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Tumor-Targeted, Cytoplasmic Delivery of Large, Polar Molecules Using a pH-Low Insertion Peptide.

Svoronos AA, Bahal R, Pereira MC, Barrera FN, Deacon JC, Bosenberg M, DiMaio D, Glazer PM, Engelman DM.

Mol Pharm. 2020 Jan 13. doi: 10.1021/acs.molpharmaceut.9b00883. [Epub ahead of print]


Mapping pH at Cancer Cell Surfaces.

Wei D, Engelman DM, Reshetnyak YK, Andreev OA.

Mol Imaging Biol. 2019 Dec;21(6):1020-1025. doi: 10.1007/s11307-019-01335-4.


Bilayer Thickness and Curvature Influence Binding and Insertion of a pHLIP Peptide.

Karabadzhak AG, Weerakkody D, Deacon J, Andreev OA, Reshetnyak YK, Engelman DM.

Biophys J. 2018 May 8;114(9):2107-2115. doi: 10.1016/j.bpj.2018.03.036.


Peptides of pHLIP family for targeted intracellular and extracellular delivery of cargo molecules to tumors.

Wyatt LC, Moshnikova A, Crawford T, Engelman DM, Andreev OA, Reshetnyak YK.

Proc Natl Acad Sci U S A. 2018 Mar 20;115(12):E2811-E2818. doi: 10.1073/pnas.1715350115. Epub 2018 Mar 5.


Applications of pHLIP Technology for Cancer Imaging and Therapy: (Trends in Biotechnology 35, 653-664, 2017).

Wyatt LC, Lewis JS, Andreev OA, Reshetnyak YK, Engelman DM.

Trends Biotechnol. 2018 Dec;36(12):1300. doi: 10.1016/j.tibtech.2017.11.005. Epub 2017 Nov 30. No abstract available.


Two transmembrane dimers of the bovine papillomavirus E5 oncoprotein clamp the PDGF β receptor in an active dimeric conformation.

Karabadzhak AG, Petti LM, Barrera FN, Edwards APB, Moya-Rodríguez A, Polikanov YS, Freites JA, Tobias DJ, Engelman DM, DiMaio D.

Proc Natl Acad Sci U S A. 2017 Aug 29;114(35):E7262-E7271. doi: 10.1073/pnas.1705622114. Epub 2017 Aug 14.


Applications of pHLIP Technology for Cancer Imaging and Therapy.

Wyatt LC, Lewis JS, Andreev OA, Reshetnyak YK, Engelman DM.

Trends Biotechnol. 2017 Jul;35(7):653-664. doi: 10.1016/j.tibtech.2017.03.014. Epub 2017 Apr 21. Review. Erratum in: Trends Biotechnol. 2017 Nov 30;:.


Targeted imaging of urothelium carcinoma in human bladders by an ICG pHLIP peptide ex vivo.

Golijanin J, Amin A, Moshnikova A, Brito JM, Tran TY, Adochite RC, Andreev GO, Crawford T, Engelman DM, Andreev OA, Reshetnyak YK, Golijanin D.

Proc Natl Acad Sci U S A. 2016 Oct 18;113(42):11829-11834. Epub 2016 Sep 29.


PET Imaging of Extracellular pH in Tumors with (64)Cu- and (18)F-Labeled pHLIP Peptides: A Structure-Activity Optimization Study.

Demoin DW, Wyatt LC, Edwards KJ, Abdel-Atti D, Sarparanta M, Pourat J, Longo VA, Carlin SD, Engelman DM, Andreev OA, Reshetnyak YK, Viola-Villegas N, Lewis JS.

Bioconjug Chem. 2016 Sep 21;27(9):2014-23. doi: 10.1021/acs.bioconjchem.6b00306. Epub 2016 Jul 21.


Probe for the measurement of cell surface pH in vivo and ex vivo.

Anderson M, Moshnikova A, Engelman DM, Reshetnyak YK, Andreev OA.

Proc Natl Acad Sci U S A. 2016 Jul 19;113(29):8177-81. doi: 10.1073/pnas.1608247113. Epub 2016 Jul 5.


OncomiR or Tumor Suppressor? The Duplicity of MicroRNAs in Cancer.

Svoronos AA, Engelman DM, Slack FJ.

Cancer Res. 2016 Jul 1;76(13):3666-70. doi: 10.1158/0008-5472.CAN-16-0359. Epub 2016 Jun 20. Review.


