摘要:
This invention relates to proteins (e.g., peptides) that are capable of facilitating transport of an active agent through a human or animal gastrointestinal tissue, and derivatives (e.g., fragments) and analogs thereof, and nucleotide sequences coding for said proteins and derivatives. The proteins of the invention have use in facilitating transport of active agents from the lumenal side of the GIT into the systemic blood system, and/or in targeting active agents to the GIT. Thus, for example, by binding (covalently or noncovalently) a protein of the invention to an orally administered drug, the drug can be targeted to specific receptor sites or transport pathways which are known to operate in the human gastrointestinal tract, thus facilitating its absorption into the systemic system.
摘要:
This invention relates to proteins (e.g., peptides) that are capable of facilitating transport of an active agent through a human or animal gastro-intestinal tissue, and derivatives (e.g., fragments) and analogs thereof, and nucleotide sequences coding for said proteins and derivatives. The proteins of the invention have use in facilitating transport of active agents from the lumenal side of the GIT into the systemic blood system, and/or in targeting active agents to the GIT. Thus, for example, by binding (covalently or noncovalently) a protein of the invention to an orally administered drug, the drug can be targeted to specific receptor sites or transport pathways which are known to operate in the human gastrointestinal tract, thus facilitating its absorption into the systemic system.
摘要:
This invention relates to proteins (e.g., peptides) that are capable of facilitating transport of an active agent through a human or animal gastro-intestinal tissue, and derivatives (e.g., fragments) and analogs thereof, and nucleotide sequences coding for said proteins and derivatives. The proteins of the invention have use in facilitating transport of active agents from the lumenal side of the GIT into the systemic blood system, and/or in targeting active agents to the GIT. Thus, for example, by binding (covalently or noncovalently) a protein of the invention to an orally administered drug, the drug can be targeted to specific receptor sites or transport pathways which are known to operate in the human gastrointestinal tract, thus facilitating its absorption into the systemic system.
摘要:
The present invention relates to a novel membrane translocating full-length peptide sequence, fragment, motif, derivative, analog or peptidomimetic thereof (MTLPs), to nucleotide sequences coding therefor, and to compositions comprising a MTLP-active agent complex and a MTLP-active particle complex. The MTLP or the nucleotide sequence coding therefor enhance movement of the active agent or of the active particle across a lipid membrane. More particularly, the present invention relates to a MTLP-active agent complex and a MTLP-active particle complex, wherein the MTLP enhances uptake of the active agent into a cell, into or out of an intracellular compartment and across a cell layer. Methods of making and methods of using MTLPs also are included.
摘要:
The present invention relates to a novel membrane translocating full-length peptide sequence, fragment, motif, derivative, analog or peptidomimetic thereof (MTLPs), to nucleotide sequences coding therefor, and to compositions comprising a MTLP-active agent complex and a MTLP-active particle complex. The MTLP or the nucleotide sequence coding therefor enhance movement of the active agent or of the active particle across a lipid membrane. More particularly, the present invention relates to a MTLP-active agent complex and a MTLP-active particle complex, wherein the MTLP enhances uptake of the active agent into a cell, into or out of an intracellular compartment and across a cell layer. Methods of making and methods of using MTLPs also are included.
摘要:
A method of identifying a peptide which permits or facilitates the transport of an active agent through a human or animal tissue. A predetermined amount of phage from a random phage library or a preselected phage library is administered in vivo or in situ to a site in an animal, such as into the gastro-intestinal tract. At a predetermined time, the phage which is transported across a tissue barrier is harvested at a harvesting site, such as in portal or systemic blood or brain tissue, which is separated from the site of administration by the tissue barrier to select transported phage. This transported phage is amplified in a host. This cycle of events is repeated (using the transported phage produced in the most recent cycle) a predetermined number of times to obtain a selected phage library containing phage which can be transported from the site of administration to the harvesting site. The identity of at least one peptide coded by phage in the selected phage library is determined to identify a peptide which permits or facilitates the transport of an active agent through a human or animal tissue.
摘要:
A composition and method for enhancing paracellular transport across cell layers in an animal comprising an antisense oligonucleotide hybridizable with a region of the messenger RNA coding for the protein occludin which, when hybridized to the occludin mRNA, interferes with its translation such that occludin function is disrupted and paracellular permeability is increased across an epithelial cell layer or and endothelial cell layer in an animal.
摘要:
Purified synthetic polypeptide ligands for targeting pharmaceutical agents and carriers comprising such agents to intestinal epithelial tissue, especially Peyer's patch and/or M-Cell tissue. Also methods of using the ligands.