Search Results - "Borchardt, R.T."

Transport characteristics of peptides and peptidomimetics: I. N-methylated peptides as substrates for the oligopeptide transporter and P-glycoprotein in the intestinal mucosa by Gao, J., Sudoh, M., Borchardt, R.T., Aubé, J.

“…: Peptides and peptidomimetics often exhibit poor oral bioavailability due to their metabolic instability and low permeation across the intestinal mucosa…”
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Synthesis and evaluation of the physicochemical properties of esterase-sensitive cyclic prodrugs of opioid peptides using coumarinic acid and phenylpropionic acid linkers by Wang, B., Wang, W., Zhang, H., Shan, D., Nimkar, K., Gudmundsson, O., Gangwar, S., Siahaan, T., Borchardt, R.T.

“…: In an attempt to improve the membrane permeabilities of opioid peptides, we have synthesized cyclic prodrugs of [Leu5]‐enkephalin and DADLE using a…”
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Transport characteristics of peptides and peptidomimetics: II. Hydroxyethylamine bioisostere-containing peptidomimetics as substrates for the oligopeptide transporter and P-glycoprotein in the intestinal mucosa by Gao, J., Winslow, S.L., Vander Velde, D., Borchardt, R.T., Aubé, J.

“…: Peptide bond bioisosteres, such as hydroxyethylamine (Hea), have frequently been used to stabilize metabolically labile peptide bonds in peptidomimetic drug…”
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Sinefungin, a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication by Pugh, C S, Borchardt, R T, Stone, H O

“…Sinefungin (A9145) and a related metabolite, A9145C, were found to be potent inhibitors of Newcastle disease virion and vaccinia virion…”
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S-adenosylmethionine and its analogs: structural features correlated with synthesis and methylation of mRNAs of cytoplasmic polyhedrosis virus [of the silkworm, Bombyx mori] by Wertheimer, A M, Chen, S Y, Borchardt, R T, Furuichi, Y

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Mechanism of inactivation of S-adenosylhomocysteine hydrolase by (Z)-4',5'-didehydro-5'-deoxy-5'-fluoroadenosine by CHONG-SHENG YUAN, YEH, J, SIMING LIU, BORCHARDT, R. T

“…S-Adenosyl-L-homocysteine (AdoHcy) hydrolase, an enzyme important in the regulation of biological methylation reactions, was shown by McCarthy et al…”
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Reactivity toward deamidation of asparagine residues in β-turn structures by Xie, M., Borchardt, R.T., Topp, E.M., Schowen, R.L., Aubé, J., Morton, M., Vander Velde, D.

“…Mimetics of β‐turn structures in proteins have been used to calibrate the relative reactivities toward deamidation of asparagine residues in the two central…”
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Synthesis and conformational analysis of a coumarinic acid-based cyclic prodrug of an opioid peptide with modified sensitivity to esterase-catalyzed bioconversion by Ouyang, H., Borchardt, R.T., Siahaan, T.J., Vander Velde, D.G.

“…: The coumarinic acid‐based cyclic DADLE (H‐Tyr‐D‐Ala‐Gly‐Phe‐D‐Leu‐OH) prodrug 1a exhibited more favorable physicochemical properties than did DADLE for…”
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Secondary structure of a dynamic type I'β-hairpin peptide by Stotz, C.E., Borchardt, R.T., Middaugh, C.R., Siahaan, T.J., Vander Velde, D., Topp, E.M.

“…:  A spontaneously folding β‐hairpin peptide (Lys‐Lys‐Tyr‐Thr‐Val‐Ser‐Ile‐Asn‐Gly‐Lys‐Lys‐Ile‐Thr‐Val‐Ser‐Ile) and related cyclic…”
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The effect of conformation on the membrane permeation of coumarinic acid- and phenylpropionic acid-based cyclic prodrugs of opioid peptides by Gudmundsson, O.S., Jois, S. D. S., Velde, D. G. Vander, Siahaan, T.J., Borchardt, R.T., Wang, B.

