MedComm,
Journal Year:
2022,
Volume and Issue:
3(4)
Published: Oct. 13, 2022
Compared
with
traditional
therapies,
targeted
therapy
has
merits
in
selectivity,
efficacy,
and
tolerability.
Small
molecule
inhibitors
are
one
of
the
primary
therapies
for
cancer.
Due
to
their
advantages
a
wide
range
targets,
convenient
medication,
ability
penetrate
into
central
nervous
system,
many
efforts
have
been
devoted
developing
more
small
inhibitors.
To
date,
88
approved
by
United
States
Food
Drug
Administration
treat
cancers.
Despite
remarkable
progress,
cancer
treatment
still
face
obstacles,
such
as
low
response
rate,
short
duration
response,
toxicity,
biomarkers,
resistance.
better
promote
development
targeting
cancers,
we
comprehensively
reviewed
involved
all
agents
pivotal
drug
candidates
clinical
trials
arranged
signaling
pathways
classification
We
discussed
lessons
learned
from
these
agents,
proper
strategies
overcome
resistance
arising
different
mechanisms,
combination
concerned
Through
our
review,
hoped
provide
insights
perspectives
research
treatment.
Molecular Cancer,
Journal Year:
2018,
Volume and Issue:
17(1)
Published: Feb. 15, 2018
The
human
genome
encodes
538
protein
kinases
that
transfer
a
γ-phosphate
group
from
ATP
to
serine,
threonine,
or
tyrosine
residues.
Many
of
these
are
associated
with
cancer
initiation
and
progression.
recent
development
small-molecule
kinase
inhibitors
for
the
treatment
diverse
types
has
proven
successful
in
clinical
therapy.
Significantly,
second
most
targeted
drug
targets,
after
G-protein-coupled
receptors.
Since
first
inhibitor,
early
1980s,
37
have
received
FDA
approval
malignancies
such
as
breast
lung
cancer.
Furthermore,
about
150
kinase-targeted
drugs
phase
trials,
many
kinase-specific
preclinical
stage
development.
Nevertheless,
factors
confound
efficacy
molecules.
Specific
tumor
genetics,
microenvironment,
resistance,
pharmacogenomics
determine
how
useful
compound
will
be
given
This
review
provides
an
overview
discovery
relation
oncology
highlights
challenges
future
potential
therapies.
Signal Transduction and Targeted Therapy,
Journal Year:
2020,
Volume and Issue:
5(1)
Published: July 2, 2020
Abstract
Ever
present
hurdles
for
the
discovery
of
new
drugs
cancer
therapy
have
necessitated
development
alternative
strategy
drug
repurposing,
old
therapeutic
purposes.
This
with
a
cost-effective
way
offers
rare
opportunity
treatment
human
neoplastic
disease,
facilitating
rapid
clinical
translation.
With
an
increased
understanding
hallmarks
and
various
data-driven
approaches,
repurposing
further
promotes
holistic
productivity
reasonably
focuses
on
target-defined
antineoplastic
compounds.
The
“treasure
trove”
non-oncology
should
not
be
ignored
since
they
could
target
only
known
but
also
hitherto
unknown
vulnerabilities
cancer.
Indeed,
different
from
targeted
drugs,
these
generic
usually
used
in
multi-target
may
bring
benefit
to
patients.
In
this
review,
aiming
demonstrate
full
potential
we
promising
repurposed
management
classify
candidates
into
their
proposed
administration
either
mono-
or
combination
therapy.
We
summarize
approaches
discuss
main
barriers
its
uptake.
Nucleic Acids Research,
Journal Year:
2023,
Volume and Issue:
52(D1), P. D1180 - D1192
Published: Nov. 2, 2023
Abstract
ChEMBL
(https://www.ebi.ac.uk/chembl/)
is
a
manually
curated,
high-quality,
large-scale,
open,
FAIR
and
Global
Core
Biodata
Resource
of
bioactive
molecules
with
drug-like
properties,
previously
described
in
the
2012,
2014,
2017
2019
Nucleic
Acids
Research
Database
Issues.
Since
its
introduction
2009,
ChEMBL’s
content
has
changed
dramatically
size
diversity
data
types.
Through
incorporation
multiple
new
datasets
from
depositors
since
update,
now
contains
slightly
more
bioactivity
deposited
vs
extracted
literature.
In
collaboration
EUbOPEN
consortium,
chemical
probe
regularly
into
ChEMBL.
Release
27
made
curated
available
for
compounds
screened
potential
anti-SARS-CoV-2
activity
several
large-scale
drug
repurposing
screens.
addition,
patent
have
been
added
to
latest
releases,
various
features
incorporated,
including
Natural
Product
likeness
score,
updated
flags
Products,
flag
Chemical
Probes,
initial
annotation
action
type
∼270
000
measurements.
