Publications

Cancer Research. 2025 Feb 17;85(4):758-76.
A potent, selective, small-molecule inhibitor of DHX9 abrogates proliferation of microsatellite instable cancers with deficient mismatch repair.
Castro J, Daniels MH, Brennan D, Johnston B, Gotur D, Lee YT, Knockenhauer KE, Lu C, Wu J, Nayak S, Collins C.

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Advances in Biological Regulation. 2025 Nov 4:101128.
Activity and Dynamics of p110α are not Differentially Modulated by Regulatory Subunit Isoforms.
Barlow-Busch I, Walsh EE, Nyvall HG, Burke JE.

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Chemical Biology & Drug Design. 2025 Dec;106(6):e70221.
New anticancer 4‐aryldihydropyrimidinone‐5‐carboxylates targeting Hsp90.
Bordoni C, Elstow TZ, Brancale A, Clarkson RW, Westwell AD.

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Nature Cancer. 2025 January 16.
First-in-class ultralong-target-residence-time p38α inhibitors as a mitosis-targeted therapy for colorectal cancer.
Rudalska, R., Harbig, J., Forster, M. et al.

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Molecular Cancer Therapeutics. 2024 Nov 4;23(11):1568-85.
Identification of ATP-Competitive Human CMG Helicase Inhibitors for Cancer Intervention that Disrupt CMG-Replisome Function. 
Xiang S, Craig KC, Luo X, Welch DL, Ferreira RB, Lawrence HR, Lawrence NJ, Reed DR, Alexandrow MG.

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Experimental & Molecular Medicine. 2024 Feb;56(2):395-407.
The deubiquitinase USP40 preserves endothelial integrity by targeting the heat shock protein HSP90β.
Miao J, Li L, Shaheen N, Wei J, Jacko AM, Sundd P, Taleb SJ, Mallampalli RK, Zhao Y, Zhao J.

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Biochemistry. 2023 Jul 5;62(14):2147-60.
Identification of 2-sulfonyl/sulfonamide pyrimidines as covalent inhibitors of WRN using a multiplexed high-throughput screening assay. 
Parker MJ, Lee H, Yao S, Irwin S, Hwang S, Belanger K, de Mare SW, Surgenor R, Yan L, Gee P, Morla S.

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bioRxiv. 2022 July 30.
Molecular basis for differential activation of p101 and p84 complexes of PI3Kγ by Ras and GPCRs.
Rathinaswamy M, Jenkins M, Zhang X, Stariha J, Ranga-Prasad H, Dalwadi U, Fleming K, Yip C, Williams R, Burke J.

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bioRxiv. 2022 July 20.
Epinephrine inhibits PI3K alpha via the Hippo kinases.
Lin T, Ramsamooj S, Liberatore K, Lantier L, Vasan N, Karukurichi K, Hwang S, Kesicki E, Kastenhuber E, Weiderhold T, Yaron T, Zhu M, Ma Y, Paddock M, Zhang G, Hopkins B, McGuinness O, Schwartz R, Cantley L, Johnson J, Goncalves M.

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bioRxiv. 2022 April 6.
Oncogenic mutations of PIK3CA lead to increased membrane of recruitment driven by reorientation of the ABD, p85, and C-terminus.
Ranga-Prasad H, Jenkins M, Parson M, Rathinaswamy M, Burke J.

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Nature Communications. 2022 Jan 28; 13(569).
Decisive role of water and protein dynamics in residence time of p38α MAP kinase inhibitors.
Pantsar T, Kaiser P, Kudolo M, Forster M, Rothbauer U, Laufer S.

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Science Advances. 2021 Aug 27; 7(35).
Structure of the phosphoinositide 3-kinase (PI3K) p110y-p101 complex reveals molecular mechanism of GPCR activation.
Rathinaswamy M, Dalwadi U, Fleming K, Adams C, Stariha J, Pardon E, Baek M, Vadas O, Dimaio F, Burke J.

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Biomolecules. 2021 Aug 12; 11(8):1196.
Structural and Functional Insights into the Biofilm-Associated BceF Tyrosine Kinase Domain Burkholderia cepacia.
Mayer M, Matiuhin Y, Nawatha M, Tabachnikov O, Fish I, Schultz N, Dvir H, Landau M.

