Prodrug strategies to improve the oral absorption of peptide mimetics

Ronald T. Borchardt; Gian Camenisch; Erin Hugger; Wei Wang; David C. Sane; Guy L. Wheeler; Che Ping Cheng; Binghe Wang

Prodrug strategies to improve the oral absorption of peptide mimetics

Ronald T. Borchardt, Gian Camenisch, Erin Hugger, Wei Wang, David C. Sane, Guy L. Wheeler, Che Ping Cheng, Binghe Wang

Research output: Contribution to journal › Conference article › peer-review

Abstract

Coumarine acid linker was used to prepare cyclic prodrugs of the RGD peptide mimetic MK-383 and several of its analogs. The corresponding cyclic prodrugs were designed to be sensitive to esterases and underwent bioconversion. These cyclic prodrugs have physicochemical properties that enhanced the cell membrane permeation and underwent bioconversion in blood and tissues to the RGD peptide mimetics. The cyclic coumarinic acid-bases prodrug of the RGD peptide mimetic MK-383 exhibited potent antithrombotic activity when orally administered to dogs.

Original language	English (US)
Pages (from-to)	257-258
Number of pages	2
Journal	American Chemical Society, Polymer Preprints, Division of Polymer Chemistry
Volume	40
Issue number	1
State	Published - Mar 1999
Externally published	Yes
Event	Proceedings of the 1999 ACS Anaheim Meeting - Anaheim, CA, USA Duration: Mar 21 1999 → Mar 25 1999

ASJC Scopus subject areas

Polymers and Plastics

Cite this

Prodrug strategies to improve the oral absorption of peptide mimetics. / Borchardt, Ronald T.; Camenisch, Gian; Hugger, Erin; Wang, Wei; Sane, David C.; Wheeler, Guy L.; Cheng, Che Ping; Wang, Binghe.

In: American Chemical Society, Polymer Preprints, Division of Polymer Chemistry, Vol. 40, No. 1, 03.1999, p. 257-258.

Research output: Contribution to journal › Conference article › peer-review

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abstract = "Coumarine acid linker was used to prepare cyclic prodrugs of the RGD peptide mimetic MK-383 and several of its analogs. The corresponding cyclic prodrugs were designed to be sensitive to esterases and underwent bioconversion. These cyclic prodrugs have physicochemical properties that enhanced the cell membrane permeation and underwent bioconversion in blood and tissues to the RGD peptide mimetics. The cyclic coumarinic acid-bases prodrug of the RGD peptide mimetic MK-383 exhibited potent antithrombotic activity when orally administered to dogs.",

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AU - Borchardt, Ronald T.

AU - Camenisch, Gian

AU - Hugger, Erin

AU - Wang, Wei

AU - Sane, David C.

AU - Wheeler, Guy L.

AU - Cheng, Che Ping

AU - Wang, Binghe

PY - 1999/3

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N2 - Coumarine acid linker was used to prepare cyclic prodrugs of the RGD peptide mimetic MK-383 and several of its analogs. The corresponding cyclic prodrugs were designed to be sensitive to esterases and underwent bioconversion. These cyclic prodrugs have physicochemical properties that enhanced the cell membrane permeation and underwent bioconversion in blood and tissues to the RGD peptide mimetics. The cyclic coumarinic acid-bases prodrug of the RGD peptide mimetic MK-383 exhibited potent antithrombotic activity when orally administered to dogs.

AB - Coumarine acid linker was used to prepare cyclic prodrugs of the RGD peptide mimetic MK-383 and several of its analogs. The corresponding cyclic prodrugs were designed to be sensitive to esterases and underwent bioconversion. These cyclic prodrugs have physicochemical properties that enhanced the cell membrane permeation and underwent bioconversion in blood and tissues to the RGD peptide mimetics. The cyclic coumarinic acid-bases prodrug of the RGD peptide mimetic MK-383 exhibited potent antithrombotic activity when orally administered to dogs.

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M3 - Conference article

AN - SCOPUS:0033089490

VL - 40

SP - 257

EP - 258

JO - American Chemical Society, Polymer Preprints, Division of Polymer Chemistry

JF - American Chemical Society, Polymer Preprints, Division of Polymer Chemistry

SN - 0032-3934

IS - 1

T2 - Proceedings of the 1999 ACS Anaheim Meeting

Y2 - 21 March 1999 through 25 March 1999

ER -

Prodrug strategies to improve the oral absorption of peptide mimetics

Abstract

ASJC Scopus subject areas

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