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Chaiken Research Group Publications


"Lytic Inactivation of HIV-1 by Dual Engagement of gp120 and gp41 Domains in the Virus Env Protein Trimer"
Parajuli B, Acharya K, Yu R, Ngo B, Rashad AA, Abrams CF, Chaiken IM
Biochemistry, DOI:10.1021/acs.biochem.6b00570, 2016

"Computational Evaluation of HIV-1 gp120 Conformations of Soluble Trimeric gp140 Structures as Targets for de Novo Docking of First- and Second-Generation Small-Molecule CD4 Mimics"
Moraca F, Acharya K, Melillo B, Smith AB 3rd, Chaiken I, Abrams CF
J Chem Inf Model, 6(10):2069-2079, 2016

"Impact of HIV-1 Membrane Cholesterol on Cell-Independent Lytic Inactivation and Cellular Infectivity"
Kalyana Sundaram RV, Li H, Bailey L, Rashad AA, Aneja R, Weiss K, Huynh J, Bastian AR, Papazoglou E, Abrams C, Wrenn S, Chaiken I
Biochemistry, 55(3):447-58, 2016


"Peptide triazole inactivators of HIV-1: how do they work and what is their potential?"
Chaiken I, Rashad AA
Future Med Chem, 7(17):2305-10, 2015

"Disulfide Sensitivity in the Env Protein Underlies Lytic Inactivation of HIV-1 by Peptide Triazole Thiols"
Bailey LD, Kalyana Sundaram RV, Li H, Duffy C, Aneja R, Rosemary Bastian A, Holmes AP, Kamanna K, Rashad AA, Chaiken I
ACS Chem Biol, 10(12):2861-73, 2015

"Macrocyclic Envelope Glycoprotein Antagonists that Irreversibly Inactivate HIV-1 before Host Cell Encounter"
Rashad AA, Kalyana Sundaram RV, Aneja R, Duffy C, Chaiken I
J Med Chem, 58(18):7603-8, 2015

"Peptide Triazole Inactivators of HIV-1 Utilize a Conserved Two-Cavity Binding Site at the Junction of the Inner and Outer Domains of Env gp120"
Aneja R, Rashad AA, Li H, Kalyana Sundaram RV, Duffy C, Bailey LD, Chaiken I
J Med Chem, 58(9):3843-58, 2015


"Mechanism of Multivalent Nanoparticle Encounter with HIV-1 for Potency Enhancement of Peptide Triazole Virus Inactivation"
Bastian AR, Nangarlia A, Bailey LD, Holmes A, Kalyana Sundaram RV, Ang C, Moreira DRM, Freedman K, Duffy C, Contarino M, Abrams CF, Root M, Chaiken IM
Journal of Biological Chemistry, 290(1): 529–543, 2014

"Abasic Phosphorothioate Oligomers Inhibit HIV-1 Reverse Transcription and Block Virus Transmission across Polarized Ectocervical Organ Cultures"
Fraietta JA, Mueller YM, Lozenski KL, Ratner D, Boesteanu AC, Hancock AS, Lackman-Smith C, Zentner IJ, Chaiken IM, Chung S, LeGrice SF, Snyder BA, Mankowski MK, Jones NM, Hope JL, Gupta P, Anderson SH, Wigdahl B, and Katsikis PD
Antimicrob Agents Chemotherapy. 2014 Dec; 58(12): 7056-71.

"Structure-based design, synthesis and validation of CD4-mimetic small molecule inhibitors of HIV-1 entry: conversion of a viral entry agonist to an antagonist"
Courter JR, Madani N, Sodroski J, Schön A, Freire E, Kwong PD, Hendrickson WA, Chaiken IM, LaLonde JM, and Smith AB
3rd. Accounts in Chemical Research. 2014 Apr 15;47(4):1228-37

"Covalent conjugation of a peptide triazole to HIV-1 gp120 enables intramolecular binding site occupancy"
Emileh A, Duffy C, Holmes AP, Rosemary Bastian A, Aneja R, Tuzer F, Rajagopal S, Li H, Abrams CF, and Chaiken IM
Biochemistry. 2014 Jun 3; 53(21): 3403-3414


"Mode of Action of the Sulfhydryl Group in Virolytic Peptide Triazole Thiol Inhibitors of HIV-1"
Bailey LD, Duffy C, Li H, Bastian AR, Emileh A, and Chaiken IM
Proc. of 23rd American Peptide Symposium. Prompt Scientific Publishing, San Diego, 2013. Print

