Small-molecule inhibitors targeting small ubiquitin-like modifier pathway for the treatment of cancers and other diseases.
Sign Up to like & getrecommendations! Published in 2022 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2022.114227
Abstract: SUMOylation is a key post-translational modification that involves the covalent attachment of small ubiquitin-like modifier (SUMO) to the lysine residues of target proteins. The well-balanced SUMOylation is essential for normal cellular behaviors, while disturbance of… read more here.
Keywords: cancers diseases; small ubiquitin; like modifier; ubiquitin like ... See more keywords
Modeling the Structure–Activity Relationship of Arbidol Derivatives and Other SARS-CoV-2 Fusion Inhibitors Targeting the S2 Segment of the Spike Protein
Sign Up to like & getrecommendations! Published in 2021 at "Journal of Chemical Information and Modeling"
DOI: 10.1021/acs.jcim.1c01061
Abstract: Umifenovir (Arbidol) has been reported to exhibit some degree of efficacy in multiple clinical trials for the treatment of COVID-19 as a monotherapy. It has also demonstrated synergistic inhibition of SARS-CoV-2 with other direct-acting antivirals… read more here.
Keywords: segment; sars cov; spike protein; fusion inhibitors ... See more keywords
Potent Long-Acting Inhibitors Targeting the HIV-1 Capsid Based on a Versatile Quinazolin-4-one Scaffold.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01732
Abstract: Long-acting (LA) human immunodeficiency virus-1 (HIV-1) antiretroviral therapy characterized by a ≥1 month dosing interval offers significant advantages over daily oral therapy. However, the criteria for compounds that enter clinical development are high. Exceptional potency… read more here.
Keywords: inhibitors targeting; potent long; hiv; long acting ... See more keywords
Synthesis of Novel Kidney-Type Glutaminase Allosteric Inhibitors Targeting the Critical Lys-320 Residue.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00302
Abstract: Reversible allosteric inhibitors of kidney-type glutaminase (GLS1, KGA) showed incomplete inhibition of cancer cell proliferation and poor in vivo efficacy. Here, we investigate some irreversible inhibitors targeting the critical K320 residue responsible for GLS1 biological… read more here.
Keywords: inhibitors targeting; kidney type; targeting critical; type glutaminase ... See more keywords
In silico identification of potential inhibitors targeting Streptococcus mutans sortase A
Sign Up to like & getrecommendations! Published in 2017 at "International Journal of Oral Science"
DOI: 10.1038/ijos.2016.58
Abstract: Dental caries is one of the most common chronic diseases and is caused by acid fermentation of bacteria adhered to the teeth. Streptococcus mutans (S. mutans) utilizes sortase A (SrtA) to anchor surface proteins to… read more here.
Keywords: potential inhibitors; silico identification; identification potential; streptococcus mutans ... See more keywords
Novel natural inhibitors targeting KRAS G12C by computational study
Sign Up to like & getrecommendations! Published in 2022 at "Anti-Cancer Drugs"
DOI: 10.1097/cad.0000000000001317
Abstract: Ideal leading and nominee compounds with inhibiting effects on KRAS G12C were selected from the ZINC database, laying a cornerstone for the progress of anticancer drugs. A variety of computational virtual screening methods were utilized… read more here.
Keywords: kras g12c; inhibitors targeting; zinc000012494057 zinc000003789195; natural inhibitors ... See more keywords
Rational design and synthesis of angiotensin-converting enzyme 2 inhibitors targeting severe acute respiratory syndrome coronavirus 2
Sign Up to like & getrecommendations! Published in 2023 at "Physiology"
DOI: 10.1152/physiol.2023.38.s1.5735074
Abstract: Objectives: The coronavirus disease 2019 (COVID-19) is still a global health concern caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The functional entry receptor utilized by SARS-CoV-2 is Angiotensin-Converting Enzyme 2 (ACE2). ACE2… read more here.
Keywords: inhibitors targeting; covid; physiology; mln 4760 ... See more keywords
Inhibitors Targeting YAP in Gastric Cancer: Current Status and Future Perspectives
Sign Up to like & getrecommendations! Published in 2021 at "Drug Design, Development and Therapy"
DOI: 10.2147/dddt.s308377
Abstract: Abstract Gastric cancer (GC) is one of the most common cancers globally, threatening global health. The deregulation of the Hippo signaling pathway has been discovered in GC and may be related to cancer development, proliferation,… read more here.
Keywords: targeting yap; yap gastric; cancer; gastric cancer ... See more keywords
Viral Entry Inhibitors Targeting Six-Helical Bundle Core Against Highly Pathogenic Enveloped Viruses with Class I Fusion Proteins.
Sign Up to like & getrecommendations! Published in 2021 at "Current medicinal chemistry"
DOI: 10.2174/0929867328666210511015808
Abstract: TypeⅠ enveloped viruses bind to cell receptors through surface glycoproteins to initiate infection or undergo receptor-mediated endocytosis. They also initiate membrane fusion in the acidic environment of endocytic compartments, releasing genetic material into the cell.… read more here.
Keywords: entry inhibitors; bundle; enveloped viruses; fusion ... See more keywords
Medicinal Chemistry of Inhibitors Targeting Resistant Bacteria.
Sign Up to like & getrecommendations! Published in 2022 at "Current topics in medicinal chemistry"
DOI: 10.2174/1568026622666220321124452
Abstract: The discovery of antibiotics was a revolutionary feat that provided countless health benefits. The identification of penicillin by Alexander Fleming initiated the era of antibiotics, represented by constant discoveries that enabled effective treatments for the… read more here.
Keywords: chemistry; chemistry inhibitors; medicinal chemistry; bacterial resistance ... See more keywords
Potential Inhibitors Targeting Papain-Like Protease of SARS-CoV-2: Two Birds With One Stone
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Chemistry"
DOI: 10.3389/fchem.2022.822785
Abstract: Severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2), the pathogen of the Coronavirus disease-19 (COVID-19), is still devastating the world causing significant chaos to the international community and posing a significant threat to global health. Since the… read more here.
Keywords: sars cov; potential inhibitors; papain like; like protease ... See more keywords