Results 201 to 210 of about 984,321 (234)

Chimeric deubiquitinase engineering reveals structural basis for specific inhibition of the mitophagy regulator USP30. [PDF]

Nat Struct Mol Biol
Kazi NH, Klink N, Gallant K, Kipka GM, Gersch M.   +4 more
europepmc   +1 more source

Design, Synthesis, and Evaluation of Naphthyl Pyrazino-Pyrido-Pyrimidinones Targeting the Phosphoinositide 3-Kinase/Alpha-Serine/Protein Kinase B/Mammalian Target of Rapamycin Pathway. [PDF]

ChemistryOpen
Marchiori MF, da Silva G, Kawano DF, Leopoldino AM, Madruga E, Martinez A, Carvalho I.   +6 more
europepmc   +1 more source

Magistral Galenic Preparations in Modern Dermatology: Our Top 10 Picks for Bridging Therapeutic Gaps. [PDF]

Medicina (Kaunas)
Cammarata E, Esposto E, Gironi LC, Zavattaro E, Savoia P.   +4 more
europepmc   +1 more source

Unifoliolate Leaves Are Compound in Neotropical Rutaceae: Novel Evidence from Lateral Leaflet Traces. [PDF]

Plants (Basel)
Raymundo CEV, Pirani JR, de Albuquerque Melo-de-Pinna GF.   +2 more
europepmc   +1 more source

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USP8 inhibitor RA-9 reduces ACTH release and cell growth in tumor corticotrophs

Endocrine-Related Cancer, 2021
Cushing’s disease (CD) is a rare endocrine disorder caused by an adrenocorticotropic hormone (ACTH)-secreting pituitary tumor. Pasireotide is the only pituitary-targeted drug approved for adult patients. Nevertheless, many side effects are encountered and curative therapy is still challenging.
Donatella Treppiedi, Genesio Di Muro, Giusy Marra, Anna Maria Barbieri, Federica Mangili, Rosa Catalano, Andreea Serban, Emanuele Ferrante, Marco Locatelli, Andrea G Lania, Maura Arosio, Anna Spada, Erika Peverelli, Giovanna Mantovani   +13 more
openaire   +2 more sources

Design and Synthesis of KRAS ^G12C Inhibitors for Antitumor Evaluation Harboring Combination Therapy with Nrf2, PARP-7, and Pan-USP Inhibitors to Alleviate Drug Resistance Synergistically

Journal of Medicinal Chemistry
Compared with positive control MRTX849, the synthesized compounds 7g, 7p, 7q, 7r, 7v, and 7y displayed stronger antiproliferative activities against H358 cells with IC50 values of < 1 nM (3D cell culture) and comparable inhibitory potency against KRASG12C.
Liangliang Tian, Qingxuan Han, Yanlong Qiao, Peng Chu, Lixue Chen   +4 more
openaire   +2 more sources

The deubiquitinating enzyme USP 8 promotes tyrosine kinase inhibitors resistance in chronic myeloid leukemia by stabilizing EIF 2 S 1 protein

The FEBS Journal
Tyrosine kinase inhibitors (TKIs), targeted therapeutic agents, have significantly improved survival outcomes in patients with chronic myeloid leukemia (CML). However, the emergence of drug resistance remains a challenge, with the underlying mechanisms still largely unknown.
Shan Zhang, Hurong Lai, Wanwan Bao, Caifeng Liao, Jian Li   +4 more
openaire   +1 more source

Abstract 3665: Insilco evaluation of multiple ubiquitin-specific protease 1 (USP1) inhibitors and selectivity profiling over other USPs using Alphafold

Cancer Research
Abstract DNA damage triggers cell signaling cascades that mediate repair. This signaling is frequently dysregulated in cancers. The proteins that mediate this signaling are potential targets for therapeutic intervention. Ubiquitin-specific protease 1 (USP1) is one such target, with small-molecule inhibitors already in clinical trials ...
Prashant Kashinath Bhavar, Uday Kumar Surampudi, Appaji Baburao Mandhare, Rupesh Chikhale   +3 more
openaire   +1 more source

Corrigendum to “Subquinocin, a small molecule inhibitor of CYLD and USP-family deubiquitinating enzymes, promotes NF-κB signaling” [Biochem. Biophys. Res. Commun. 524 (1) (2020) 1–7]

Biochemical and Biophysical Research Communications, 2021
Satoshi Yamanaka, Yusuke Sato, Daisuke Oikawa, Eiji Goto, Shuya Fukai, Fuminori Tokunaga, Hirotaka Takahashi, Tatsuya Sawasaki   +7 more
openaire   +1 more source