"Interactions of peptide triazole thiols with Env gp120 induce irreversible breakdown and inactivation of HIV-1 virions"
Bastian AR, Contarino M, Bailey LD, Aneja R, Moreira RMD, Freedman K, McFadden K, Duffy C, Emileh A, Leslie G, Jacobson JM, Hoxie JA, and Chaiken IM
Retrovirology. 2013, 10: 153

"Click chemistry in peptide-based drug design"
Li H, Aneja R, and Chaiken I
Molecules. 2013 Aug 16;18(8):9797-817

"Chimeric Cyanovirin-MPER Recombinantly Engineered Proteins Cause Cell-Free Virolysis of HIV-1"
Contarino M, Bastian AR, Sundaram RVK, McFadden K, Duffy C, Gangupomu V, Baker M, Abrams C, and Chaiken IM
Antimicrobial Agents and Chemotherapy. (10): 4743-50, 2013

"A model of the peptide triazole entry inhibitor binding to HIV-1 gp120 and mechanism of bridging sheet disruption"
Emileh A, Tuzer F, Yeh H, Umashankara M, Moreira DR, LaLonde J, Bewley C, Abrams C, and Chaiken IM
Biochemistry. 52: 2245-2261, 2013

"Solid-State Nanopore Detection of Protein Complexes; Applications in Healthcare and Protein Kinetics"
Freedman KJ, Bastian AR, Chaiken I, and Kim MJ
Small. 2013 Mar 11; 9(5): 750-759


"Non-Natural Peptide Triazole Antagonists of HIV-1 Envelope gp120"
Kamanna K, Aneja R, Duffy C, Kubinski P, Rodrigo Moreira D, Bailey LD, McFadden K, Schӧn A, Holmes A, Tuzer F, Contarino M, Freire E, and Chaiken IM
ChemMedChem, 2012

"HIV-1 Env gp120 Structural Determinants for Peptide Triazole Dual Receptor Site Antagonism"
Tuzer F, Madani M, Kantharaju, Zentner I, LaLonde J, Holmes A, Upton E, Rajagopal S, McFadden K, Contarino M, Sodroski, and Chaiken IM
Proteins: Structure, Function, and Bioinformatics 2012, Proteins. 2013 Feb;81(2):271-90

"Antiviral Breadth and Combination Potential of Peptide Triazole HIV-1 Entry Inhibitors"
McFadden K, Fletcher P, Rossi F, Kantharaju, Umashankara M, Pirrone V, Rajagopal S, Gopi H, Krebs FC, Martin-Garcia J, Shattock, RJ, and Chaiken IM
Antimicrob Agents Chemother. 56(2): 1073-80, 2012


"Multivalent and Flexible PEG-Nitrilotriacetic Acid Derivatives for Non-covalent Protein Pegylation"
Mero A, Ishino T, Chaiken IM, Veronese FM, and Pasut G
Pharm Res. 2011 Oct;28(10):2412-21. Epub May 25 2011

"A Protein Engineering Approach Differentiates the Functional Importance of Carbohydrate Moieties of Interleukin-5 Receptor α"
Ishino T, Economou NJ, McFadden K, Zaks-Zilberman M, Jost M, Baxter S, Contarino MR, Harrington AE, Loll PJ, Pasut G, Lievens S, Tavernier J, and Chaiken IM
Biochemistry. 2011 Sep 6;50(35):7546-56. Epub Aug 10 2011

"Cell Free HIV-1 Virucidal Action by Modified Peptide Triazole Inhibitors of Env gp120"
Bastian AR, Kantharaju, McFadden K, Duffy C, Rajagopal S, Contarino M, Papazoglou E, and Chaiken IM
ChemMedChem. 6: 1-5, 2011

"Monoclonal Antibody m18 Epitopes Leading to Dual Receptor Antagonism of HIV-1 gp120"
Gift SK, McFadden K, Zentner IJ, Rajagopal S, Zhang MY, Dimitrov DS, and Chaiken IM
Biochemistry. 50: 2769–2779, 2011

"Conformational and Structural Features of HIV-1 gp120 Underlying Dual Receptor Antagonism by the Cross-Reactive Neutralizing Antibody m18"
Gift SK, Zentner I, Schon A, McFadden K, UmaShankara M, Rajagopal S, Contarino M, Duffy C, Courter JR, Zhang MY, Gershoni J, Cocklin S, Dimitrov DS, Smith AB III, Freire E, and Chaiken IM
Biochemistry. 50: 2756–2768, 2011


