Small‐Molecule Inhibitors of the Tumor Suppressor Fhit
Sign Up to like & getrecommendations! Published in 2017 at "ChemBioChem"
DOI: 10.1002/cbic.201700226
Abstract: The tumor suppressor Fhit and its substrate diadenosine triphosphate (Ap3A) are important factors in cancer development and progression. Fhit has Ap3A hydrolase activity and cleaves Ap3A into adenosine monophosphate (AMP) and adenosine diphosphate (ADP); this… read more here.
Keywords: fhit; suppressor fhit; tumor suppressor; small molecule ... See more keywords
Small‐Molecule Inhibitors of METTL3, the Major Human Epitranscriptomic Writer
Sign Up to like & getrecommendations! Published in 2020 at "ChemMedChem"
DOI: 10.1002/cmdc.202000011
Abstract: The RNA methylase METTL3 catalyzes the transfer of a methyl group from the cofactor S‐adenosyl‐L‐methionine (SAM) to the N6 atom of adenine. We have screened a library of 4000 analogues and derivatives of the adenosine… read more here.
Keywords: small molecule; human epitranscriptomic; molecule inhibitors; inhibitors mettl3 ... See more keywords
Small molecule inhibitors of mammalian thioredoxin reductase as potential anticancer agents: An update
Sign Up to like & getrecommendations! Published in 2019 at "Medicinal Research Reviews"
DOI: 10.1002/med.21507
Abstract: Mammalian thioredoxin reductase (TrxR) enzymes are homodimeric flavin proteins sharing a unique yet essential selenocysteine residue at their C‐terminus. TrxRs, together with their endogenous substrate thioredoxins, play a crucial role in regulating diverse cellular redox… read more here.
Keywords: thioredoxin reductase; molecule; inhibitors mammalian; small molecule ... See more keywords
Small-Molecule Inhibitors for the Treatment of Diffuse Large B Cell Lymphoma
Sign Up to like & getrecommendations! Published in 2018 at "Current Hematologic Malignancy Reports"
DOI: 10.1007/s11899-018-0467-5
Abstract: Purpose of ReviewDiffuse large B cell lymphoma (DLBCL) remains the most common non-Hodgkin lymphoma (NHL) in developed countries. Up to 30–40% of patients experience either refractory or relapsed disease following receipt of front-line chemoimmunotherapy, and… read more here.
Keywords: small molecule; treatment; molecule inhibitors; large cell ... See more keywords
Design, synthesis and activity of novel 2,6-disubstituted purine derivatives, potential small molecule inhibitors of signal transducer and activator of transcription 3.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.06.017
Abstract: Sustained activation of STAT3 is closely related to the cancer development, but the inhibitors for STAT3 overexpression are still in the clinical research stage. In this study, a series of 2,6-disubstituted purine derivatives were designed… read more here.
Keywords: disubstituted purine; purine derivatives; small molecule; molecule inhibitors ... See more keywords
Discovery and Mechanism of Small Molecule Inhibitors Selective for the Chromatin-Binding Domains of Oncogenic UHRF1.
Sign Up to like & getrecommendations! Published in 2022 at "Biochemistry"
DOI: 10.1021/acs.biochem.1c00698
Abstract: Chromatin abnormalities are common hallmarks of cancer cells, which exhibit alterations in DNA methylation profiles that can silence tumor suppressor genes. These epigenetic patterns are partly established and maintained by UHRF1 (ubiquitin-like PHD and RING… read more here.
Keywords: molecule inhibitors; small molecule; histone; chromatin ... See more keywords
Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01312
Abstract: KRAS, the most frequently mutated oncogene, plays a predominant role in driving initiation and progression of cancers. Decades of effort to target KRAS using small molecules has been unsuccessful, causing KRAS to be considered an… read more here.
Keywords: directly targeting; inhibitors directly; small molecule; chemistry ... See more keywords
Discovery of Small-Molecule Inhibitors of the PD-1/PD-L1 Axis That Promote PD-L1 Internalization and Degradation.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01682
Abstract: Several monoclonal antibodies targeting the programmed cell death-1/programmed cell death-ligand 1 (PD-1/PD-L1) pathway have been used successfully in anticancer immunotherapy. Inherent limitations of antibody-based therapies remain, however, and alternative small-molecule inhibitors that can block the… read more here.
Keywords: molecule inhibitors; small molecule; degradation; discovery ... See more keywords
Small Molecule Inhibitors of Lymphocyte Perforin as Focused Immunosuppressants for Infection and Autoimmunity
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c01338
Abstract: New drugs that precisely target the immune mechanisms critical for cytotoxic T lymphocyte (CTL) and natural killer (NK) cell driven pathologies are desperately needed. In this perspective, we explore the cytolytic protein perforin as a… read more here.
Keywords: molecule inhibitors; small molecule; inhibitors lymphocyte; perforin ... See more keywords
Carbohydrate Strengthens the Immunotherapeutic Effect of Small-Molecule PD-L1 Inhibitors.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01347
Abstract: PD-1/PD-L1 checkpoint blockade has demonstrated great success in cancer immunotherapy. Small-molecule PD-L1 inhibitors also attract significant research interests but remain challenging in the efficacy and safety. Carbohydrate moiety and carbohydrate-binding proteins (lectins) play important roles… read more here.
Keywords: molecule inhibitors; small molecule; carbohydrate; effect small ... See more keywords
Small Molecule Inhibitors of Protein Kinase D: Early Development, Current Approaches, and Future Directions.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01599
Abstract: Now entering its fourth decade, research on the biological function, small molecule inhibition, and disease relevance of the three known isoforms of protein kinase D, PKD1, PKD2, and PKD3, has entered a mature development stage.… read more here.
Keywords: molecule inhibitors; small molecule; protein kinase; development ... See more keywords