Pyrrolopyridazine MEK Inhibitors.

ChemInform ◽  
2006 ◽  
Vol 37 (18) ◽  
Author(s):  
Zhong Chen ◽  
et al. et al.
Keyword(s):  
Mek Inhibitors

MEK inhibitors in fracture healing and NF1 pseudarthrosis

2013 ◽  
Author(s):  
David Little ◽  
Jad El-Hoss ◽  
Mille Kollind ◽  
Nikita Deo ◽  
Michelle McDonald ◽  
...  
Keyword(s):  
Fracture Healing ◽  
Mek Inhibitors

Prolonged survival of a patient with brain melanoma metastasis treated with BRAF and MEK inhibitors combination therapy

2020 ◽  
Vol 155 (2) ◽  
Author(s):  
Giulia Spallone ◽  
Virginia Garofalo ◽  
Eliseo Picchi ◽  
Rossella Pitocco ◽  
Federico Bianchi ◽  
...  
Keyword(s):  
Combination Therapy ◽  
Prolonged Survival ◽  
Melanoma Metastasis ◽  
Mek Inhibitors

scholarly journals Monosomy 3 Is Linked to Resistance to MEK Inhibitors in Uveal Melanoma

2021 ◽  
Vol 22 (13) ◽  
pp. 6727
Author(s):  
Svenja Mergener ◽  
Jens T. Siveke ◽  
Samuel Peña-Llopis
Keyword(s):  
Cell Lines ◽  
Uveal Melanoma ◽  
Survival Data ◽  
Translation Initiation Factor ◽  
The Cancer Genome Atlas ◽  
Initiation Factor ◽  
Chromosome 3 ◽  
Mek Inhibitors ◽  
Mek Inhibition ◽  
Insight Into

The use of MEK inhibitors in the therapy of uveal melanoma (UM) has been investigated widely but has failed to show benefits in clinical trials due to fast acquisition of resistance. In this study, we investigated a variety of therapeutic compounds in primary-derived uveal melanoma cell lines and found monosomy of chromosome 3 (M3) and mutations in BAP1 to be associated with higher resistance to MEK inhibition. However, reconstitution of BAP1 in a BAP1-deficient UM cell line was unable to restore sensitivity to MEK inhibition. We then compared UM tumors from The Cancer Genome Atlas (TCGA) with mutations in BAP1 with tumors with wild-type BAP1. Principal component analysis (PCA) clearly differentiated both groups of tumors, which displayed disparate overall and progression-free survival data. Further analysis provided insight into differential expression of genes involved in signaling pathways, suggesting that the downregulation of the eukaryotic translation initiation factor 2A (EIF2A) observed in UM tumors with BAP1 mutations and M3 UM cell lines might lead to a decrease in ribosome biogenesis while inducing an adaptive response to stress. Taken together, our study links loss of chromosome 3 with decreased sensitivity to MEK inhibition and gives insight into possible related mechanisms, whose understanding is fundamental to overcome resistance in this aggressive tumor.

Combining BRAF/MEK Inhibitors with Immunotherapy in the Treatment of Metastatic Melanoma

2021 ◽  
Vol 22 (3) ◽  
pp. 301-314
Author(s):  
Dimitrios C. Ziogas ◽  
Frosso Konstantinou ◽  
Spyros Bouros ◽  
Maria Theochari ◽  
Helen Gogas
Keyword(s):  
Metastatic Melanoma ◽  
Mek Inhibitors

scholarly journals Overcoming Adaptive Resistance to KRAS and MEK Inhibitors by Co-targeting mTORC1/2 Complexes in Pancreatic Cancer

2020 ◽  
Vol 1 (8) ◽  
pp. 100131
Author(s):  
Wells S. Brown ◽  
Paul C. McDonald ◽  
Oksana Nemirovsky ◽  
Shannon Awrey ◽  
Shawn C. Chafe ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Mek Inhibitors ◽  
Adaptive Resistance

scholarly journals MEK inhibitors potentiate dexamethasone lethality in acute lymphoblastic leukemia cells through the pro-apoptotic molecule BIM

Leukemia ◽  
2009 ◽  
Vol 23 (10) ◽  
pp. 1744-1754 ◽  
Author(s):  
A A Rambal ◽  
Z L G Panaguiton ◽  
L Kramer ◽  
S Grant ◽  
H Harada
Keyword(s):  
Acute Lymphoblastic Leukemia ◽  
Lymphoblastic Leukemia ◽  
Leukemia Cells ◽  
Mek Inhibitors

Outcome of combination therapy using BRAF and MEK inhibitors among Asian patients with advanced melanoma: An analysis of 112 cases

2021 ◽  
Vol 145 ◽  
pp. 210-220
Author(s):  
Yasuhiro Fujisawa ◽  
Takamichi Ito ◽  
Hiroshi Kato ◽  
Hiroyuki Irie ◽  
Tatsuya Kaji ◽  
...  
Keyword(s):  
Combination Therapy ◽  
Advanced Melanoma ◽  
Mek Inhibitors ◽  
Asian Patients
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