Tumor targeting agents and uses thereof
A tumor targeting and detection agent technology, applied in the field of tumor targeting agents, can solve the problems of not revealing tumors, resistance reducing the effectiveness of available drugs, hindering delivery, etc.
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[0405] Preparation of targeting unit and targeting agent of the present invention
[0406] The targeting unit according to the invention is preferably a synthetic peptide. Peptides can be synthesized by various known techniques, such as solid phase synthesis methods (FMOC, BOC and other protection schemes, various resin types), solution phase synthesis methods (FMOC, BOC and other variants) and combinations thereof. Even automated synthesis apparatus / equipment are commercially available for this purpose, as are routine synthesis and purification services. These methods are well known to those skilled in the art. Some methods and materials are described, for example, in the following references:
[0407] Bachem AG, SASRIN TM (1999), The BACHEM Practice of SPPS (2000), Bachem 2001 catalog (2001), Novabiochem 2000 Catalog (2000), Peptide and Peptidomimetic Synthesis (2000) and The Combinatorial Chemistry Catalog & Solid Phase Organic Chemistry (SPOC) 9 Handbook 98 / 9. The synt...
Embodiment 1
[0475] Synthesis of Targeting Motif / Targeting Unit (Peptide) IRE; Use of Peptide Synthesis Resin Without Pre-Coupling with Amino Acid Residues; and Derivatization of said Resin with Protected Amino Acid Derivatives (Residues)
[0476] The targeting motif / targeting unit (peptide) IRE (isoleucyl-arginyl-glutamic acid) was synthesized using manual solid-phase peptide synthesis as detailed in Example 2 below.
[0477] The coupling (bonding) of the first amino acid unit (residue) to the hydroxyl group of the peptide synthetic resin (HMP type; see the list of raw materials given below) is carried out by the method of dichlorobenzoyl chloride, which As in the method used for the derivatives of L-glutamine in which the amino function is protected by a 9-fluorenylmethoxycarbonyl (=Fmoc) group, the "side chain" carboxyl function (carbonyl) of the glutamic acid, i.e. The carbonyl remote from the amino function is protected as its tert-butyl ester. The procedure used is as follows:
[0...
Embodiment 2
[0495] General Procedures for Peptide Synthesis: Manual Solid-Phase Peptide Synthesis; and Mass Spectrometric Measurements
[0496] All syntheses were performed in a sealable glass funnel equipped with a sintered glass filter disc of porosity class 2 to 4 and with a polypropylene or Bakelite screw cap on top (for sealing), and two PTFE pushbutton pistons: one located under the filter disc (for draining) and the other on a beveled corner on the neck shoulder of the screw cap tube (for argon inlet).
[0497] Fill the funnel with the appropriate solid-phase synthetic resin and solution for each treatment and shake the "wrist motion" bottle shaker (Gallenkamp TM ) with the help of vigorous shaking for an appropriate period of time, followed by filtration under a moderate pressure of argon.
[0498] The general procedure for one synthesis cycle (=addition of one amino acid unit) is as follows:
[0499] It will be loaded with about 1 mmol of Fmoc-peptide (=peptide whose amino-term...
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Abstract
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