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Science Advances. 2021 Aug 6; 7(32).
The structural basis of bacterial manganese import.
Neville S, JÖHAMN J, Watts J, Macdermott-Opeskin H, Fairweather S, Ganio K, Hulyer A, McGrath A, Hayes A, Malcom T, Davies M, Nomura N, Iwata S, O’mara M, Maher M, McDevitt C.

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ChemBioChem. 2021 July 22; 22:3236-3253.
Enzymatic Assays to Explore Viral mRNA Capping Machinery.
Kasprzyk R, Jemielity J.

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ChemRxiv. 2021 July 20.
Jaeger-Hunting for Anti-Malarials with Generative Chemistry.
Godinez W, Ma E, Chao A, Pei L, Skewes-Cox P, Canham S, Jenkins J, Young J, Martin E, Guiguemde A.

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eLife. 2021 Mar 4; 10:e64691.
Disease-related mutations in PI3Ky disrupt regulatory C-terminal dynamics and reveal a path to selective inhibitors.
Rathinaswamy M, Gaieb Z, Fleming K, Borsari C, Harris N, Moeller B, Wymann M, Amaro R, Burke J.

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eLife. 2021 Feb 19; 10:e63524.
Molecular Structures of the Eukaryotic Retinal Importer ABCA4.
Liu F, Lee J, Chen J.

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Cancer Research. 2020 Dec 2; 80(23):5270-5281.
A Novel Inhibitor of HSP70 Induces Mitochondrial Toxicity and Immune Cell Recruitment in Tumors.
Barnoud T, Leung J, I-Ju Leu J, Basu S, Narayana Reddy Poli A, Parris J, Indeglia A, Martynyuk T, Good M, Gnanapradeepan A, Liu Q, Speicher D, Gabrilovich D, Salvino J, George D, Murphy M.

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Nature Communications. 2020 Oct 20; 11(5237)
CHIP phosphorylation by protein kinase G enhances protein quality control and attenuates cardiac ischemic injury.
Ranek M, Oeing C, Sanchez-Hodge R, Kokkonen-Simon K, Dillard D, Aslam I, Rainer P, Mishra S, Dunkerly-Erying B, Holewinski R, Virus C, Zhang H, Mannion M, Agrawal V, Hahn V, Lee D, Sasaki M, Van Eyk K, Willis M, Page R, Schisler J, Kass D.

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J Comput Aided Mol Des. 2020 June 30; 34:1091-1103.
Novel phosphatidylinositol 4-kinases III beta (PI4KIIIβ) inhibitors discovered by virtual screening using free energy models.
Colodette N, Franco L, Maia R, Fokoue H, Sant’Anna C, Barreiro E.

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Molecules. 2020 May 2; 25(9):2135.
Phenylpyrazalopyrimidines as Tyrosine Kinase Kinase Inhibitors: Synthesis, Antiproliferative Activity, and Molecular Simulations.
Chhikara B, Ashraf S, Mozaffari S, St. Jeans N, Mandal D, Tiwari R, Ul-Haq Z, Parang K.

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Structure. 2020 Feb 4; 28(2):145-156.
Defining How Oncogenic and Developmental Mutations of PIK3R1 Alter the Regulation of Class 1A Phosphoinositide 3-Kinases.
Dornan G, Stariha J, Rathinaswamy M, Powell C, Boulanger M, Burke J.

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Cell Chemical Biology. 2020 Feb 3.
Small Molecule Inhibition of CPS1 Activity through an Allosteric Pocket.
Yao S, Nguyen TV, Rolfe A, Agrawal AA, Ke J, Peng S, Colombo F, Yu S, Bouchard P, Wu J, Huang KC.

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Science. 2019 Nov 8;366(6466):714-23.
Double PIK3CA mutations in cis increase oncogenicity and sensitivity to PI3Kα inhibitors.
Vasan N, Razavi P, Johnson JL, Shao H, Shah H, Antoine A, Ladewig E, Gorelick A, Lin TY, Toska E, Xu G.

