Frontiers in Pharmacology,
Journal Year:
2025,
Volume and Issue:
15
Published: Jan. 6, 2025
Diffuse
large
B-cell
lymphoma
(DLBCL)
is
the
most
common
subtype
of
non-Hodgkin's
(NHL),
up
to
30%-40%
patients
will
relapse
and
10%-15%
have
primary
refractory
disease,
so
exploring
new
treatment
options
necessary.
Ferroptosis
a
non-apoptotic
cell
death
mode
discovered
in
recent
years.
Its
occurrence
pathway
plays
an
essential
impact
on
therapeutic
effect
tumors.
Numerous
studies
shown
that
modulating
critical
factors
ferroptosis
can
influence
growth
tumor
cells
hematological
malignancies
including
DLBCL.
This
review
highlights
advances
ferroptosis-related
genes
(FRGs),
STAT3,
Nrf2,
ZEB1,
focuses
clinical
potential
inducers
such
as
IKE,
α-KG,
DMF,
APR-246,
which
are
currently
being
explored
for
their
effects
Correlational
provide
novel
idea
research
DLBCL
other
lay
solid
foundation
future
studies.
Molecules,
Journal Year:
2023,
Volume and Issue:
28(5), P. 2400 - 2400
Published: March 6, 2023
In
the
last
few
decades,
there
has
been
a
growing
interest
in
Bruton’s
tyrosine
kinase
(BTK)
and
compounds
that
target
it.
BTK
is
downstream
mediator
of
B-cell
receptor
(BCR)
signaling
pathway
affects
proliferation
differentiation.
Evidence
demonstrating
expression
on
majority
hematological
cells
led
to
hypothesis
inhibitors
(BTKIs)
such
as
ibrutinib
can
be
an
effective
treatment
for
leukemias
lymphomas.
However,
body
experimental
clinical
data
demonstrated
significance
BTK,
not
just
malignancies,
but
also
solid
tumors,
breast,
ovarian,
colorectal,
prostate
cancers.
addition,
enhanced
activity
correlated
with
autoimmune
disease.
This
gave
rise
beneficial
therapy
rheumatoid
arthritis
(RA),
systemic
lupus
erythematosus
(SLE),
multiple
sclerosis
(MS),
Sjögren’s
syndrome
(SS),
allergies,
asthma.
this
review
article,
we
summarize
most
recent
findings
regarding
well
advanced
have
developed
date
their
applications
mainly
cancer
chronic
inflammatory
disease
patients.
Nature Communications,
Journal Year:
2024,
Volume and Issue:
15(1)
Published: Jan. 4, 2024
Targeted
protein
degradation
(TPD)
mediates
level
through
small
molecule
induced
redirection
of
E3
ligases
to
ubiquitinate
neo-substrates
and
mark
them
for
proteasomal
degradation.
TPD
has
recently
emerged
as
a
key
modality
in
drug
discovery.
So
far
only
few
have
been
utilized
TPD.
Interestingly,
the
workhorse
ligase
CRBN
observed
be
downregulated
settings
resistance
immunomodulatory
inhibitory
drugs
(IMiDs).
Here
we
show
that
essential
receptor
DCAF1
can
harnessed
utilizing
selective,
non-covalent
binder.
We
confirm
this
binder
functionalized
into
an
efficient
DCAF1-BRD9
PROTAC.
Chemical
genetic
rescue
experiments
validate
specific
via
CRL4
Journal of Hematology & Oncology,
Journal Year:
2025,
Volume and Issue:
18(1)
Published: Jan. 13, 2025
The
tumor
microenvironment
(TME)
is
integral
to
cancer
progression,
impacting
metastasis
and
treatment
response.
It
consists
of
diverse
cell
types,
extracellular
matrix
components,
signaling
molecules
that
interact
promote
growth
therapeutic
resistance.
Elucidating
the
intricate
interactions
between
cells
TME
crucial
in
understanding
progression
challenges.
A
critical
process
induced
by
epithelial-mesenchymal
transition
(EMT),
wherein
epithelial
acquire
mesenchymal
traits,
which
enhance
their
motility
invasiveness
progression.
By
targeting
various
components
TME,
novel
investigational
strategies
aim
disrupt
TME's
contribution
EMT,
thereby
improving
efficacy,
addressing
resistance,
offering
a
nuanced
approach
therapy.
This
review
scrutinizes
key
players
emphasizing
avenues
therapeutically
components.
Moreover,
article
discusses
implications
for
resistance
mechanisms
highlights
current
toward
modulation
along
with
potential
caveats.
Biomarker Research,
Journal Year:
2022,
Volume and Issue:
10(1)
Published: Nov. 23, 2022
Abstract
Chimeric
antigen
receptor
T
(CAR-T)
cell
therapy
has
significantly
improved
the
life
expectancy
for
patients
with
refractory
or
relapse
B
lymphoma.
As
acute
lymphoblastic
leukemia
(B-ALL),
although
primary
response
rate
is
promising,
high
incidence
of
early
caused
modest
long-term
survival
CAR-T
alone.
