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New analogs of the clinical complement inhibitor compstatin with subnanomolar affinity and enhanced pharmacokinetic properties.

Qu H, Ricklin D, Bai H, Chen H, Reis ES, Maciejewski M, Tzekou A, DeAngelis RA, Resuello RR, Lupu F, Barlow PN, Lambris JD.

Immunobiology. 2013 Apr;218(4):496-505. doi: 10.1016/j.imbio.2012.06.003. Epub 2012 Jun 17.


Novel analogues of the therapeutic complement inhibitor compstatin with significantly improved affinity and potency.

Qu H, Magotti P, Ricklin D, Wu EL, Kourtzelis I, Wu YQ, Kaznessis YN, Lambris JD.

Mol Immunol. 2011 Jan;48(4):481-9. doi: 10.1016/j.molimm.2010.10.004. Epub 2010 Nov 9.


Conjugation to albumin-binding molecule tags as a strategy to improve both efficacy and pharmacokinetic properties of the complement inhibitor compstatin.

Huang Y, Reis ES, Knerr PJ, van der Donk WA, Ricklin D, Lambris JD.

ChemMedChem. 2014 Oct;9(10):2223-6. doi: 10.1002/cmdc.201402212. Epub 2014 Jul 23.


C3 activation is inhibited by analogs of compstatin but not by serine protease inhibitors or peptidyl alpha-ketoheterocycles.

Furlong ST, Dutta AS, Coath MM, Gormley JJ, Hubbs SJ, Lloyd D, Mauger RC, Strimpler AM, Sylvester MA, Scott CW, Edwards PD.

Immunopharmacology. 2000 Jul 20;48(2):199-212.


A simple, yet highly accurate, QSAR model captures the complement inhibitory activity of compstatin.

Mulakala C, Lambris JD, Kaznessis Y.

Bioorg Med Chem. 2007 Feb 15;15(4):1638-44. Epub 2006 Dec 13.


Compstatin: a C3-targeted complement inhibitor reaching its prime for bedside intervention.

Mastellos DC, Yancopoulou D, Kokkinos P, Huber-Lang M, Hajishengallis G, Biglarnia AR, Lupu F, Nilsson B, Risitano AM, Ricklin D, Lambris JD.

Eur J Clin Invest. 2015 Apr;45(4):423-40. doi: 10.1111/eci.12419. Epub 2015 Mar 9. Review.


Synthesis and activity of thioether-containing analogues of the complement inhibitor compstatin.

Knerr PJ, Tzekou A, Ricklin D, Qu H, Chen H, van der Donk WA, Lambris JD.

ACS Chem Biol. 2011 Jul 15;6(7):753-60. doi: 10.1021/cb2000378. Epub 2011 May 23.


Compstatin: a complement inhibitor on its way to clinical application.

Ricklin D, Lambris JD.

Adv Exp Med Biol. 2008;632:273-92. Review.


A new generation of potent complement inhibitors of the Compstatin family.

López de Victoria A, Gorham RD Jr, Bellows-Peterson ML, Ling J, Lo DD, Floudas CA, Morikis D.

Chem Biol Drug Des. 2011 Jun;77(6):431-40. doi: 10.1111/j.1747-0285.2011.01111.x. Epub 2011 Apr 26.


Structure-kinetic relationship analysis of the therapeutic complement inhibitor compstatin.

Magotti P, Ricklin D, Qu H, Wu YQ, Kaznessis YN, Lambris JD.

J Mol Recognit. 2009 Nov-Dec;22(6):495-505. doi: 10.1002/jmr.972.


Inhibition of heparin/protamine complex-induced complement activation by Compstatin in baboons.

Soulika AM, Khan MM, Hattori T, Bowen FW, Richardson BA, Hack CE, Sahu A, Edmunds LH Jr, Lambris JD.

Clin Immunol. 2000 Sep;96(3):212-21.


New compstatin peptides containing N-terminal extensions and non-natural amino acids exhibit potent complement inhibition and improved solubility characteristics.

Gorham RD Jr, Forest DL, Khoury GA, Smadbeck J, Beecher CN, Healy ED, Tamamis P, Archontis G, Larive CK, Floudas CA, Radeke MJ, Johnson LV, Morikis D.

J Med Chem. 2015 Jan 22;58(2):814-26. doi: 10.1021/jm501345y. Epub 2014 Dec 29.


Peptide inhibitors of C3 activation as a novel strategy of complement inhibition for the treatment of paroxysmal nocturnal hemoglobinuria.

Risitano AM, Ricklin D, Huang Y, Reis ES, Chen H, Ricci P, Lin Z, Pascariello C, Raia M, Sica M, Del Vecchio L, Pane F, Lupu F, Notaro R, Resuello RR, DeAngelis RA, Lambris JD.

Blood. 2014 Mar 27;123(13):2094-101. doi: 10.1182/blood-2013-11-536573. Epub 2014 Feb 4.


Compstatin inhibits complement activation by binding to the beta-chain of complement factor 3.

Soulika AM, Holland MC, Sfyroera G, Sahu A, Lambris JD.

Mol Immunol. 2006 May;43(12):2023-9. Epub 2006 Feb 10.


Molecular dynamics in drug design: new generations of compstatin analogs.

Tamamis P, López de Victoria A, Gorham RD Jr, Bellows-Peterson ML, Pierou P, Floudas CA, Morikis D, Archontis G.

Chem Biol Drug Des. 2012 May;79(5):703-18. doi: 10.1111/j.1747-0285.2012.01324.x. Epub 2012 Feb 9.


Integrated computational and experimental approach for lead optimization and design of compstatin variants with improved activity.

Klepeis JL, Floudas CA, Morikis D, Tsokos CG, Argyropoulos E, Spruce L, Lambris JD.

J Am Chem Soc. 2003 Jul 16;125(28):8422-3.


Binding kinetics, structure-activity relationship, and biotransformation of the complement inhibitor compstatin.

Sahu A, Soulika AM, Morikis D, Spruce L, Moore WT, Lambris JD.

J Immunol. 2000 Sep 1;165(5):2491-9.


Development of a new pharmacophore model that discriminates active compstatin analogs.

Chiu TL, Mulakala C, Lambris JD, Kaznessis YN.

Chem Biol Drug Des. 2008 Oct;72(4):249-56. doi: 10.1111/j.1747-0285.2008.00709.x.


Design of a modified mouse protein with ligand binding properties of its human analog by molecular dynamics simulations: the case of C3 inhibition by compstatin.

Tamamis P, Pierou P, Mytidou C, Floudas CA, Morikis D, Archontis G.

Proteins. 2011 Nov;79(11):3166-79. doi: 10.1002/prot.23149. Epub 2011 Aug 30.


Studies of structure-activity relations of complement inhibitor compstatin.

Soulika AM, Morikis D, Sarrias MR, Roy M, Spruce LA, Sahu A, Lambris JD.

J Immunol. 2003 Aug 15;171(4):1881-90. Erratum in: J Immunol. 2004 Apr 15;172(8):following 5127.

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