Results 1 to 10 of about 246,536 (223)

Topical VX-509 Attenuates Psoriatic Inflammation Through the STAT3/FABP5 Pathway in Keratinocytes.

Pharmacological Research, 2022
BACKGROUND Psoriasis is a chronic inflammatory disease, with lesions mainly manifesting as scaly erythematous plaques. The mild or moderate of psoriasis is the main type of patients in hospital, and topical application remains the preferred treatment ...
B. Yan, Panpan Liu, Xiaoqing Yi, Jie Li, Nian Liu, Wu Zhu, Y. Kuang, Xiang Chen, C. Peng   +8 more
semanticscholar   +3 more sources

The Caspase 1 Inhibitor VX-765 Protects the Isolated Rat Heart via the RISK Pathway [PDF]

Cardiovascular Drugs and Therapy, 2018
PURPOSE: Protecting the heart from ischaemia-reperfusion (IR) injury is a major goal in patients presenting with an acute myocardial infarction. Pyroptosis is a novel form of cell death in which caspase 1 is activated and cleaves interleukin 1β.
Arjun, S, Davidson, SM, Do Carmo, H, Petrucci, O, Yellon, DM   +4 more
core   +2 more sources

VX-770-mediated potentiation of numerous human CFTR disease mutants is influenced by phosphorylation level [PDF]

Scientific Reports, 2019
VX-770 (ivacaftor) is approved for clinical use in CF patients bearing multiple CFTR mutations. VX-770 potentiated wildtype CFTR and several disease mutants expressed in oocytes in a manner modulated by PKA-mediated phosphorylation.
G. Cui, Brandon Stauffer, Barry R. Imhoff, A. Rab, Jeong S. Hong, E. Sorscher, N. McCarty   +6 more
semanticscholar   +2 more sources

Selective Inhibition of NaV1.8 with VX-548 for Acute Pain.

New England Journal of Medicine, 2023
BACKGROUND The NaV1.8 voltage-gated sodium channel, expressed in peripheral nociceptive neurons, plays a role in transmitting nociceptive signals. The effect of VX-548, an oral, highly selective inhibitor of NaV1.8, on control of acute pain is being ...
Jim Jones, D. Correll, S. Lechner, Ina Jazic, Xiaopeng Miao, David Shaw, Christopher Simard, Jeremiah D. Osteen, Brian Hare, Alina Beaton, Todd Bertoch, A. Buvanendran, Ashraf S Habib, L. Pizzi, R. Pollak, S. Weiner, C. Bozic, PaulA . Negulescu, P. White   +18 more
semanticscholar   +1 more source

Theratyping of the Rare CFTR Genotype A559T in Rectal Organoids and Nasal Cells Reveals a Relevant Response to Elexacaftor (VX-445) and Tezacaftor (VX-661) Combination

International Journal of Molecular Sciences, 2023
Despite the promising results of new CFTR targeting drugs designed for the recovery of F508del- and class III variants activity, none of them have been approved for individuals with selected rare mutations, because uncharacterized CFTR variants lack ...
K. Kleinfelder, V. Villella, Anca Manuela Hristodor, C. Laudanna, G. Castaldo, F. Amato, P. Melotti, C. Sorio   +7 more
semanticscholar   +1 more source

Vx-809/Vx-770 treatment reduces inflammatory response to Pseudomonas aeruginosa in primary differentiated cystic fibrosis bronchial epithelial cells. [PDF]

American Journal of Physiology - Lung cellular and Molecular Physiology, 2018
M. Ruffin, Lucie Roussel, É. Maillé, S. Rousseau, E. Brochiero   +4 more
semanticscholar   +2 more sources

Phase 1 study of the ATR inhibitor berzosertib (formerly M6620, VX-970) combined with gemcitabine ± cisplatin in patients with advanced solid tumours

British Journal of Cancer, 2021
Berzosertib (formerly M6620, VX-970) is a highly potent and selective, first-in-class inhibitor of ataxia telangiectasia and Rad3-related protein kinase (ATR). We assessed multiple ascending doses of berzosertib + gemcitabine ± cisplatin in patients with
M. Middleton, E. Dean, T. Evans, G. Shapiro, John Pollard, B. Hendriks, M. Falk, I. Díaz-Padilla, R. Plummer   +8 more
semanticscholar   +1 more source

The anti-caspase 1 inhibitor VX-765 reduces immune activation, CD4+ T cell depletion, viral load, and total HIV-1 DNA in HIV-1 infected humanized mice

bioRxiv, 2022
Background HIV-1 infection results in the activation of inflammasome involving NLRP3, IFI16, caspase-1 and release of IL-1 β and IL-18. Early inflammasome activation may facilitate viral spread and establishment of the viral reservoir.
Mathieu Amand, Philipp Adams, Rafaëla Schober, Gilles Iserentant, J. Servais, M. Moutschen, C. Seguin-Devaux   +6 more
semanticscholar   +1 more source

VX-765 Alleviates β-Amyloid Deposition and Secondary Degeneration in the Ipsilateral Hippocampus and Ameliorates Cognitive Decline after Focal Cortical Infarction in Rats

Journal of Molecular Neuroscience, 2022
Focal cortical infarction leads to secondary degeneration of the ipsilateral hippocampus, which is associated with poststroke cognitive impairment.
D. Dong, Aihui Ren, Ying Yang, Jiayi Su, Libin Liu, Wen-Yan Zhuo, Yubin Liang   +6 more
semanticscholar   +1 more source

VX‐765 ameliorates renal injury and fibrosis in diabetes by regulating caspase‐1‐mediated pyroptosis and inflammation

Journal of Diabetes Investigation, 2021
As a lytic inflammatory cell death, pyroptosis has been recently described but has not been unequivocally elucidated in diabetic nephropathy (DN). VX‐765 is a safe and effective inhibitor of caspase‐1, that was well tolerated in a phase II clinical trial
Si Wen, F. Deng, Lulu Li, Li Xu, Xin Li, Qiuling Fan   +5 more
semanticscholar   +1 more source