Membranes Do Not Tell Proteins How To Fold.

Popot JL, Engelman DM.

Biochemistry. 2016 Jan 12;55(1):5-18. doi: 10.1021/acs.biochem.5b01134. Epub 2015 Dec 19. Review.


Biologically active LIL proteins built with minimal chemical diversity.

Heim EN, Marston JL, Federman RS, Edwards AP, Karabadzhak AG, Petti LM, Engelman DM, DiMaio D.

Proc Natl Acad Sci U S A. 2015 Aug 25;112(34):E4717-25. doi: 10.1073/pnas.1514230112. Epub 2015 Aug 10.


The pH low insertion peptide pHLIP Variant 3 as a novel marker of acidic malignant lesions.

Tapmeier TT, Moshnikova A, Beech J, Allen D, Kinchesh P, Smart S, Harris A, McIntyre A, Engelman DM, Andreev OA, Reshetnyak YK, Muschel RJ.

Proc Natl Acad Sci U S A. 2015 Aug 4;112(31):9710-5. doi: 10.1073/pnas.1509488112. Epub 2015 Jul 20.


Targeting acidity in diseased tissues: mechanism and applications of the membrane-inserting peptide, pHLIP.

Deacon JC, Engelman DM, Barrera FN.

Arch Biochem Biophys. 2015 Jan 1;565:40-8. doi: 10.1016/ Epub 2014 Nov 18.


MicroRNA silencing for cancer therapy targeted to the tumour microenvironment.

Cheng CJ, Bahal R, Babar IA, Pincus Z, Barrera F, Liu C, Svoronos A, Braddock DT, Glazer PM, Engelman DM, Saltzman WM, Slack FJ.

Nature. 2015 Feb 5;518(7537):107-10. doi: 10.1038/nature13905. Epub 2014 Nov 17.


pHLIP-FIRE, a cell insertion-triggered fluorescent probe for imaging tumors demonstrates targeted cargo delivery in vivo.

Karabadzhak AG, An M, Yao L, Langenbacher R, Moshnikova A, Adochite RC, Andreev OA, Reshetnyak YK, Engelman DM.

ACS Chem Biol. 2014 Nov 21;9(11):2545-53. doi: 10.1021/cb500388m. Epub 2014 Sep 10.


Mapping the homodimer interface of an optimized, artificial, transmembrane protein activator of the human erythropoietin receptor.

Cohen EB, Jun SJ, Bears Z, Barrera FN, Alonso M, Engelman DM, DiMaio D.

PLoS One. 2014 Apr 30;9(4):e95593. doi: 10.1371/journal.pone.0095593. eCollection 2014.


Understanding the pharmacological properties of a metabolic PET tracer in prostate cancer.

Viola-Villegas NT, Carlin SD, Ackerstaff E, Sevak KK, Divilov V, Serganova I, Kruchevsky N, Anderson M, Blasberg RG, Andreev OA, Engelman DM, Koutcher JA, Reshetnyak YK, Lewis JS.

Proc Natl Acad Sci U S A. 2014 May 20;111(20):7254-9. doi: 10.1073/pnas.1405240111. Epub 2014 May 1.


Targeting diseased tissues by pHLIP insertion at low cell surface pH.

Andreev OA, Engelman DM, Reshetnyak YK.

Front Physiol. 2014 Mar 13;5:97. doi: 10.3389/fphys.2014.00097. eCollection 2014. Review.


Hepatitis C virus RNA replication and virus particle assembly require specific dimerization of the NS4A protein transmembrane domain.

Kohlway A, Pirakitikulr N, Barrera FN, Potapova O, Engelman DM, Pyle AM, Lindenbach BD.

J Virol. 2014 Jan;88(1):628-42. doi: 10.1128/JVI.02052-13. Epub 2013 Oct 30.


Aspartate embedding depth affects pHLIP's insertion pKa.

Fendos J, Barrera FN, Engelman DM.

Biochemistry. 2013 Jul 9;52(27):4595-604. doi: 10.1021/bi400252k. Epub 2013 Jun 27.


Family of pH (low) insertion peptides for tumor targeting.

Weerakkody D, Moshnikova A, Thakur MS, Moshnikova V, Daniels J, Engelman DM, Andreev OA, Reshetnyak YK.

Proc Natl Acad Sci U S A. 2013 Apr 9;110(15):5834-9. doi: 10.1073/pnas.1303708110. Epub 2013 Mar 25.