One
main
challenges
limited
persistence
cells.
To
further
optimize
clinical
effects
cells,
many
studies
have
focused
on
modifying
CAR
structure
and
regulating
differentiation.
In
this
review,
we
focus
summarize
latest
progress
strategies
adopted
during
in
vitro
culture
stage
to
immunotherapy
by
improving
persistence.
Such
include
choosing
a
suitable
source,
conditions,
combining
cells
conventional
drugs,
applying
genetic
manipulations,
all
which
may
improve
hematologic
malignancies
reducing
probability
recurrence
after
infusion
provide
clues
solid
tumor
development.
Molecules,
Journal Year:
2023,
Volume and Issue:
28(7), P. 3043 - 3043
Published: March 29, 2023
The
mammalian
bromodomain
and
extra-terminal
domain
(BET)
family
of
proteins
consists
four
conserved
members
(Brd2,
Brd3,
Brd4,
Brdt)
that
regulate
numerous
cancer-related
immunity-associated
genes.
They
are
epigenetic
readers
histone
acetylation
with
broad
specificity.
BET
linked
to
cancer
progression
due
their
interaction
cellular
including
chromatin-modifying
factors,
transcription
modification
enzymes.
spectacular
growth
in
the
clinical
development
small-molecule
inhibitors
underscores
interest
importance
this
protein
as
an
anticancer
target.
Current
approaches
targeting
for
therapy
rely
on
mimics
block
bromodomains
from
binding
chromatin.
However,
bromodomain-targeted
agents
suffering
dose-limiting
toxicities
because
effects
other
bromodomain-containing
proteins.
In
review,
we
provided
updated
summary
about
evolution
inhibitors.
design
bivalent
inhibitors,
kinase
dual
proteolysis-targeting
chimeras
(PROTACs),
Brd4-selective
discussed.
novel
strategy
unique
C-terminal
(ET)
its
therapeutic
significance
will
also
be
highlighted.
Apart
single
agent
treatment
alone,
have
been
combined
chemotherapeutic
modalities
demonstrating
favorable
outcomes.
investigation
specific
biomarkers
predicting
efficacy
resistance
is
needed
fully
realize
potential
setting.
Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
67(2), P. 864 - 884
Published: Jan. 10, 2024
The
DNA-encoded
library
(DEL)
discovery
platform
has
emerged
as
a
powerful
technology
for
hit
identification
in
recent
years.
It
become
one
of
the
major
parallel
workstreams
small
molecule
drug
along
with
other
strategies
such
HTS
and
data
mining.
For
many
researchers
working
DEL
field,
it
increasingly
evident
that
hits
leads
discovered
via
screening
bind
to
target
proteins
unique
unprecedented
binding
modes.
This
Perspective
is
our
attempt
analyze
reports
purpose
providing
rigorous
useful
account
modes
observed
DEL-derived
ligands
focus
on
mode
novelty.
International Journal of Molecular Sciences,
Journal Year:
2024,
Volume and Issue:
25(4), P. 2208 - 2208
Published: Feb. 12, 2024
Bruton’s
tyrosine
kinase
(BTK)
inhibitors
have
revolutionized
the
landscape
for
treatment
of
hematological
malignancies,
solid
tumors,
and,
recently,
autoimmune
disorders.
The
BTK
receptor
is
expressed
in
several
hematopoietic
cells
such
as
macrophages,
neutrophils,
mast
cells,
and
osteoclasts.
Similarly,
involved
signaling
pathways
chemokine
signaling,
Toll-like
Fc
signaling.
Due
to
their
unique
mechanism,
these
agents
provide
a
diverse
utility
variety
disease
states
not
limited
field
malignant
hematology
are
generally
well-tolerated.
Pharmaceuticals,
Journal Year:
2024,
Volume and Issue:
17(1), P. 100 - 100
Published: Jan. 11, 2024
PROTAC
is
a
rapidly
developing
engineering
technology
for
targeted
protein
degradation
using
the
ubiquitin–proteasome
system,
which
has
promising
applications
inflammatory
diseases,
neurodegenerative
and
malignant
tumors.
This
paper
gives
brief
overview
of
development
design
principles
PROTAC,
with
special
focus
on
PROTAC-based
explorations
in
recent
years
aimed
at
achieving
controlled
improving
bioavailability
as
well
TPD
technologies
that
use
other
pathways
such
autophagy
lysosomes
to
achieve
degradation.
Journal of Medicinal Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Feb. 3, 2025
This
review
is
the
next
installment
of
an
annual
series
that
discusses
synthetic
routes
to
access
28
small
molecule
drugs
were
approved
worldwide
in
2023.
A
brief
description
each
drug's
mechanism
action,
history
its
discovery
and
development,
approaches
published
primary
or
patent
literature
most
likely
used
for
clinical
studies
development
are
included.
Synthetic
chemistry,
convert
complex
intermediates
active
compounds
build
a
new
drug
from
basic
building
block
chemicals,
critical
delivery
treatments
disease
patients.