"The Active Core in a Triazole Peptide Dual-Site Antagonist of HIV-1 gp120"
Umashankara M, McFadden K, Zentner I, Schön A, Rajagopal S, Tuzer F, Kuriakose SA, Contarino M, Lalonde J, Freire E, and Chaiken IM
ChemMedChem. 2010

"Use of the quartz crystal microbalance to monitor ligand-induced conformational rearrangements in HIV-1 envelope protein gp120"
Lee HS, Contarino M, Umashankara M, Schon A, Freire E, Smith AB, Chaiken IM, and Penn LS
Analytical and Bioanalytical Chemistry. Volume 396, Number 3, 1143-1152. 2010


"Introducing metallocene into a triazole peptide conjugate reduces its off-rate and enhances its affinity and antiviral potency for HIV-1 gp120"
Gopi H, Cocklin S, Pirrone V, McFadden K, Tuzer F, Zentner I, Ajith S, Baxter S, Jawanda N, Krebs F, and Chaiken IM
Journal of Molecular Recognition 22: 169-174, 2009

"Isotropic display of biomolecules on CNT arrayed nanostructures"
Contarino M, Withey G, and Chaiken IM
In: Biosensing Using Nanomaterials. Arben Merkoci, editor. Wiley Interscience, 2009. pp. 39-65


"Structural determinants for affinity enhancement of a dual antagonist peptide entry inhibitor of HIV-1 envelope gp120"
Gopi H, Pirrone V, LaLonde J, Madani N, Tuzer F, Baxter S, Zentner I, Cocklin S, Miller S, Krebs F, Sodroski J, and Chaiken IM
Journal of Medicinal Chemistry 51: 2638-47, 2008

"Structure-based rationale for Interleukin 5 receptor antagonism"
Ishino T, Harrington A, Gopi H, and Chaiken IM
Current Pharmaceutical Design 14: 1231-9, 2008

"Slow-dissociation effect of common signaling subunit beta on IL5 and GM-CSF receptor assembly"
Ishino T, Harrington A, Zaks-Zilberman M, Scibek J, and Chaiken IM
Cytokine 42: 179-90, 2008

"Interleukin-5 receptor subunit oligomerization and rearrangement revealed by fluorescence resonance energy transfer imaging"
Zaks-Zilberman M, Harrington A, Ishino T, and Chaiken IM
Journal of Biological Chemistry 283: 13398-406, 2008

"Enhanced EGFR inhibition and distinct epitope recognition by EGFR antagonistic MABS C225 and 425"
Kamat V, Donaldson J, Kari C, Quadros M, Lelkes P, Chaiken I, Cocklin S, Williams J, Papazoglou E, and Ulrich R
Cancer Biology and Therapy 7: 726-33, 2008

"HIV envelope binding by macrophage-expressed gp340 promotes HIV-1 infection"
Cannon G, Yi Y, Ni H, Stoddard E, Scales DA, Van Ryk DI, Chaiken I, Malamud D, and Weissman D
Journal of Immunology 181: 2065-2070, 2008


"A recombinant allosteric lectin antagonist of HIV-1 envelope gp120 interactions"
McFadden K, Cocklin S, Gopi HN, Baxter S, Ajith S, Mahmood N, Shattock R, and Chaiken IM
Proteins: Structure, Function and Bioinformatics 67: 617-629, 2007

"Recruitment pharmacophore for Interleukin 5 receptor alpha antagonism"
Bhattacharya M, Pillalamari U, Sarkhel S, Ishino T, Urbina C, Jamerson B, and Chaiken I
Biopolymers Peptide Science 88: 83-93, 2007

"Machines and networks: protein recognition in biology"
McCourt P, Nickels J, Ishino T, and Chaiken I
In: Handbook of Biosensors and Biochips, Marks, R.S., Lowe, C., Cullen, D.C., Weetall, H. and Karube, I., Eds., John Wiley and Sons, 2007, pp; 61-81

"Broad-spectrum anti-HIV potential of a peptide HIV-1 entry inhibitor"
Cocklin S, Gopi, H, Querido B, Nimmagadda D, Kuriakose S, Cicala C, Ajith S, Baxter S, Arthos J, Martin-Garcia J, and Chaiken I
Journal of Virology 81: 3645-8, 2007


"Click chemistry on azidoproline: high-affinity dual antagonist for HIV-1 envelope glycoprotein gp120"
Gopi HN, Tirupula KC, Baxter S, Ajith S, and Chaiken IM
ChemMedChem 1: 54-57, 2006

