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.
Nature Communications,
Journal Year:
2020,
Volume and Issue:
11(1)
Published: Jan. 9, 2020
Abstract
Nano-flow
liquid
chromatography
tandem
mass
spectrometry
(nano-flow
LC–MS/MS)
is
the
mainstay
in
proteome
research
because
of
its
excellent
sensitivity
but
often
comes
at
expense
robustness.
Here
we
show
that
micro-flow
LC–MS/MS
using
a
1
×
150
mm
column
shows
reproducibility
chromatographic
retention
time
(<0.3%
coefficient
variation,
CV)
and
protein
quantification
(<7.5%
data
from
>2000
samples
human
cell
lines,
tissues
body
fluids.
Deep
analysis
identifies
>9000
proteins
>120,000
peptides
16
h
sample
multiplexing
tags
increases
throughput
to
11
proteomes
h.
The
system
>30,000
phosphopeptides
12
protein-protein
or
protein-drug
interaction
experiments
can
be
analyzed
20
min
per
sample.
We
same
used
analyze
>7500
without
apparent
loss
performance.
This
study
demonstrates
suitable
for
broad
range
proteomic
applications.
Molecular & Cellular Proteomics,
Journal Year:
2018,
Volume and Issue:
18(3), P. 576 - 593
Published: Dec. 19, 2018
Signaling
pathways
are
orchestrated
by
post-translational
modifications
(PTMs)
such
as
phosphorylation.
However,
pathway
analysis
of
PTM
data
sets
generated
mass
spectrometry
(MS)-based
proteomics
is
typically
performed
at
a
gene-centric
level
because
the
lack
appropriately
curated
signature
databases
and
bioinformatic
tools
that
leverage
site-specific
information.
Here
we
present
first
version
PTMsigDB,
database
modification
signatures
perturbations,
kinase
activities
signaling
from
more
than
2,500
publications.
We
adapted
widely
used
single
sample
Gene
Set
Enrichment
Analysis
approach
to
utilize
enabling
Pharmaceutics,
Journal Year:
2022,
Volume and Issue:
14(5), P. 1001 - 1001
Published: May 6, 2022
Janus
kinase
(JAK)
is
a
family
of
cytoplasmic
non-receptor
tyrosine
kinases
that
includes
four
members,
namely
JAK1,
JAK2,
JAK3,
and
TYK2.
The
JAKs
transduce
cytokine
signaling
through
the
JAK-STAT
pathway,
which
regulates
transcription
several
genes
involved
in
inflammatory,
immune,
cancer
conditions.
Targeting
JAK
with
small-molecule
inhibitors
has
proved
to
be
effective
treatment
different
types
diseases.
In
current
review,
eleven
received
approval
for
clinical
use
have
been
discussed.
These
drugs
are
abrocitinib,
baricitinib,
delgocitinib,
fedratinib,
filgotinib,
oclacitinib,
pacritinib,
peficitinib,
ruxolitinib,
tofacitinib,
upadacitinib.
aim
review
was
provide
an
integrated
overview
chemical
pharmacological
data
globally
approved
inhibitors.
synthetic
routes
were
described.
addition,
their
inhibitory
activities
against
uses
also
explained.
Moreover,
crystal
structures
summarized,
primary
focus
on
binding
modes
interactions.
proposed
metabolic
pathways
metabolites
these
illustrated.
To
sum
up,
could
help
design
new
potential
therapeutic
benefits
inflammatory
autoimmune
