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Inhibition of Prostaglandin-Degrading Enzyme 15-PGDH Mitigates Acute Murine Lung Allograft Rejection
PurposeAcute rejection is a frequent complication among lung transplant recipients and poses substantial therapeutic challenges....
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HPLC fingerprint of flavonoids, enzyme inhibition and antioxidant activity of Newbouldia laevis stem-bark: an in vitro and in silico study
BackgroundMedicinal plant contains multiple bioactive compounds with therapeutic potentials. Due to their availability, affordability, and minimal...
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Metabolic profiling and enzyme inhibitory activity of the essential oil of citrus aurantium fruit peel
BackgroundBitter orange ( Citrus aurantium ) is a fruiting shrub native to tropical and subtropical countries around the world and cultivated in many...
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Inhibition of the deubiquitinating enzyme USP47 as a novel targeted therapy for hematologic malignancies expressing mutant EZH2
Activating mutations in EZH2, the catalytic component of PRC2, promote cell proliferation, tumorigenesis, and metastasis through enzymatic or...
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BTK inhibition limits microglia-perpetuated CNS inflammation and promotes myelin repair
In multiple sclerosis (MS), persisting disability can occur independent of relapse activity or development of new central nervous system (CNS)...
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Chimeric kinase ALK induces expression of NAMPT and selectively depends on this metabolic enzyme to sustain its own oncogenic function
As we show in this study, NAMPT, the key rate-limiting enzyme in the salvage pathway, one of the three known pathways involved in NAD synthesis, is...
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Inhibition of cc chemokine receptor 10 ameliorates osteoarthritis via inhibition of the phosphoinositide-3-kinase/Akt/mammalian target of rapamycin pathway
BackgroundOsteoarthritis (OA) is a joint disease characterized by inflammation and progressive cartilage degradation. Chondrocyte apoptosis is the...
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Advances in Immune Tolerance Induction in Enzyme Replacement Therapy
Inborn errors of metabolism (IEMs) are a group of genetic diseases that occur due to the either deficiency of an enzyme involved in a...
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Angiotensin converting enzyme (ACE) inhibitors activity from purified compounds Fructus Phaleria macrocarpa (Scheff) Boerl
BackgroundMahkota Dewa [ Phaleria macrocarpa (Scheff) Boerl.] fruit in vitro and in- vivo can decrease and prevent elevation of the blood pressure,...
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Pharmacologic targeting of Nedd8-activating enzyme reinvigorates T-cell responses in lymphoid neoplasia
Neddylation is a sequential enzyme-based process which regulates the function of E3 Cullin-RING ligase (CRL) and thus degradation of substrate...
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Stearoyl-CoA desaturase 1 inhibition induces ER stress-mediated apoptosis in ovarian cancer cells
Ovarian cancer is a leading cause of death among gynecologic tumors, often detected at advanced stages. Metabolic reprogramming and increased lipid...
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SHP2 inhibitors maintain TGFβ signalling through SMURF2 inhibition
Despite the promising antitumor activity of SHP2 inhibitors in RAS-dependent tumours, overall responses have been limited by their narrow therapeutic...
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Small molecule inhibition of deubiquitinating enzyme JOSD1 as a novel targeted therapy for leukemias with mutant JAK2
Mutations in the Janus Kinase 2 (JAK2) gene resulting in constitutive kinase activation represent the most common genetic event in myeloproliferative...
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Inhibition of post-lanosterol biosynthesis by fentanyl: potential implications for Fetal Fentanyl Syndrome (FFS)
A recent study discovered a novel, complex developmental disability syndrome, most likely caused by maternal fentanyl use disorder. This Fetal...
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DHODH inhibition represents a therapeutic strategy and improves abiraterone treatment in castration-resistant prostate cancer
Castration-resistant prostate cancer (CRPC) is an aggressive disease with poor prognosis, and there is an urgent need for more effective therapeutic...
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Optimization of extraction conditions and evaluation of Manilkara zapota (L.) P. Royen fruit peel extract for in vitro α-glucosidase enzyme inhibition and free radical scavenging potential
BackgroundMost of the edible portions like peel and skin of some fruits is discarded while consuming it, though they are rich in several health...
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A positive feedback inhibition of isocitrate dehydrogenase 3β on paired-box gene 6 promotes Alzheimer-like pathology
Impaired brain glucose metabolism is an early indicator of Alzheimer’s disease (AD); however, the fundamental mechanism is unknown. In this study, we...
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Ubiquitin-conjugating enzyme E2C (UBE2C) is a prognostic indicator for cholangiocarcinoma
Cholangiocarcinoma is the most common malignant bile duct tumor in Southeast Asia. The special location of cholangiocarcinoma leads to it being...
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BTK inhibition potentiates anti-PD-L1 treatment in murine melanoma: potential role for MDSC modulation in immunotherapy
Myeloid-derived suppressor cells (MDSC) have been linked to loss of immune effector cell function through a variety of mechanisms such as the...
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Mitochondrial regulation of GPX4 inhibition–mediated ferroptosis in acute myeloid leukemia
Resistance to apoptosis in acute myeloid leukemia (AML) cells causes refractory or relapsed disease, associated with dismal clinical outcomes....