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Bioorganic & medicinal chemistry letters. 2019 Jun 15;29(12):1497-501.
Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.
Hamilton GL, Chen H, Deshmukh G, Eigenbrot C, Fong R, Johnson A, Kohli PB, Lupardus PJ, Liederer BM, Ramaswamy S, Wang H.

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bioRxiv. 2019 Jan 1:634592.
Characterisation of the c10orf76-PI4KB complex, and its necessity for Golgi PI4P levels and enterovirus replication.
McPhail JA, Lyoo H, Pemberton JG, Hoffmann RM, van Elst W, Strating JR, Jenkins ML, Stariha J, van Kuppeveld FJ, Balla T, Burke JE.

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Nature. 2018 May;557(7704):196.
Structural basis for dual-mode inhibition of the ABC transporter MsbA.
Ho H, Miu A, Alexander MK, Garcia NK, Oh A, Zilberleyb I, Reichelt M, Austin CD, Tam C, Shriver S, Hu H.

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Antimicrobial agents and chemotherapy. 2018 Apr 1;62(4):e02151-17.
A novel inhibitor of the LolCDE ABC transporter essential for lipoprotein trafficking in Gram-negative bacteria.
Nickerson NN, Jao CC, Xu Y, Quinn J, Skippington E, Alexander MK, Miu A, Skelton N, Hankins JV, Lopez MS, Koth CM.

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SLAS DISCOVERY: Advancing Life Sciences R&D. 2018 Jan;23(1):11-22.
A High-throughput screening triage workflow to authenticate a novel series of PFKFB3 inhibitors.
St-Gallay SA, Bennett N, Critchlow SE, Curtis N, Davies G, Debreczeni J, Evans N, Hardern I, Holdgate G, Jones NP, Leach L.

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SLAS DISCOVERY: Advancing Life Sciences R&D. 2017 Feb 1:2472555217695080.
A High-Throughput Method for Measuring Drug Residence Time Using the Transcreener ADP Assay.
Kumar M, Lowery RG.

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Journal of Biomolecular Screening. 2016 Oct;21(9):912-22.
Development of a 3D Tissue Culture–Based High-Content Screening Platform That Uses Phenotypic Profiling to Discriminate Selective Inhibitors of Receptor Tyrosine Kinases.
Booij TH, Klop MJ, Yan K, Szántai-Kis C, Szokol B, Orfi L, van de Water B, Keri G, Price LS.

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PloS one. 2015 Apr 14;10(4):e0124234.
Targeting Vascular Endothelial Growth Factor Receptor 2 and Protein Kinase D1 Related Pathways by a Multiple Kinase Inhibitor in Angiogenesis and Inflammation Related Processes In Vitro.
Varga A, Gyulavári P, Greff Z, Futosi K, Németh T, Simon-Szabó L, Kerekes K, Szántai-Kis C, Brauswetter D, Kokas M, Borbély G.

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Analytical Methods. 2014;6(5):1468-74.
Development of a sensitive assay for SERCA activity using FRET detection of ADP.
Jing M, Verardi R, Veglia G, Bowser MT.

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Molecular cancer therapeutics. 2014 Jun 1;13(6):1442-56.
A novel CDK9 inhibitor shows potent antitumor efficacy in preclinical hematologic tumor models.
Yin T, Lallena MJ, Kreklau EL, Fales KR, Carballares S, Torrres R, Wishart GN, Ajamie RT, Cronier DM, Iversen PW, Meier TI.

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Biochemical Journal. 2013 Aug 15;454(1):49-57.
Evolutionarily conserved structural changes in phosphatidylinositol 5-phosphate 4-kinase (PI5P4K) isoforms are responsible for differences in enzyme activity and localization.
Clarke JH, Irvine RF.

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J Biol Chem. 2013 May 23. [Epub ahead of print]
Primuline Derivatives That Mimic RNA To Stimulate Hepatitis C Virus NS3 Helicase-Catalyzed ATP Hydrolysis.
Sweeney NL, Shadrick WR, Mukherjee S, Li K, Frankowski KJ, Schoenen FJ, Frick DN.

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J Biomol Screen. 2013 Mar 27. [Epub ahead of print]
Discovering New Medicines Targeting Helicases: Challenges and Recent Progress.
Shadrick WR, Ndjomou J, Kolli R, Mukherjee S, Hanson AM, Frick DN.

