A small molecule inhibitor of VSIG-8 prevents its binding to VISTA
Sign Up to like & getrecommendations! Published in 2022 at "Investigational New Drugs"
DOI: 10.1007/s10637-022-01244-4
Abstract: The V-region immunoglobulin-containing suppressor of T cell activation (VISTA), a unique B7 family member, is an attractive immunotherapeutic target for cancer, autoimmune and inflammatory diseases. In 2016, a patent demonstrated V-Set and Immunoglobulin domain containing… read more here.
Keywords: vsig; small molecule; inhibitor vsig; vista ... See more keywords
Small molecule inhibitor agerafenib effectively suppresses neuroblastoma tumor growth in mouse models via inhibiting ERK MAPK signaling.
Sign Up to like & getrecommendations! Published in 2019 at "Cancer letters"
DOI: 10.1016/j.canlet.2019.05.011
Abstract: Neuroblastoma (NB) is the most common extracranial solid tumor in early childhood. Despite intensive multimodal therapy, nearly half of children with high-risk disease will relapse with therapy-resistant tumors. Dysregulation of MAPK pathway has been implicated… read more here.
Keywords: molecule inhibitor; small molecule; mapk signaling; agerafenib ... See more keywords
A small-molecule inhibitor of MDMX suppresses cervical cancer cells via the inhibition of E6-E6AP-p53 axis.
Sign Up to like & getrecommendations! Published in 2022 at "Pharmacological research"
DOI: 10.1016/j.phrs.2022.106128
Abstract: Dysfunction of p53 is observed in many malignant tumors, which is related to cancer susceptibility. In cervical cancer, p53 is primarily degradated through the complex of high-risk human papillomaviruses (HPV) oncoprotein E6 and E6-associated protein… read more here.
Keywords: cancer; cervical cancer; small molecule; p53 ... See more keywords
Novel Small-Molecule PD-L1 Inhibitor Induces PD-L1 Internalization and Optimizes the Immune Microenvironment.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01801
Abstract: Blocking the PD-1/PD-L1 interaction has become an important strategy for tumor therapy, which has shown outstanding therapeutic effects in clinical settings. However, unsatisfactory response rates and immune-related adverse effects limit the use of anti-PD1/PD-L1 antibodies.… read more here.
Keywords: small molecule; internalization; tumor; molecule inhibitor ... See more keywords
Rational Design of a Robust Antibody-Like Small Molecule Inhibitor Nanoplatform for Enhanced Photoimmunotherapy.
Sign Up to like & getrecommendations! Published in 2020 at "ACS applied materials & interfaces"
DOI: 10.1021/acsami.0c11156
Abstract: Immune checkpoint blockade of programmed cell death-ligand 1/programmed cell death-1 (PD-L1/PD-1) pathway via antibody is a potent strategy for T cells remodeling. Nevertheless, the potency of antibody is partly compromised by its high price, instability,… read more here.
Keywords: molecule inhibitor; molecule; nanoplatform; small molecule ... See more keywords
First‐in‐human study of deucravacitinib: A selective, potent, allosteric small‐molecule inhibitor of tyrosine kinase 2
Sign Up to like & getrecommendations! Published in 2022 at "Clinical and Translational Science"
DOI: 10.1111/cts.13435
Abstract: This randomized, double‐blind, single‐ and multiple‐ascending dose study assessed the pharmacokinetics (PKs), pharmacodynamics, and safety of deucravacitinib (Sotyktu™), a selective and potent small‐molecule inhibitor of tyrosine kinase 2, in 100 (75 active, 25 placebo) healthy… read more here.
Keywords: small molecule; selective potent; inhibitor tyrosine; molecule inhibitor ... See more keywords
Small-molecule inhibitor targeting the Hsp90-Cdc37 protein-protein interaction in colorectal cancer
Sign Up to like & getrecommendations! Published in 2019 at "Science Advances"
DOI: 10.1126/sciadv.aax2277
Abstract: Directly disrupting the Hsp90-Cdc37 complex can selectively down-regulate kinase clients of Hsp90 and achieve cell cycle arrest. Disrupting the interactions between Hsp90 and Cdc37 is emerging as an alternative and specific way to regulate the… read more here.
Keywords: cdc37; small molecule; molecule inhibitor; hsp90 cdc37 ... See more keywords
Abstract LB-193: Protein phosphatase 2A inhibition,with a novel small molecule inhibitor, LB-100, achieves durable immune-mediated antitumor activity when combined with PD1 blockade in a preclinical model
Sign Up to like & getrecommendations! Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-lb-193
Abstract: LB-100 is a novel, first-in-class, small molecule inhibitor of protein phosphatase 2A (PP2A) recently shown in a Phase I trial to be well-tolerated at doses associated with stabilization of progressive solid tumors (Chung. Clin Cancer… read more here.
Keywords: molecule inhibitor; cd4 cells; small molecule; treatment ... See more keywords
RK-33, a small molecule inhibitor of host RNA helicase DDX3, suppresses multiple variants of SARS-CoV-2
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Microbiology"
DOI: 10.3389/fmicb.2022.959577
Abstract: SARS-CoV-2, the virus behind the deadly COVID-19 pandemic, continues to spread globally even as vaccine strategies are proving effective in preventing hospitalizations and deaths. However, evolving variants of the virus appear to be more transmissive… read more here.
Keywords: small molecule; rna helicase; molecule inhibitor; host ... See more keywords
Discovery of a Small Molecule Inhibitor of Human Adenovirus Capable of Preventing Escape from the Endosome
Sign Up to like & getrecommendations! Published in 2021 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms22041617
Abstract: Human adenoviruses (HAdVs) display a wide range of tissue tropism and can cause an array of symptoms from mild respiratory illnesses to disseminated and life-threatening infections in immunocompromised individuals. However, no antiviral drug has been… read more here.
Keywords: molecule inhibitor; discovery small; inhibitor; small molecule ... See more keywords
Inhibition of neuroblastoma proliferation by PF-3758309, a small-molecule inhibitor that targets p21-activated kinase 4
Sign Up to like & getrecommendations! Published in 2017 at "Oncology Reports"
DOI: 10.3892/or.2017.5989
Abstract: Neuroblastoma is the most common extracranial solid childhood tumor. Despite the availability of advanced multimodal therapy, high-risk patients still have low survival rates. p21-activated kinase 4 (PAK4) has been shown to regulate many cellular processes… read more here.
Keywords: molecule inhibitor; p21 activated; small molecule; activated kinase ... See more keywords