Peptide targeting and imaging of damaged lung tissue in influenza-infected mice.

Li N, Yin L, Thévenin D, Yamada Y, Limmon G, Chen J, Chow VT, Engelman DM, Engelward BP.

Future Microbiol. 2013 Feb;8(2):257-69. doi: 10.2217/fmb.12.134.


pHLIP peptide targets nanogold particles to tumors.

Yao L, Daniels J, Moshnikova A, Kuznetsov S, Ahmed A, Engelman DM, Reshetnyak YK, Andreev OA.

Proc Natl Acad Sci U S A. 2013 Jan 8;110(2):465-70. doi: 10.1073/pnas.1219665110. Epub 2012 Dec 24. Erratum in: Proc Natl Acad Sci U S A. 2013 Feb 26;110(9):3651. Danniels, Jennifer [corrected to Daniels, Jennifer].


pH (low) insertion peptide (pHLIP) targets ischemic myocardium.

Sosunov EA, Anyukhovsky EP, Sosunov AA, Moshnikova A, Wijesinghe D, Engelman DM, Reshetnyak YK, Andreev OA.

Proc Natl Acad Sci U S A. 2013 Jan 2;110(1):82-6. doi: 10.1073/pnas.1220038110. Epub 2012 Dec 17.


Membrane physical properties influence transmembrane helix formation.

Barrera FN, Fendos J, Engelman DM.

Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14422-7. doi: 10.1073/pnas.1212665109. Epub 2012 Aug 20.


Modulation of the pHLIP transmembrane helix insertion pathway.

Karabadzhak AG, Weerakkody D, Wijesinghe D, Thakur MS, Engelman DM, Andreev OA, Markin VS, Reshetnyak YK.

Biophys J. 2012 Apr 18;102(8):1846-55. doi: 10.1016/j.bpj.2012.03.021.


In vivo pH imaging with (99m)Tc-pHLIP.

Macholl S, Morrison MS, Iveson P, Arbo BE, Andreev OA, Reshetnyak YK, Engelman DM, Johannesen E.

Mol Imaging Biol. 2012 Dec;14(6):725-34. doi: 10.1007/s11307-012-0549-z.


Tuning a polar molecule for selective cytoplasmic delivery by a pH (Low) insertion peptide.

Wijesinghe D, Engelman DM, Andreev OA, Reshetnyak YK.

Biochemistry. 2011 Nov 29;50(47):10215-22. doi: 10.1021/bi2009773. Epub 2011 Nov 4.


Roles of carboxyl groups in the transmembrane insertion of peptides.

Barrera FN, Weerakkody D, Anderson M, Andreev OA, Reshetnyak YK, Engelman DM.

J Mol Biol. 2011 Oct 21;413(2):359-71. doi: 10.1016/j.jmb.2011.08.010. Epub 2011 Aug 23.


Thrombopoietin receptor activation: transmembrane helix dimerization, rotation, and allosteric modulation.

Matthews EE, Thévenin D, Rogers JM, Gotow L, Lira PD, Reiter LA, Brissette WH, Engelman DM.

FASEB J. 2011 Jul;25(7):2234-44. doi: 10.1096/fj.10-178673. Epub 2011 Mar 14.


Measuring tumor aggressiveness and targeting metastatic lesions with fluorescent pHLIP.

Reshetnyak YK, Yao L, Zheng S, Kuznetsov S, Engelman DM, Andreev OA.

Mol Imaging Biol. 2011 Dec;13(6):1146-56. doi: 10.1007/s11307-010-0457-z.


The membrane-spanning domain of gp41 plays a critical role in intracellular trafficking of the HIV envelope protein.

Miyauchi K, Curran AR, Long Y, Kondo N, Iwamoto A, Engelman DM, Matsuda Z.

Retrovirology. 2010 Nov 13;7:95. doi: 10.1186/1742-4690-7-95.


pH-(low)-insertion-peptide (pHLIP) translocation of membrane impermeable phalloidin toxin inhibits cancer cell proliferation.

An M, Wijesinghe D, Andreev OA, Reshetnyak YK, Engelman DM.

Proc Natl Acad Sci U S A. 2010 Nov 23;107(47):20246-50. doi: 10.1073/pnas.1014403107. Epub 2010 Nov 3.


pH-sensitive membrane peptides (pHLIPs) as a novel class of delivery agents.

Andreev OA, Engelman DM, Reshetnyak YK.

