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ESKM, a novel therapeutic agent for sensitive and resistant PH+ leukemias

Effects of PARP inhibitors in BRCA gene-mutated ovarian cancer

The mechanism of resistance to JAK2 inhibitor in myeloproliferative neoplasms patients

DASATINIB; An inhibitor of Receptor Tyrosine Kinase

GP130/JAK/STAT3 signaling pathway induces multiple myeloma

E1 Activating

Blocking neddylation elicits antiviral effect against hepatitis B virus replication

52 views | Nov 23 2021

Karima Abounouh et al. provided new tools interfering with HBV persistence as well as novel therapeutic strategies against chronic hepatitis B. [Read the Full Post]

Pevonedistat attenuates cisplatin-induced nephrotoxicity in mice by downregulating the release of inflammatory mediators

123 views | Sep 22 2021

Yousra M El-Far et al. found that pevonedistat alleviated CIS-induced nephrotoxicity that might be attributed to suppression of the inflammation induced in renal tissue. [Read the Full Post]

Direct Conjugation of NEDD8 to the N-Terminus of a Model Protein Can Induce Degradation

256 views | May 03 2021

Kartikeya Vijayasimha et al. suggested that under certain conditions, such as the model system described here, the covalent linkage of NEDD8 to a protein substrate might result in the target proteins degradation. [Read the Full Post]

SLFN11 inactivation induces proteotoxic stress and sensitizes cancer cells to ubiquitin activating enzyme inhibitor TAK-243

267 views | May 01 2021

Yasuhisa Murai et al. found that findings uncover a previously unknown function of SLFN11 as a regulator of protein quality control and attenuator of ER stress and UPR. Moreover, they suggest the potential value of TAK-243 in SLFN11-deficient tumors. [Read the Full Post]

Neddylation inhibitor MLN4924 has anti-HBV activity via modulating the ERK-HNF1α-C/EBPα-HNF4α axis

180 views | Dec 05 2020

Mingjie Xie et al. revealed that neddylation inhibitor MLN4924 had impressive anti-HBV activity by inhibiting HBV replication, thus providing sound rationale for future MLN4924 clinical trial as a novel anti-HBV therapy. [Read the Full Post]

Pevonedistat (MLN4924): mechanism of cell death induction and therapeutic potential in colorectal cancer

174 views | Sep 15 2020

Jennifer Ferris et al. suggested that this second-generation proteostasis-disrupting agent might have its most widespread activity in CRC, in combination with irinotecan-containing treatment regimens. [Read the Full Post]

Blocking PD1/PDL1 Interactions Together With MLN4924 Therapy Is a Potential Strategy for Glioma Treatment

251 views | Feb 26 2020

Natalia Filippova et al. concluded that i) PDL1 up-regulation in gliomas and the glioma microenvironment is an important chemotherapeutic target; ii) MLN4924 therapy, combined with a blockage of the PD1/PDL1 pathway, should be considered as a potential strategy for glioma treatment. [Read the Full Post]

Pevonedistat (MLN4924), a First-in-Class NEDD8-activating enzyme inhibitor, in patients with acute myeloid leukaemia and myelodysplastic syndromes: a phase 1 study

0 views | Dec 28 2019

Swords RT et al. indicated that administration of the first-in-class agent, pevonedistat, was feasible in patients with MDS and AML and modest clinical activity was observed. [Read the Full Post]

Pevonedistat (MLN4924), a First-in-Class NEDD8-activating enzyme inhibitor, in patients with acute myeloid leukaemia and myelodysplastic syndromes: a phase 1 study

369 views | Jul 08 2019

Swords RT et al. indicated that administration of the first-in-class agent, pevonedistat, was feasible in patients with MDS and AML and modest clinical activity was observed. [Read the Full Post]

Identifying Regulatory Posttranslational Modifications of PD-L1: A Focus on Monoubiquitinaton

565 views | Aug 04 2018

Horita H et al. highlights the significance of identifying novel PTMs for PD-L1 and reveals potentially critical regulatory mechanisms that may be valuable therapeutic targets. In a broader context, this report validates an approach whereby one can gain insight into novel mechanisms of action by a simple and unbiased analysis of a PTM profile of potentially any endogenous protein of interest. [Read the Full Post]