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p38 MAPK

Activity of Birinapant, a SMAC Mimetic Compound, Alone or in Combination in NSCLCs With Different Mutations

31 views | Dec 31 2020

Marika Colombo et al. showed how the use of Birinapant could be a viable therapeutic option for patients with LKB1-mutated NSCLCs. [Read the Full Post]

Phase 1 trial of ralimetinib (LY2228820) with radiotherapy plus concomitant temozolomide in the treatment of newly diagnosed glioblastoma

30 views | Dec 31 2020

J Biau et al. showed the phase 1 trial.This phase 1 trial was the first trial to study the combination of a p38-MAPK inhibitor, ralimetinib, with radiotherapy (RT) and chemotherapy (TMZ), in the treatment of newly diagnosed glioblastoma (GBM) patients. [Read the Full Post]

Physical Nature of Substituent Effects in XH/π Interactions

32 views | Dec 09 2020

Jacob W G Bloom et al. showed that the impact of substituents on XH/π interactions depended strongly on the identity of the XH group, and the strength of these effects increased with increasing polarization of the XH bond. [Read the Full Post]

Targeting of BCR-ABL1 and IRE1α induces synthetic lethality in Philadelphia-positive acute lymphoblastic leukemia

0 views | Nov 01 2020

Margherita Vieri et al. found that the identified combined action of nilotinib and MKC-8866 might represent a successful therapeutic strategy in high-risk Ph + ALL. [Read the Full Post]

Selective targeting of the αC and DFG-out pocket in p38 MAPK

42 views | Nov 01 2020

Sandra Röhm et al. provided valuable insights into back-pocket interactions that were not addressed in SR-318 and it provided an alternative chemical tool with good cellular activity targeting also the p38 back pocket. [Read the Full Post]

Transient Receptor Potential Ankyrin 1 (TRPA1) is Up-Regulated in Response to Lipopolysaccharide via P38/ Mitogen-Activated Protein Kinase (MAPK) in Dental Pulp Cells and Promotes Mineralization

69 views | Sep 22 2020

Kento Tazawa et al. demonstrated that LPS stimulation induced TRPA1 via the NO-p38 MAPK signaling pathway and TRPA1 agonists promoted differentiation or mineralization of dental pulp cells. [Read the Full Post]

SB203580 Protects Against Inflammatory Response and Lung Injury in a Mouse Model of lipopolysaccharide‑induced Acute Lung Injury

106 views | Jul 12 2020

Guirong Li et al. demonstrated that SB203580 protected against inflammatory responses and lung injury by inhibiting lung edema and downregulating proinflammatory mediators in LPS‑induced lung injury. [Read the Full Post]

Characterization of LY2228820 Dimesylate, a Potent and Selective Inhibitor of p38 MAPK With Antitumor Activity

119 views | Apr 26 2020

Robert M Campbell et al. showed that LY2228820 is a p38 MAPK inhibitor, which has been optimized for potency, selectivity, drug-like properties (such as oral bioavailability), and efficacy in animal models of human cancer. [Read the Full Post]

A First-in-Human Phase I Study of the Oral p38 MAPK Inhibitor, Ralimetinib (LY2228820 Dimesylate), in Patients With Advanced Cancer

138 views | Apr 26 2020

Amita Patnaik et al. demonstrated acceptable safety, tolerability, and pharmacokinetics for patients with advanced cancer. [Read the Full Post]

Inhibitory effect of 4-(4-fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)1H - imidazole on HCMV DNA replication and permissive infection

150 views | Mar 03 2020

Johnson RA et al. described FHPI as a novel anti-HCMV compound that inhibits synthesis/activation of cellular and/or viral factors required for initiation of HCMV DNA replication. [Read the Full Post]