Results 161 to 170 of about 35,931 (278)

The potential for biased signalling in the P2Y receptor family of GPCRs

open access: yesBritish Journal of Pharmacology, EarlyView.
The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk   +2 more
wiley   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown   +2 more
wiley   +1 more source

Hypoxia Independently Induces AID Expression in CH12 B Cells. [PDF]

open access: yesEur J Immunol
Heyer V   +5 more
europepmc   +1 more source

Cancer pain: current practice and emerging targets

open access: yesBritish Journal of Pharmacology, EarlyView.
Cancer pain (CP) arises from a complex interplay between the tumour and its microenvironment. Many patients experience a mixed pain phenotype that encompasses nociceptive, neuropathic and neuroinflammatory mechanisms, and vary across tumour type and disease stage. Despite decades of intensive research, the mainstay of cancer pain treatment is still non‐
Yi Ye   +5 more
wiley   +1 more source

MAPK Inhibitor‐Tolerant Persister Cells in Melanoma: Mechanisms and Therapeutic Vulnerabilities

open access: yesCancer Science, EarlyView.
Melanoma response to MAPK inhibition progresses from drug‐sensitive cells to drug‐tolerant persister states, which enable survival through adaptive signaling, metabolic rewiring, and phenotypic plasticity. These persister cells serve as an intermediate reservoir from which resistant tumors ultimately emerge. ABSTRACT Though major advancements have been
Bhoomi Shah   +3 more
wiley   +1 more source

ADSC‐Derived CCL8 Regulates HIF‐1α Signaling and Promotes Colorectal Cancer Progression in a 3D Coculture Platform

open access: yesCancer Science, EarlyView.
Schematic illustration showing how CRC‐associated ADSC‐derived CCL8 promotes colorectal cancer cell migration through ERK/HIF‐1α signaling in a 3D coculture platform. ABSTRACT This study aimed to recapitulate adipose‐tumor interactions within the colorectal cancer (CRC) tumor microenvironment (TME) and to elucidate the role of adipose‐derived stem ...
Jeong‐Eun Yun   +7 more
wiley   +1 more source

Lactate Accelerates Early Angiogenesis and Bone Regeneration Through Macrophage M1 Polarisation

open access: yesCell Proliferation, EarlyView.
During the early stage of bone defect healing, lactate accumulates and contributes to increasing NOD1 expression by stabilising HIF1α that in turn triggers a calcium influx, which ultimately polarises macrophages towards the M1 phenotype and accelerates vascularisation of endothelial cells.
Lulu Liu   +10 more
wiley   +1 more source

HIF inhibition: Current strategies and clinical challenges. [PDF]

open access: yesRedox Biol
Więch-Walów A   +7 more
europepmc   +1 more source

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