5(13):2203-2206]

Cited: 20 times

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Modular evolution of a chiral auxiliary for the 1,3-dipolar cycloaddition of isomünchnones with vinyl ethers.

Sergey N Savinov, David J Austin,

[reaction: see text]. The 1,3-dipolar cycloaddition reaction has long been recognized as a powerful methodology in organic synthesis. More recently, this reaction has become a popular manifold for the construction of chemical diversity. Herein, we report the development of a chiral template for the facially selective cycloaddition of isomünchnones, a ... Read more >>

Org. Lett. (Organic letters)
[2002, 4(9):1415-1418]

Cited: 1 time

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Diastereofacial solid phase synthesis and self-promoted cleavage of a [2.2.1] bicyclic diversity scaffold.

Sergey N Savinov, David J Austin,

[reaction: see text]. We have previously described a diastereofacially selective 1,3-dipolar cycloaddition reaction of isomünchnones with vinyl ethers. While adapting this methodology for solid phase synthesis, we discovered a chemoselective and self-promoted linker aminolysis that provides liberated product in high purity, at a significantly enhanced rate. Herein we describe the ... Read more >>

Org. Lett. (Organic letters)
[2002, 4(9):1419-1422]

Cited: 3 times

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