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Jose A. Halperin, MD


  • Mahalingam P, Takrouri K, Chen T, Sahoo R, Papadopoulos E, Chen L, Wagner G, Aktas BH, Halperin JA, Chorev M.Synthesis of Rigidified eIF4E/eIF4G Inhibitor-1 (4EGI-1) Mimetic and Their in Vitro Characterization as Inhibitors of Protein-Protein Interaction.J Med Chem. 2014 Jun 4.
  • Takrouri K, Chen T, Papadopoulos E, Sahoo R, Kabha E, Chen H, Cantel S, Wagner G, Halperin JA, Aktas BH, Chorev M.Structure-activity relationship study of 4EGI-1, small molecule eIF4E/eIF4G protein-protein interaction inhibitors.Eur J Med Chem. 2014 Apr 22;77:361-77.
  • Yefidoff-Freedman R, Chen T, Sahoo R, Chen L, Wagner G, Halperin JA, Aktas BH, Chorev M.3-substituted indazoles as configurationally locked 4EGI-1 mimetics and inhibitors of the eIF4E/eIF4G interaction.Chembiochem. 2014 Mar 3;15(4):595-611.
  • Aktas BH, Qiao Y, Ozdelen E, Schubert R, Sevinc S, Harbinski F, Grubissich L, Singer S, Halperin JA.Small-Molecule targeting of translation initiation for cancer therapy.Oncotarget. 2013 Oct;4(10):1606-17.
  • Denoyelle S, Chen T, Yang H, Chen L, Zhang Y, Halperin JA, Aktas BH, Chorev M.Synthesis and SAR study of novel 3,3-diphenyl-1,3-dihydroindol-2-one derivatives as potent eIF2·GTP·Met-tRNAiMet ternary complex inhibitors.Eur J Med Chem. 2013 Nov;69:537-53.
  • Chen L, Aktas BH, Wang Y, He X, Sahoo R, Zhang N, Denoyelle S, Kabha E, Yang H, Freedman RY, Supko JG, Chorev M, Wagner G, Halperin JA.Tumor suppression by small molecule inhibitors of translation initiation.Oncotarget. 2012 Aug;3(8):869-81.
  • Hu W, Ge X, You T, Xu T, Zhang J, Wu G, Peng Z, Chorev M, Aktas BH, Halperin JA, Brown JR, Qin X.Human CD59 Inhibitor Sensitizes Rituximab-Resistant Lymphoma Cells to Complement-Mediated Cytolysis.Cancer Res. 2011 Mar 15;71(6):2298-307.
  • Wu G, Chen T, Shahsafaei A, Hu W, Bronson RT, Shi GP, Halperin JA, Aktas H, Qin X.Complement Regulator CD59 Protects Against Angiotensin II-Induced Abdominal Aortic Aneurysms in Mice.Circulation. 2010 Mar 23;121(11):1338-46.
  • Hu W, Yu Q, Hu N, Byrd D, Amet T, Shikuma C, Shiramizu B, Halperin JA, Qin X.A high-affinity inhibitor of human CD59 enhances complement-mediated virolysis of HIV-1: implications for treatment of HIV-1/AIDS.J Immunol. 2010 Jan 1;184(1):359-68.
  • Cantel S,Halperin JA,Chorev M,Scrima M,D'Ursi AM,Levy JJ,DiMarchi RD,Le Chevalier A,Rovero P,Papini AM.Side chain-to-side chain cyclization by intramolecular click reaction--building blocks, solid phase synthesis and conformational characterization.Adv Exp Med Biol. 2009;611:175-6.
  • Qin X,Hu W,Song W,Blair P,Wu G,Hu X,Song Y,Bauer S,Feelisch M,Leopold JA,Loscalzo J,Halperin JA.Balancing role of nitric oxide in complement-mediated activation of platelets from mCd59a and mCd59b double-knockout mice.Am J Hematol. 2009 Apr;84(4):221-7.
  • Wu G,Hu W,Shahsafaei A,Song W,Dobarro M,Sukhova GK,Bronson RR,Shi GP,Rother RP,Halperin JA,Qin X.Complement regulator CD59 protects against atherosclerosis by restricting the formation of complement membrane attack complex.Circ Res. 2009 Feb 27;104(4):550-8.
  • Carganico S,Rovero P,Halperin JA,Papini AM,Chorev M.Building blocks for the synthesis of post-translationally modified glycated peptides and proteins.J Pept Sci. 2009 Feb;15(2):67-71.
  • Qin X,Hu W,Song W,Grubissich L,Hu X,Wu G,Ferris S,Dobarro M,Halperin JA.Generation and phenotyping of mCd59a and mCd59b double-knockout mice.Am J Hematol. 2009 Feb;84(2):65-70.