Mol Membr Biol. 2010 Oct;27(7):341-52. doi: 10.3109/09687688.2010.509285. Epub 2010 Oct 13. Review.


Analysis of membrane proteins in metagenomics: networks of correlated environmental features and protein families.

Patel PV, Gianoulis TA, Bjornson RD, Yip KY, Engelman DM, Gerstein MB.

Genome Res. 2010 Jul;20(7):960-71. doi: 10.1101/gr.102814.109. Epub 2010 Apr 29.


pH (low) insertion peptide (pHLIP) inserts across a lipid bilayer as a helix and exits by a different path.

Andreev OA, Karabadzhak AG, Weerakkody D, Andreev GO, Engelman DM, Reshetnyak YK.

Proc Natl Acad Sci U S A. 2010 Mar 2;107(9):4081-6. doi: 10.1073/pnas.0914330107. Epub 2010 Feb 16.


Construction and genetic selection of small transmembrane proteins that activate the human erythropoietin receptor.

Cammett TJ, Jun SJ, Cohen EB, Barrera FN, Engelman DM, Dimaio D.

Proc Natl Acad Sci U S A. 2010 Feb 23;107(8):3447-52. doi: 10.1073/pnas.0915057107. Epub 2010 Feb 8.


Accurate analysis of tumor margins using a fluorescent pH Low Insertion Peptide (pHLIP).

Segala J, Engelman DM, Reshetnyak YK, Andreev OA.

Int J Mol Sci. 2009 Aug 4;10(8):3478-87. doi: 10.3390/ijms10083478.


Tuning the insertion properties of pHLIP.

Musial-Siwek M, Karabadzhak A, Andreev OA, Reshetnyak YK, Engelman DM.

Biochim Biophys Acta. 2010 Jun;1798(6):1041-6. doi: 10.1016/j.bbamem.2009.08.023. Epub 2009 Sep 18.


Computational analysis of membrane proteins: the largest class of drug targets.

Arinaminpathy Y, Khurana E, Engelman DM, Gerstein MB.

Drug Discov Today. 2009 Dec;14(23-24):1130-5. doi: 10.1016/j.drudis.2009.08.006. Epub 2009 Sep 3. Review.


pHLIP-mediated translocation of membrane-impermeable molecules into cells.

Thévenin D, An M, Engelman DM.

Chem Biol. 2009 Jul 31;16(7):754-62. doi: 10.1016/j.chembiol.2009.06.006.


Artificial transmembrane oncoproteins smaller than the bovine papillomavirus E5 protein redefine sequence requirements for activation of the platelet-derived growth factor beta receptor.

Talbert-Slagle K, Marlatt S, Barrera FN, Khurana E, Oates J, Gerstein M, Engelman DM, Dixon AM, Dimaio D.

J Virol. 2009 Oct;83(19):9773-85. doi: 10.1128/JVI.00946-09. Epub 2009 Jul 15.


Molecular dynamics studies of the transmembrane domain of gp41 from HIV-1.

Kim JH, Hartley TL, Curran AR, Engelman DM.

Biochim Biophys Acta. 2009 Sep;1788(9):1804-12. doi: 10.1016/j.bbamem.2009.06.011. Epub 2009 Jun 21.


A novel technology for the imaging of acidic prostate tumors by positron emission tomography.

Vāvere AL, Biddlecombe GB, Spees WM, Garbow JR, Wijesinghe D, Andreev OA, Engelman DM, Reshetnyak YK, Lewis JS.

Cancer Res. 2009 May 15;69(10):4510-6. doi: 10.1158/0008-5472.CAN-08-3781. Epub 2009 May 5.


Energetics of peptide (pHLIP) binding to and folding across a lipid bilayer membrane.

Reshetnyak YK, Andreev OA, Segala M, Markin VS, Engelman DM.

Proc Natl Acad Sci U S A. 2008 Oct 7;105(40):15340-5. doi: 10.1073/pnas.0804746105. Epub 2008 Sep 30.


Bilayer interactions of pHLIP, a peptide that can deliver drugs and target tumors.

Zoonens M, Reshetnyak YK, Engelman DM.

Biophys J. 2008 Jul;95(1):225-35. doi: 10.1529/biophysj.107.124156. Epub 2008 Mar 21.


Protein area occupancy at the center of the red blood cell membrane.

Dupuy AD, Engelman DM.

Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):2848-52. doi: 10.1073/pnas.0712379105. Epub 2008 Feb 19.

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