• Receptor tyrosine kinase Axl is a

  2025-02-17

  

  Receptor tyrosine kinase Axl is a member of the TAM (Tyro3/Axl/Mer) family, and has reported been associated with a spectrum of human cancers [8]. Numerous studies have revealed that the oncogenic potential of Axl is attributed to the anti-apoptotic and proliferative signaling pathways triggered by

• In conclusion AXL overexpression preexisted in a subgroup of

  2025-02-17

  

  In conclusion, AXL overexpression preexisted in a subgroup of treatment-naive lung adenocarcinoma specimens harboring an activating EGFR mutation or in those with wild-type EGFR. Anti-AXL therapeutics delivered up front in combination with the EGFR inhibitor might overcome intrinsic or acquired resi

• Skeletal pain associated with bone fracture is another

  2025-02-17

  

  Skeletal pain associated with bone fracture is another area of critical need for a novel pain medication. NSAIDs and opiates are the two major therapies currently used to manage bone fracture pain. However, both of these therapies lead to significant unwanted side effects. Using the osteotomy model

• br Conclusion br Acknowledgments This research has been supp

  2025-02-17

  

  Conclusion Acknowledgments This research has been supported by the Ratchadaphiseksomphot Endowment Fund 2013 of Chulalongkorn University (CU-56-341-AS) and the Ratchadapiseksompotch Fund (RA55/22), Faculty of Medicine, Chulalongkorn University. The authors commemorate the 100th Anniversary of

• br Other Strategies for HIF Inhibition NSC is

  2025-02-15

  

  Other Strategies for HIF-α Inhibition NSC-644221 is another HIF-α inhibitor acting at the translational level, independently of proteasomal degradation and VHL status, and is devoid of DNA damage-inducing properties [70]. NSC-644221 arrests brucine australia in G2–M through a cell type-specific T

• br Angiotensin receptor neprilysin inhibitors Sacubitril

  2025-02-15

  

  Angiotensin receptor-neprilysin inhibitors Sacubitril/valsartan is the first-in-class ARNI, comprising of molecular moieties of valsartan (ARB) and a neprilysin inhibitor prodrug, sacubitril (AHU377) [51]. Upon ingestion, sacubitril is rapidly metabolised into an active neprilysin inhibitor, sacu

• br STAR Methods br AMPK A Therapeutic Target

  2025-02-15

  

  STAR★Methods AMPK: A Therapeutic Target in the β Cell? Loss of pancreatic β cell function is a hallmark of the transition to a diagnosis of T2DM (see Glossary) 1, 2, 3, 4. AMPK activation has gained attention for the treatment of hyperglycemia in prediabetes as an insulin-sensitizing agent bec

• br Conclusion br Conflicts of interest br

  2025-02-15

  

  Conclusion Conflicts of interest Introduction Alzheimer’s disease is the most common neurodegenerative condition known to cause dementia (Ferri et al., 2005). Alzheimer’s dementia typically presents with initial recent episodic memory deficits, word finding difficulty and later with apraxia

• Ketogenic diets are more effective in

  2025-02-15

  

  Ketogenic diets are more effective in promoting weight loss than conventional caloric restriction [26] however, their effect on hepatic glucose and lipid metabolism remains inconclusive. Blood glucose homeostasis is tightly regulated. In both mice and humans consuming KD, baseline blood glucose decr

• Furthermore stress hormones can indirectly induce DNA

  2025-02-15

  

  Furthermore, stress hormones can indirectly induce DNA damage, for example by altering DNA repair and transcriptional regulation of the cell cycle. It has been found that stress hormones induce the up-regulation of checkpoint kinase 1 (Chk1) and checkpoint kinase 2 (Chk2) and proto-oncogene cell div

• Metformin s pluripotent roles are alluded to in terms

  2025-02-15

  

  Metformin's pluripotent roles are alluded to in terms of its antitumorigenic, glucose-lowering, and cardioprotective effects, which are due in part to its upregulation of AMPK activity [39,40]. Metformin's glucose-lowering effect is a result of reduced hepatic gluconeogenesis, whereas improved insul

• A high throughput small molecule ACK biochemical inhibition

  2025-02-15

  

  A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found 6-Aminonicotinamide to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) w

• br Methods br Results and discussion

  2025-02-14

  

  Methods Results and discussion Conclusions Acknowledgements The authors thank Dr. Francois Alhenc-Gelas (then INSERM U367, Paris, France), who kindly provided the plasmid for truncated soluble recombinant human ACE – WTΔ, Dr. Elena Arablinskaya (Institute of Phtiziopulmonology, Moscow, R

• At present drugs that specifically inhibit

  2025-02-14

  

  At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi

• An AXL decoy receptor with enhanced GAS

  2025-02-14

  

  An AXL decoy receptor with enhanced GAS6-binding properties, MYD1, was engineered as a therapeutic tool to disrupt GAS6/AXL signaling in vivo (Kariolis et al., 2014). MYD1 was shown to block metastasis of human ovarian cancer topirimate australia and a murine breast cancer cell line in grafting ass

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