Chemically programmed antibodies

Endothelin receptor targeting CovX-Bodies™

Venkata R. Doppalapudi, Nancy Tryder, Lingna Li, Teresa Aja, David Griffith, Francesca-Fang Liao, Giovanni Roxas, Mysore P. Ramprasad, Curt Bradshaw, Carlos F. Barbas

Research output: Contribution to journalArticle

44 Citations (Scopus)

Abstract

Aryl sulfonamide-based endothelin antagonists were synthesized and covalently linked to the reactive lysine of the m38C2 antibody to create a series of CovX-Bodies. These chemically programmed antibodies behaved as potent endothelin receptor antagonists in vitro and had antitumor efficacy in a prostate cancer xenograft model which, on a molar basis, far exceeded the activity of the parent small molecule.

Original languageEnglish (US)
Pages (from-to)501-506
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number2
DOIs
StatePublished - Jan 15 2007
Externally publishedYes

Fingerprint

Endothelin Receptors
Antibodies
Sulfonamides
Heterografts
Lysine
Prostatic Neoplasms
Molecules
Endothelin Receptor Antagonists
In Vitro Techniques

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Chemically programmed antibodies : Endothelin receptor targeting CovX-Bodies™. / Doppalapudi, Venkata R.; Tryder, Nancy; Li, Lingna; Aja, Teresa; Griffith, David; Liao, Francesca-Fang; Roxas, Giovanni; Ramprasad, Mysore P.; Bradshaw, Curt; Barbas, Carlos F.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 17, No. 2, 15.01.2007, p. 501-506.

Research output: Contribution to journalArticle

Doppalapudi, VR, Tryder, N, Li, L, Aja, T, Griffith, D, Liao, F-F, Roxas, G, Ramprasad, MP, Bradshaw, C & Barbas, CF 2007, 'Chemically programmed antibodies: Endothelin receptor targeting CovX-Bodies™', Bioorganic and Medicinal Chemistry Letters, vol. 17, no. 2, pp. 501-506. https://doi.org/10.1016/j.bmcl.2006.10.009
Doppalapudi, Venkata R. ; Tryder, Nancy ; Li, Lingna ; Aja, Teresa ; Griffith, David ; Liao, Francesca-Fang ; Roxas, Giovanni ; Ramprasad, Mysore P. ; Bradshaw, Curt ; Barbas, Carlos F. / Chemically programmed antibodies : Endothelin receptor targeting CovX-Bodies™. In: Bioorganic and Medicinal Chemistry Letters. 2007 ; Vol. 17, No. 2. pp. 501-506.
@article{1ebff4ccc6bc457dbecfde0b3f988972,
title = "Chemically programmed antibodies: Endothelin receptor targeting CovX-Bodies™",
abstract = "Aryl sulfonamide-based endothelin antagonists were synthesized and covalently linked to the reactive lysine of the m38C2 antibody to create a series of CovX-Bodies. These chemically programmed antibodies behaved as potent endothelin receptor antagonists in vitro and had antitumor efficacy in a prostate cancer xenograft model which, on a molar basis, far exceeded the activity of the parent small molecule.",
author = "Doppalapudi, {Venkata R.} and Nancy Tryder and Lingna Li and Teresa Aja and David Griffith and Francesca-Fang Liao and Giovanni Roxas and Ramprasad, {Mysore P.} and Curt Bradshaw and Barbas, {Carlos F.}",
year = "2007",
month = "1",
day = "15",
doi = "10.1016/j.bmcl.2006.10.009",
language = "English (US)",
volume = "17",
pages = "501--506",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "2",

}

TY - JOUR

T1 - Chemically programmed antibodies

T2 - Endothelin receptor targeting CovX-Bodies™

AU - Doppalapudi, Venkata R.

AU - Tryder, Nancy

AU - Li, Lingna

AU - Aja, Teresa

AU - Griffith, David

AU - Liao, Francesca-Fang

AU - Roxas, Giovanni

AU - Ramprasad, Mysore P.

AU - Bradshaw, Curt

AU - Barbas, Carlos F.

PY - 2007/1/15

Y1 - 2007/1/15

N2 - Aryl sulfonamide-based endothelin antagonists were synthesized and covalently linked to the reactive lysine of the m38C2 antibody to create a series of CovX-Bodies. These chemically programmed antibodies behaved as potent endothelin receptor antagonists in vitro and had antitumor efficacy in a prostate cancer xenograft model which, on a molar basis, far exceeded the activity of the parent small molecule.

AB - Aryl sulfonamide-based endothelin antagonists were synthesized and covalently linked to the reactive lysine of the m38C2 antibody to create a series of CovX-Bodies. These chemically programmed antibodies behaved as potent endothelin receptor antagonists in vitro and had antitumor efficacy in a prostate cancer xenograft model which, on a molar basis, far exceeded the activity of the parent small molecule.

UR - http://www.scopus.com/inward/record.url?scp=33846061734&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=33846061734&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2006.10.009

DO - 10.1016/j.bmcl.2006.10.009

M3 - Article

VL - 17

SP - 501

EP - 506

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 2

ER -