Results 21 to 30 of about 81,917 (261)

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

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

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

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

Ligand‐dependent transcriptional heterogeneity in cell cycle gene expression delays G1/S entry

FEBS Letters, EarlyView.
EGF and HRG induce distinct G1/S progression programs in ErbB2‐amplified BT474 breast cancer cells. Despite activating the potent ErbB2–ErbB3 heterodimer, HRG does not accelerate cell‐cycle entry. Instead, EGF promotes earlier restriction‐point passage via ERK–FOS signaling, whereas HRG activates the AKT–MYC axis, driving transcriptional heterogeneity ...
Ririn Rahmala Febri, Ayaka Nagasato‐Ichikawa, Keita Iida, Shuhei Kimura, Akira Imamoto, Mariko Okada   +5 more
wiley   +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

Off-Target Effects of MEK Inhibitors [PDF]

Biochemistry, 2013
The mitogen-activated protein kinases (MAPKs) ERK1/2 regulate numerous cellular processes, including gene transcription, proliferation, and differentiation. The only known substrates of the MAP2Ks MEK1/2 are ERK1/2; thus, MEK inhibitors PD98059, U0126, and PD0325901 have been important tools in determining the functions of ERK1/2.
Eric M, Wauson, Marcy L, Guerra, Barbara, Barylko, Joseph P, Albanesi, Melanie H, Cobb   +4 more
openaire   +2 more sources

A context‐dependent modulatory role for eIF6 in acquired resistance to vemurafenib in melanoma

FEBS Letters, EarlyView.
Acquired resistance to vemurafenib upregulates the translation factor eIF6 in melanoma cells. Silencing eIF6 in resistant cells reduces proliferation and partially restores drug sensitivity, whereas its overexpression increases sensitivity across melanoma lines regardless of BRAF status, via modulation of mTOR, S6K, and MAPK signaling.
George Kyriakopoulos, Antonia Petropoulou, Alexandra Anastogianni, Angelina Bania, Vassilis Stamatakis, Argyris Alexiou, Chi‐Ping Day, Glenn Merlino, Katerina Grafanaki, Constantinos Stathopoulos   +9 more
wiley   +1 more source