Results 21 to 30 of about 79,283 (266)

A CRISPR screen identifies MAPK7 as a target for combination with MEK inhibition in KRAS mutant NSCLC. [PDF]

PLoS ONE, 2018
Mutant KRAS represents one of the most frequently observed oncogenes in NSCLC, yet no therapies are approved for tumors that express activated KRAS variants. While there is strong rationale for the use of MEK inhibitors to treat tumors with activated RAS/
Nicholas Dompe, Christiaan Klijn, Sara A Watson, Katherine Leng, Jenna Port, Trinna Cuellar, Colin Watanabe, Benjamin Haley, Richard Neve, Marie Evangelista, David Stokoe   +10 more
doaj   +1 more source

Current Development Status of MEK Inhibitors [PDF]

Molecules, 2017
The current development status of mitogen-activated protein kinase kinase (MEK) inhibitors, including the preclinical data and clinical study progress, has been summarized in this review. Different MEK inhibitors, possessing specific physicochemical properties and bioactivity characteristics, may provide different options for patients seeking treatment
Ying Cheng, Hongqi Tian
openaire   +3 more sources

A role for the unfolded protein response stress sensor ERN1 in regulating the response to MEK inhibitors in KRAS mutant colon cancers

Genome Medicine, 2018
Background Mutations in KRAS are frequent in human cancer, yet effective targeted therapeutics for these cancers are still lacking. Attempts to drug the MEK kinases downstream of KRAS have had limited success in clinical trials.
Tonći Šuštić, Sake van Wageningen, Evert Bosdriesz, Robert J. D. Reid, John Dittmar, Cor Lieftink, Roderick L. Beijersbergen, Lodewyk F. A. Wessels, Rodney Rothstein, René Bernards   +9 more
doaj   +1 more source

Reversing melanoma cross-resistance to BRAF and MEK inhibitors by co-targeting the AKT/mTOR pathway. [PDF]

PLoS ONE, 2011
The sustained clinical activity of the BRAF inhibitor vemurafenib (PLX4032/RG7204) in patients with BRAF(V600) mutant melanoma is limited primarily by the development of acquired resistance leading to tumor progression.
Mohammad Atefi, Erika von Euw, Narsis Attar, Charles Ng, Connie Chu, Deliang Guo, Ramin Nazarian, Bartosz Chmielowski, John A Glaspy, Begonya Comin-Anduix, Paul S Mischel, Roger S Lo, Antoni Ribas   +12 more
doaj   +1 more source

Hubungan Kuantitatif Struktur-Aktivitas (HKSA) dan Penambatan Molekul Senyawa Turunan Benzamida sebagai Inhibitor Alosterik Mitogen Enhanced Kinase (MEK)

Jurnal Kimia Valensi, 2018
Jalur sinyal protein kinase Ras-Raf-MEK-ERK adalah salah satu target penting dalam penemuan obat antikanker. Senyawa turunan benzamida diketahui berpotensi sebagai inhibitor alosterik Mitogen Enhanced Kinase (MEK).
Muhammad Arba, Ruslin Ruslin, Nursan Nursan, Maulidiyah Maulidiyah, Daryono Hadi Tjahjono   +4 more
doaj   +1 more source

MEK and the inhibitors: from bench to bedside [PDF]

Journal of Hematology & Oncology, 2013
Abstract Four distinct MAP kinase signaling pathways involving 7 MEK enzymes have been identified. MEK1 and MEK2 are the prototype members of MEK family proteins. Several MEK inhibitors are in clinical trials. Trametinib is being evaluated by FDA for the treatment of metastatic melanoma with BRAF V600 mutation. Selumetinib has been studied in
Akinleye, Akintunde, Furqan, Muhammad, Mukhi, Nikhil, Ravella, Pavan, Liu, Delong   +4 more
openaire   +2 more sources

Inhibition of MEK-ERK pathway enhances oncolytic vaccinia virus replication in doxorubicin-resistant ovarian cancer

Molecular Therapy: Oncolytics, 2022
Oncolytic vaccinia virus (OVV) has been reported to induce cell death in various types of cancer; however, the oncolytic activity of OVV in drug-resistant ovarian cancer remains limited.
Seoyul Lee, Wookyeom Yang, Dae Kyoung Kim, Hojun Kim, Minjoo Shin, Kyung Un Choi, Dong Soo Suh, Yun Hak Kim, Tae-Ho Hwang, Jae Ho Kim   +9 more
doaj   +1 more source

Combination of a Selective HSP90α/β Inhibitor and a RAS-RAF-MEK-ERK Signaling Pathway Inhibitor Triggers Synergistic Cytotoxicity in Multiple Myeloma Cells.

PLoS ONE, 2015
Heat shock protein (HSP)90 inhibitors have shown significant anti-tumor activities in preclinical settings in both solid and hematological tumors. We previously reported that the novel, orally available HSP90α/β inhibitor TAS-116 shows significant anti ...
Rikio Suzuki, Shohei Kikuchi, Takeshi Harada, Naoya Mimura, Jiro Minami, Hiroto Ohguchi, Yasuhiro Yoshida, Morihiko Sagawa, Gullu Gorgun, Diana Cirstea, Francesca Cottini, Jana Jakubikova, Yu-Tzu Tai, Dharminder Chauhan, Paul G Richardson, Nikhil Munshi, Kiyoshi Ando, Teruhiro Utsugi, Teru Hideshima, Kenneth C Anderson   +19 more
doaj   +1 more source

MEK inhibition induced downregulation of MRP1 and MRP3 expression in experimental hepatocellular carcinoma

Cancer Cell International, 2013
Background Hepatocellular carcinoma (HCC) exhibits strong intrinsic and acquired drug resistance which is the main obstacle to chemotherapy. Overexpression of ATP binding cassette (ABC) proteins correlates with activation of mitogen activated protein ...
Lin Shibo, Hoffmann Katrin, Xiao Zhi, Jin Nan, Galli Uwe, Mohr Elvira, Büchler Markus W, Schemmer Peter   +7 more
doaj   +1 more source

PD-L1 induction via the MEK-JNK-AP1 axis by a neddylation inhibitor promotes cancer-associated immunosuppression

Cell Death and Disease, 2022
MLN4924 is a first-in-class small molecule inhibitor of NEDD8-activating enzyme (NAE), which is currently in several clinical trials for anti-cancer applications.
Shizhen Zhang, Xiahong You, Tiantian Xu, Qian Chen, Hua Li, Longyu Dou, Yilun Sun, Xiufang Xiong, Morgan A. Meredith, Yi Sun   +9 more
doaj   +1 more source