Antibody-drug Conjugate

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Antibody-drug Conjugate

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Gene transcription is a process that transfers the genetic information into carriers such as mRNA and guides subsequent cellular metabolic activities. Interruption of gene transcription will result in catastrophic impacts and lead to cell death. Many of the transcription inhibitors have decent pharmacological effects against tumor growth and a number of anti-cancer drugs have been identified or developed to restrain transcription, among which amatoxins have been shown to exhibit high tumor inhibition potency – PowerPoint PPT presentation

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Title: Antibody-drug Conjugate

1
Antibody-drug Conjugates

https//www.creative-biolabs.com/adc

2
Amatoxins

Gene transcription is a process that transfers
the genetic information into carriers such as
mRNA and guides subsequent cellular metabolic
activities. Interruption of gene transcription
will result in catastrophic impacts and lead to
cell death. Many of the transcription inhibitors
have decent pharmacological effects against tumor
growth and a number of anti-cancer drugs have
been identified or developed to restrain
transcription, among which amatoxins have been
shown to exhibit high tumor inhibition potency

Amatoxins are a group of toxic compounds commonly
produced by green and white Amanita muscaria and
result in fatal human Amanita intoxications upon
ingestion. They are synthesized via the cleavage,
modification, and cyclization of precursor
peptides that usually contain a 10 amino
acid-residue leader peptide followed by the
amatoxin peptide and a recognition sequence.

The recognition sequence starts with a conserved
Cys residue and has several conserved peptide
motifs including the DDV motif and the LLTRGE
motif. Chemically, amatoxins are cyclic
octapeptides with a basic peptide sequence
template Ile-Trp-Gly-Ile-Gly-Cys-Asn-Pro.
This octapeptide is cyclized by the peptide bond
between Ile and Pro residues and it is also
featured by an internal cross-bridge formed by
the Cys and Trp residues.

4
LOREM IPSUM DOLOR
Cyclic octapeptide structure of amatoxin and its
variants. Amatoxins are chemically versatile with
different modifications on the R groups
generate at least 9 variants.
5
taxoids

Taxoids, also known as paclitaxel, are
derivatives from taxol, an early potent
anticancer compound extracted from Pacific yew
(Taxus brevifolia Nutt). Taxiods was first
discovered and named by Wall et al. in 1966 and
their cytotoxcicity was later demonstrated in 9
KB cancer cell and tissue culture. Since then,
taxiods have been documented to show anti-cancer
activity against leukemia and murine melanoma
cell cultures, as well as various xenograft mouse
models bearing MX1 (breast), CX1 (colon) and LX1
(lung) carcinomas.

6
Thailanstatin a

Thailanstatin A, a promising lead compound for
drug discovery and development efforts, is
derived from Thailandensis burkholderia MSMB43.
It reveals low nanomolar to subnanomolar
cytotoxicity against a variety of human cancer
cell lines. The mechanism of action (MOA) of
thailanstatin A is the inhibition of spliceosome
assembly. Thailanstatin A binds firmly to the
SF3b subunit of the U2 snRNA sub-complex, a
crucial component of the spliceosome. Since the
spliceosomes of cancer cells are more active and
exhibits higher mutation rates than those of
normal cells, this sub-cellular component is by
far the most well-established anti-tumor target
in novel drug discoveries.