RTRAIL Mutant and Monomethyl Auristatin E Conjugate Thereof
AssigneeZhejiang University a university
InventorsShuqing CHEN, Liqiang PAN
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AssigneeZhejiang University a university
InventorsShuqing CHEN, Liqiang PAN
Estimating the term…
Disclosed are an rTRAIL mutant and monomethyl auristatin E (MMAE) conjugate thereof. The amino acid sequence thereof is as represented by SEQ ID No.1. Also disclosed are a coding gene of the rTRAIL mutant and expression system, recombinant vector and expression unit containing the coding gene. Also disclosed are an rTRAIL mutant-vcMMAE conjugate and preparation and uses thereof. The conjugate of the present invention has the biological functions of both the rTRAIL mutant and the MMAE; the MMAE is directionally transferred to a tumor cell through the specific binding between the rTRAIL mutant and a death receptor on the surface of the tumor cell, and is released and takes effect in the tumor cell, thus killing the tumor cells less sensitive or even resistant to TRAIL, and reducing the toxicity generated by the separate administration of the MMAE.
An rTRAIL mutant, characterized in that the amino acid sequence is represented by SEQ ID No.1.
An rTRAIL mutant-MMAE conjugate, characterized in that it is formed by conjugating monomethyl auristatin E (MMAE) with an rTRAIL mutant trimer through a linker, the amino acid sequence of the rTRAIL mutant is represented by SEQ ID No.1, and said linker is a maleimide-modified valine-citrulline dipeptide.
(canceled)
A method of preparing an rTRAIL mutant-MMAE conjugate, comprising:
Dependencies are inferred from the claim text.