“…: In an earlier study using Caco‐2 cells, an in vitro cell culture model of the intestinal mucosa, we have shown that the coumarinic‐based (3 and 4) and the…”
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Effects of solution polarity and viscosity on peptide deamidation by Li, R., D'souza, A.J., Schowen, R.L., Borchardt, R.T., Topp, E.M., Laird, B.B.

“…: Deamidation kinetics were measured for a model hexapeptide (l‐Val‐l‐Tyr‐l‐Pro‐l‐Asn‐Gly‐l‐Ala, 0.02 mg/mL) in aqueous solutions containing glycerol (0–50%…”
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Synthesis and evaluation of the physicochemical properties of esterase-sensitive cyclic prodrugs of opioid peptides using an (acyloxy)alkoxy linker by Bak, A., Gudmundsson, O.S., Gangwar, S., Friis, G.J., Siahaan, T.J., Borchardt, R.T.

“…: The objective of this work was to synthesize the cyclic prodrugs 1 and 2 of [Leu5]‐enkephalin (Tyr‐Gly‐Gly‐Phe‐Leu‐OH) and DADLE…”
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The effect of conformation of the acyloxyalkoxy-based cyclic prodrugs of opioid peptides on their membrane permeability by Gudmundsson, O.S., Vander Velde, D.G., Jois, S.D.S., Bak, A., Siahaan, T.J., Borchardt, R.T.

“…: In an earlier study using Caco‐2 cells, an in vitro cell culture model of the intestinal mucosa, we have shown that the acyloxyalkoxy‐based cyclic prodrugs 3…”
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Limited Proteolysis of S-Adenosylhomocysteine Hydrolase: Implications for the Three-Dimensional Structure by Gupta, R.A., Yuan, C.S., Aultriche, D.B., Borchardt, R.T.

“…S-Adenosylhomocysteine (AdoHcy) hydrolase was subjected to limited proteolytic digestion utilizing the proteases trypsin, V8, and papain. Results of the…”
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Substrate specificity and some properties of phenol sulfotransferase from human intestinal Caco-2 cells by Baranczyk-Kuzma, A, Garren, J A, Hidalgo, I J, Borchardt, R T

“…The phase II metabolic reactions, sulfation and glucuronidation, were studied in a human colon carcinoma cell line (Caco-2), which has been developed as a…”
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Peptidyl Dipeptidase A-Catalyzed Metabolism of Delta Sleep-Inducing Peptide in Bovine Brain Microvessel Endothelial Cells: A Cell Culture Model of the Blood-Brain Barrier by Augustijns, P.F., Ng, K., Williams, T.M., Borchardt, R.T.

“…Previous studies have shown that the metabolism of delta sleep-inducing peptide (DSIP) in the blood-brain barrier (BBB) is catalyzed by aminopeptidases. In…”
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Demonstration and structural comparison of receptors for insulin-like growth factor-I and -II (IGF-I and -II) in brain and blood-brain barrier by Rosenfeld, R G, Pham, H, Keller, B T, Borchardt, R T, Pardridge, W M

“…Specific receptors for insulin-like growth factors (IGF) I and II on microvessel-free rat brain cell membranes (RBCM) and in the microvessels that constitute…”
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Deamidation of a model hexapeptide in poly(vinyl alcohol) hydrogels and xerogels by Lai, M.C., Schowen, R.L., Borchardt, R.T., Topp, E.M.

“…: Polymeric controlled release systems have been proposed to prolong the half‐lives of protein and peptide drugs in vivo and to deliver active drug at a…”
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Synthesis and Antiviral Activity of [2-[[4-[3-[(1-Methylethyl)amino]-2-Pyridyl]-1-Piperazinyl]Carbonyl]-1H-Indol-5-yl] (BHAP) Acylsphingosine HIV Reverse Transcriptase Inhibitors by Islam, I., Hinshaw, R.R., Chong, K.T., Kato, A., Borchardt, R.T., Fisher, J.F.

“…The galactosylceramide lipid is recognized and tightly complexed by the HIV-1 membrane glycoprotein gp120 in the initial step of viral infection of certain…”
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Sinefungin, a potent inhibitor or S-adenosylmethionine: protein O-methyltransferase by Borchardt, R T, Eiden, L E, Wu, B, Rutledge, C O

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