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Advances in Biological Regulation. 2013 Jan 31;53(1):97-110.
Dynamic steps in receptor tyrosine kinase mediated activation of class IA phosphoinositide 3-kinases (PI3K) captured by H/D exchange (HDX-MS).
Burke JE, Williams RL.

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Assay Drug Dev Technol. 2012 Jun;10(3):260-8. Epub 2011 Dec 22.
High-Throughput Screening for RecA Inhibitors Using a Transcreener Adenosine 5′-O-Diphosphate Assay.
Peterson EJ, Janzen WP, Kireev D, Singleton SF.

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Mol Cell. 2011 Mar 4;41(5):567-78.
Structure of lipid kinase p110ß/p85ß elucidates an unusual SH2-domain-mediated inhibitory mechanism.
Zhang X, Vadas O, Perisic O, Anderson KE, Clark J, Hawkins PT, Stephens LR, Williams RL.

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Mol Biochem Parasitol. 2011 Jan: 175(1):21-29
Identification of inhibitors for putative malaria drug targets among novel antimalarial compounds
Crowther GJ, Napuli AJ, Gilligan JH, Gagaring K, Borboa R, Francek C, Chen Z, Dagostino EF, Stockmyer JB, Wang Y, Rodenbough PP, Castaneda LJ, Leibly DJ, Bhandari J, Gelb MH, Brinker A, Engels IH, Taylor J, Chatterjee AK, Fantauzzi P, Glynne RJ, Van Voorhis WC, Kuhen KL.

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J Biomol Screen. 2010 Mar;15(3):279-86. Epub 2010 Feb 10.
Detection of the ATPase activity of the molecular chaperones Hsp90 and Hsp72 using the Transcreener ADP assay kit.
Rowlands M, McAndrew C, Prodromou C, Pearl L, Kalusa A, Jones K, Workman P, Aherne W.

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J Biomol Screen. 2009; 14(7): 838-844
High-Throughput, Cell-Free, Liposome-Based Approach for Assessing In Vitro Activity of Lipid Kinases
Demian DJ, Clugston SL, Foster MM, Rameh L, Sarkes D, Townson SA, Yang L, Zhang M, Charlton ME

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J Biomol Screen. 2009; 14(6): 679-689
Efficient Elimination of Nonstoichiometric Enzyme Inhibitors from HTS Hit Lists
Habig M, Blechschmidt A, Dressler S, Hess B, Patel V, Billich A, Ostermeier C, Beer D, Klumpp M.

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Comb Chem High Throughput Screen 2009; 12(3):258-68
Development and Validation of a High-density Fluorescence Polarization-based Assay for the Trypanosoma RNA Triphosphatase TbCet1
Antczak C, Shum D, Radu C, Seshan VE, Djaballah H.

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Assay Drug Dev Technol. 2009; 7(1):56-67
Characterization and Optimization of a Red-Shifted Fluorescence Polarization ADP Detection Assay
Kleman-Leyer KM, Klink TA, Kopp AL, Westermeyer TA, Koeff MD, Larson BR, Worzella TJ, Pinchard CA, van de Kar SAT, Zaman GJR, Hornberg JJ, Lowery RG.

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J Biomol Screen. 2008; 13(6):476-485
Evaluating PI3 Kinase Isoforms Using Transcreener™ ADP Assays
Klink TA, Kleman-Leyer K, Kopp A, Westermeyer TA, Lowery RG.

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J Biomol Screen. 2007; 12(4):578-584
Development of a Transcreener™ Kinase Assay for Protein Kinase A and Demonstration of concordance of Data with a Filter-Binding Assay Format
Huss KL, Blonigen PE, Campbell RM.

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Assay Drug Dev Technol. 2007; 5:225-235
Discovery of Acetyl-Coenzyme A Carboxylase 2 Inhibitors: Comparison of a Fluorescence Intensity-Based Phosphate Assay and a Fluorescence Polarization-Based ADP Assay for High-Throughput Screening
Liu Y, Zalameda L, Kim KW, Wang M, McCarter JD.