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Follow the Mutations: Toward Class-Specific, Small-Molecule Reactivation of p53.

Loh SN.

Biomolecules. 2020 Feb 14;10(2). pii: E303. doi: 10.3390/biom10020303. Review.


A Single Protein Disruption Site Results in Efficient Reassembly by Multiple Engineering Methods.

Ha JH, Presti MF, Loh SN.

Biophys J. 2019 Jul 9;117(1):56-65. doi: 10.1016/j.bpj.2019.06.002. Epub 2019 Jun 7.


Combinatorial Therapy of Zinc Metallochaperones with Mutant p53 Reactivation and Diminished Copper Binding.

Zaman S, Yu X, Bencivenga AF, Blanden AR, Liu Y, Withers T, Na B, Blayney AJ, Gilleran J, Boothman DA, Loh SN, Kimball SD, Carpizo DR.

Mol Cancer Ther. 2019 Aug;18(8):1355-1365. doi: 10.1158/1535-7163.MCT-18-1080. Epub 2019 Jun 13.


Zinc Metallochaperones Reactivate Mutant p53 Using an ON/OFF Switch Mechanism: A New Paradigm in Cancer Therapeutics.

Yu X, Kogan S, Chen Y, Tsang AT, Withers T, Lin H, Gilleran J, Buckley B, Moore D, Bertino J, Chan C, Kimball SD, Loh SN, Carpizo DR.

Clin Cancer Res. 2018 Sep 15;24(18):4505-4517. doi: 10.1158/1078-0432.CCR-18-0822. Epub 2018 Jun 18.


Large enhancement of response times of a protein conformational switch by computational design.

DeGrave AJ, Ha JH, Loh SN, Chong LT.

Nat Commun. 2018 Mar 9;9(1):1013. doi: 10.1038/s41467-018-03228-6.


Tumor suppressor Tsc1 is a new Hsp90 co-chaperone that facilitates folding of kinase and non-kinase clients.

Woodford MR, Sager RA, Marris E, Dunn DM, Blanden AR, Murphy RL, Rensing N, Shapiro O, Panaretou B, Prodromou C, Loh SN, Gutmann DH, Bourboulia D, Bratslavsky G, Wong M, Mollapour M.

EMBO J. 2017 Dec 15;36(24):3650-3665. doi: 10.15252/embj.201796700. Epub 2017 Nov 10.


Quantification of Membrane Protein-Detergent Complex Interactions.

Wolfe AJ, Si W, Zhang Z, Blanden AR, Hsueh YC, Gugel JF, Pham B, Chen M, Loh SN, Rozovsky S, Aksimentiev A, Movileanu L.

J Phys Chem B. 2017 Nov 9;121(44):10228-10241. doi: 10.1021/acs.jpcb.7b08045. Epub 2017 Oct 31.


Interrogating Detergent Desolvation of Nanopore-Forming Proteins by Fluorescence Polarization Spectroscopy.

Wolfe AJ, Hsueh YC, Blanden AR, Mohammad MM, Pham B, Thakur AK, Loh SN, Chen M, Movileanu L.

Anal Chem. 2017 Aug 1;89(15):8013-8020. doi: 10.1021/acs.analchem.7b01339. Epub 2017 Jul 10.


Thiosemicarbazones Functioning as Zinc Metallochaperones to Reactivate Mutant p53.

Yu X, Blanden A, Tsang AT, Zaman S, Liu Y, Gilleran J, Bencivenga AF, Kimball SD, Loh SN, Carpizo DR.

Mol Pharmacol. 2017 Jun;91(6):567-575. doi: 10.1124/mol.116.107409. Epub 2017 Mar 20.


Construction of Allosteric Protein Switches by Alternate Frame Folding and Intermolecular Fragment Exchange.

Ha JH, Loh SN.

Methods Mol Biol. 2017;1596:27-41. doi: 10.1007/978-1-4939-6940-1_2.


Small Molecule-Induced Domain Swapping as a Mechanism for Controlling Protein Function and Assembly.

Karchin JM, Ha JH, Namitz KE, Cosgrove MS, Loh SN.

Sci Rep. 2017 Mar 13;7:44388. doi: 10.1038/srep44388.


Corrigendum to "Reactivating mutant p53 using small molecules as zinc metallochaperones: awakening a sleeping giant in cancer" [Drug Discov. Today 20 (11) (2015) 1391-1397].

Blanden AR, Yu X, Loh SN, Levine AJ, Carpizo DR.

Drug Discov Today. 2016 Oct;21(10):1728. doi: 10.1016/j.drudis.2016.07.012. Epub 2016 Jul 29. No abstract available.


The FNIP co-chaperones decelerate the Hsp90 chaperone cycle and enhance drug binding.

Woodford MR, Dunn DM, Blanden AR, Capriotti D, Loiselle D, Prodromou C, Panaretou B, Hughes PF, Smith A, Ackerman W, Haystead TA, Loh SN, Bourboulia D, Schmidt LS, Marston Linehan W, Bratslavsky G, Mollapour M.

Nat Commun. 2016 Jun 29;7:12037. doi: 10.1038/ncomms12037.


Engineered Domain Swapping as an On/Off Switch for Protein Function.

Ha JH, Karchin JM, Walker-Kopp N, CastaƱeda CA, Loh SN.

Chem Biol. 2015 Oct 22;22(10):1384-93. doi: 10.1016/j.chembiol.2015.09.007.


Reactivating mutant p53 using small molecules as zinc metallochaperones: awakening a sleeping giant in cancer.

Blanden AR, Yu X, Loh SN, Levine AJ, Carpizo DR.

Drug Discov Today. 2015 Nov;20(11):1391-7. doi: 10.1016/j.drudis.2015.07.006. Epub 2015 Jul 20. Review. Erratum in: Drug Discov Today. 2016 Oct;21(10 ):1728.


Synthetic metallochaperone ZMC1 rescues mutant p53 conformation by transporting zinc into cells as an ionophore.

Blanden AR, Yu X, Wolfe AJ, Gilleran JA, Augeri DJ, O'Dell RS, Olson EC, Kimball SD, Emge TJ, Movileanu L, Carpizo DR, Loh SN.

Mol Pharmacol. 2015 May;87(5):825-31. doi: 10.1124/mol.114.097550. Epub 2015 Feb 20. Erratum in: Mol Pharmacol. 2015 Dec;88(6):1084.


Small molecule restoration of wildtype structure and function of mutant p53 using a novel zinc-metallochaperone based mechanism.

Yu X, Blanden AR, Narayanan S, Jayakumar L, Lubin D, Augeri D, Kimball SD, Loh SN, Carpizo DR.

Oncotarget. 2014 Oct 15;5(19):8879-92.


Converting a binding protein into a biosensing conformational switch using protein fragment exchange.

Zheng H, Bi J, Krendel M, Loh SN.

Biochemistry. 2014 Sep 2;53(34):5505-14. doi: 10.1021/bi500758u. Epub 2014 Aug 13.


Stepwise conversion of a binding protein to a fluorescent switch: application to Thermoanaerobacter tengcongensis ribose binding protein.

Ha JH, Shinsky SA, Loh SN.

Biochemistry. 2013 Jan 29;52(4):600-12. doi: 10.1021/bi301105u. Epub 2013 Jan 17.


Protein conformational switches: from nature to design.

Ha JH, Loh SN.

Chemistry. 2012 Jun 25;18(26):7984-99. doi: 10.1002/chem.201200348. Epub 2012 Jun 11. Review.

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