"Asymmetric usage of antagonist charged residues derives interleukin-5 receptor recruitment but is insufficient for receptor activation"
Ishino T, Pillalamarri U, Panarello D, Bhattacharya M, Urbina C, Horvat S, Sarkhel S, Jameson B, and Chaiken IM
Biochemistry 45: 1106-1115, 2006

"Real-time monitoring of the membrane-binding and insertion properties of the cholesterol-dependent cytolysin anthrolysin O from Bacillus anthracis"
Cocklin S, Jost M, Robertson NM, Weeks SD, Weber H-W, Young E, Seal S, Zhang C, Mosser E, Loll PJ, Saunders AJ, Rest R, and Chaiken IM
Journal of Molecular Recognition 19: 354-62, 2006

"Modular, self-assembling peptide linkers for stable and regenerable carbon nanotube biosensor interfaces"
Contarino M, Sergi M, Harrington A, Lazareck A, Xu J, and Chaiken IM
Journal of Molecular Recognition 19: 363-371, 2006

"Antibody binding in proximity to retroviral envelope glycoproteins leads to a basal level of neutralization"
Yang X, Lipchina I, Cocklin S, Chaiken I, and Sodroski J
Journal of Virology, 80: 11404-8, 2006


"Receptor epitope usage by interleukin 5 mimetic peptide"
Ishino T, Urbina C, Bhattacharya M, Panarello D, and Chaiken IM
Journal of Biological Chemistry 280: 22951 22961, 2005

"Advancement and utilization of biosensors for protein interaction analysis and proteomics"
Cocklin S, Ishino T, Sergi M, Nedelkov D, Nelson R, and Chaiken IM
Protein-Protein Interactions: A Molecular Cloning Manual. E. Golemis and P. Adams, eds., Cold Spring Harbor Press, Cold Spring Harbor, NY, 377-398, 2005

"Interaction with CD4 and antibodies to CD4-induced epitopes of monomeric gp120 from a microglia-adapted human immunodeficiency virus type 1 isolate"
Martín-García J, Cocklin S, Chaiken IM, and González-Scarano F
Journal of Virology 79: 6703-6713, 2005

"Cytokine recognition of human IL5 receptor"
Ishino T, Robertson N, and Chaiken IM
Vitamins and Hormones (Litwack, G., ed) 71: 321-344, Academic Press, NY, 2005


"Mode of action for linear peptide inhibitors of HIV-1 gp120 interactions"
Biorn AC, Cocklin S, Madani N, Si Z, Ivanovic T, Samanen J, Van Ryk DI, Pantophlet R, Burton DR, Freire E, Sodroski J, and Chaiken IM
Biochemistry 43: 1928-1938, 2004

"Kinetic interaction analysis of human interleukin 5 receptor α mutants reveals a unique binding topology and charge distribution for cytokine recognition"
Ishino T, Pasut G, Scibek J, and Chaiken IM
Journal of Biological Chemistry 279: 9547-9556, 2004

"Cyclic peptide interleukin 5 antagonists mimic CD turn recognition epitope for receptor α"
Ruchala P, Varadi G, Ishino T, Scibek J, Bhattacharya M, Urbina C, Van Ryk D, Uings I, and Chaiken IM
Biopolymers 73: 556-568, 2004

"Proteins, recognition networks and developing interfaces for macromolecular biosensing"
Sergi M, Zurawski J, Cocklin S, and Chaiken I
Journal of Molecular Recognition 17: 198-208, 2004

"Small-molecule inhibitors of HIV-1 entry block receptor-induced conformational changes in the viral envelope glycoproteins"
Si Z, Madani N, Cox JM, Chruma JJ, Klein JC, Schon A, Phan N, Wang L, Biorn AB, Cocklin S, Chaiken I, Freire E, Smith AB, and Sodroski JG
Proceedings of the National Academy of Science U.S.A., 101: 5036-4, 2004

"Biosensor analysis of receptor-ligand interactions"
Wu S-J and Chaiken IM
Methods in Molecular Biology 249: 93-110, 2004

"Interactions of HIV-1 proteins gp120 and Nef with cellular partners define a novel allosteric paradigm"
Leavitt SA, Schön A, Klein JC, Manjappara U, Chaiken IM, and Freire E
Current Protein and Peptide Science, 5: 1-8, 2004

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The Chaiken Research Group investigates the fundamental nature of protein interactions in solution and in cells, and their roles in disease pathogenesis.