  • Cantel S,Isaad Ale C,Scrima M,Levy JJ,DiMarchi RD,Rovero P,Halperin JA,D'Ursi AM,Papini AM,Chorev M.Synthesis and conformational analysis of a cyclic peptide obtained via i to i+4 intramolecular side-chain to side-chain azide-alkyne 1,3-dipolar cycloaddition.J Org Chem. 2008 Aug 1;73(15):5663-74.
  • Hu W, Ferris SP, Tweten RK, Wu G, Radaeva S, Gao B, Bronson RT, Halperin JA, Qin X.Rapid conditional targeted ablation of cells expressing human CD59 in transgenic mice by intermedilysin.Nat Med. 2008 Jan;14(1):98-103.
  • Hyberts SG, Heffron GJ, Tarragona NG, Solanky K, Edmonds KA, Luithardt H, Fejzo J, Chorev M, Aktas H, Colson K, Falchuk KH, Halperin JA, Wagner G.Ultrahigh-resolution (1)H-(13)C HSQC spectra of metabolite mixtures using nonlinear sampling and forward maximum entropy reconstruction.J Am Chem Soc. 2007 Apr 25;129(16):5108-16.
  • Moerke NJ, Aktas H, Chen H, Cantel S, Reibarkh MY, Fahmy A, Gross JD, Degterev A, Yuan J, Chorev M, Halperin JA, Wagner G.Small-molecule inhibition of the interaction between the translation initiation factors eIF4E and eIF4G.Cell. 2007 Jan 26;128(2):257-67.
  • Qin X, Dobarro M, Bedford SJ, Ferris S, Miranda PV, Song W, Bronson RT, Visconti PE, Halperin JA.Further characterization of reproductive abnormalities in mCd59b knockout mice: a potential new function of mCd59 in male reproduction.J Immunol. 2005 Nov 15;175(10):6294-302.
  • Halperin AC, Rigotti NA.US public universities' compliance with recommended tobacco-control policies.J Am Coll Health. 2003 Mar;51(5):181-8.
  • Palakurthi SS, Aktas H, Grubissich LM, Mortensen RM, Halperin JA.Anticancer effects of thiazolidinediones are independent of peroxisome proliferator-activated receptor gamma and mediated by inhibition of translation initiation.Cancer Res. 2001 Aug 15;61(16):6213-8.
  • Qin X, Miwa T, Aktas H, Gao M, Lee C, Qian YM, Morton CC, Shahsafaei A, Song WC, Halperin JA.Genomic structure, functional comparison, and tissue distribution of mouse Cd59a and Cd59b.Mamm Genome. 2001 Aug;12(8):582-9.
  • Qian YM, Qin X, Miwa T, Sun X, Halperin JA, Song WC.Identification and functional characterization of a new gene encoding the mouse terminal complement inhibitor CD59.J Immunol. 2000 Sep 1;165(5):2528-34.
  • Palakurthi SS, Flckiger R, Aktas H, Changolkar AK, Shahsafaei A, Harneit S, Kilic E, Halperin JA.Inhibition of translation initiation mediates the anticancer effect of the n-3 polyunsaturated fatty acid eicosapentaenoic acid.Cancer Res. 2000 Jun 1;60(11):2919-25.
  • Acosta J, Hettinga J, Flckiger R, Krumrei N, Goldfine A, Angarita L, Halperin J.Molecular basis for a link between complement and the vascular complications of diabetes.Proc Natl Acad Sci U S A. 2000 May 9;97(10):5450-5.
  • Aktas H, Flckiger R, Acosta JA, Savage JM, Palakurthi SS, Halperin JA.Depletion of intracellular Ca2+ stores, phosphorylation of eIF2alpha, and sustained inhibition of translation initiation mediate the anticancer effects of clotrimazole.Proc Natl Acad Sci U S A. 1998 Jul 7;95(14):8280-5.
  • Shen Y, Halperin JA, Benzaquen L, Lee CM.Characterization of neuronal cell death induced by complement activation.Brain Res Brain Res Protoc. 1997 May;1(2):186-94.
  • Acosta JA, Benzaquen LR, Goldstein DJ, Tosteson MT, Halperin JA.The transient pore formed by homologous terminal complement complexes functions as a bidirectional route for the transport of autocrine and paracrine signals across human cell membranes.Mol Med. 1996 Nov;2(6):755-65.
  • Benzaquen LR, Brugnara C, Byers HR, Gatton-Celli S, Halperin JA.Clotrimazole inhibits cell proliferation in vitro and in vivo.Nat Med. 1995 Jun;1(6):534-40.
  • Shen Y, Halperin JA, Lee CM.Complement-mediated neurotoxicity is regulated by homologous restriction.Brain Res. 1995 Feb 13;671(2):282-92.
  • Benzaquen LR, Nicholson-Weller A, Halperin JA.Terminal complement proteins C5b-9 release basic fibroblast growth factor and platelet-derived growth factor from endothelial cells.J Exp Med. 1994 Mar 1;179(3):985-92.
  • Berger HJ, Taratuska A, Smith TW, Halperin JA.Activated complement directly modifies the performance of isolated heart muscle cells from guinea pig and rat.Am J Physiol. 1993 Jul;265(1 Pt 2):H267-72.
  • Halperin JA, Taratuska A, Nicholson-Weller A.Terminal complement complex C5b-9 stimulates mitogenesis in 3T3 cells.J Clin Invest. 1993 May;91(5):1974-8.
  • Halperin JA, Taratuska A, Rynkiewicz M, Nicholson-Weller A.Transient changes in erythrocyte membrane permeability are induced by sublytic amounts of the complement membrane attack complex (C5b-9).Blood. 1993 Jan 1;81(1):200-5.
  • Nicholson-Weller A, Halperin JA.Membrane signaling by complement C5b-9, the membrane attack complex.Immunol Res. 1993;12(3):244-57.
  • Halperin JA, Cornelius F.A voltage-activated cation transport pathway associated with the sodium pump.Biochim Biophys Acta. 1991 Dec 9;1070(2):497-500.
  • Tosteson MT, Halperin JA, Kishi Y, Tosteson DC.Palytoxin induces an increase in the cation conductance of red cells.J Gen Physiol. 1991 Nov;98(5):969-85.
  • Halperin JA, Brugnara C, Van Ha T, Tosteson DC.Voltage-activated cation permeability in high-potassium but not low-potassium red blood cells.Am J Physiol. 1990 Jun;258(6 Pt 1):C1169-72.
  • Lorenzo AV, Taratuska A, Halperin JA.Suppression of cerebrospinal fluid (CSF) production by a Na+/K+ pump inhibitor extracted from human cerebrospinal fluid.Z Kinderchir. 1989 Dec;44 Suppl 1:24-6.
  • Halperin JA, Brugnara C, Tosteson MT, Van Ha T, Tosteson DC.Voltage-activated cation transport in human erythrocytes.Am J Physiol. 1989 Nov;257(5 Pt 1):C986-96.
  • Halperin JA, Brugnara C, Nicholson-Weller A.Ca2+-activated K+ efflux limits complement-mediated lysis of human erythrocytes.J Clin Invest. 1989 May;83(5):1466-71.
  • Halperin JA.Digitalis-like properties of an inhibitor of the Na+/K+ pump in human cerebrospinal fluid.J Neurol Sci. 1989 Apr;90(2):217-30.
  • Nicholson-Weller A, Halperin JA.Mechanisms by which the erythrocyte protects itself from complement damage.Prog Clin Biol Res. 1989;297:263-70; discussion 270-1.
  • Halperin JA, Nicholson-Weller A.Paroxysmal nocturnal hemoglobinuria. A complement-mediated disease.Complement Inflamm. 1989;6(1):65-72.
  • Halperin JA, Nicholson-Weller A, Brugnara C, Tosteson DC.Complement induces a transient increase in membrane permeability in unlysed erythrocytes.J Clin Invest. 1988 Aug;82(2):594-600.
  • Halperin JA, Riordan JF, Tosteson DC.Characteristics of an inhibitor of the Na+/K+ pump in human cerebrospinal fluid.J Biol Chem. 1988 Jan 15;263(2):646-51.
  • Halperin JA, Brugnara C, Kopin AS, Ingwall J, Tosteson DC.Properties of the Na+-K+ pump in human red cells with increased number of pump sites.J Clin Invest. 1987 Jul;80(1):128-37.
  • Halperin JA, Lobb RR.Effect of heparin-binding growth factors on monovalent cation transport in Balb/C 3T3 cells.Biochem Biophys Res Commun. 1987 Apr 14;144(1):115-22.
  • Halperin JA, Martin AM, Malave S.Increased digitalis-like activity in human cerebrospinal fluid after expansion of the extracellular fluid volume.Life Sci. 1985 Aug 12;37(6):561-6.
  • Halpern J, Schaeffer R, Galvez L, Malav S.Ouabain-like activity in human cerebrospinal fluid.Proc Natl Acad Sci U S A. 1983 Oct;80(19):6101-4.
  • Goldstein DJ, Marante Perez DJ, Gunst JP, Halperin JA.Prostaglandin E1 inhibits acute cell dehydration thirst.Pharmacol Biochem Behav. 1979 Jun;10(6):895-8.
  • Goldstein DJ, Halperin JA.Mast cell histamine and cell dehydration thirst.Nature. 1977 May 19;267(5608):250-2.