Results 41 to 50 of about 130,251 (209)

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

CRAF R391W is a melanoma driver oncogene. [PDF]

, 2016
Approximately 75% of melanomas have known driver oncogenic mutations in BRAF, NRAS, GNA11 or GNAQ, while the mutations providing constitutive oncogenic signaling in the remaining melanomas are not known.
Atefi, Mohammad, Avramis, Earl, Chmielowski, Bartosz, Friedman, Michael, Graeber, Thomas G, Lassen, Amanda, Le, Allison, Lomova, Anastasia, Ng, Charles, Ribas, Antoni, Titz, Bjoern, Tsoi, Jennifer   +11 more
core   +3 more sources

Activation of MAPK signalling results in resistance to saracatinib (AZD0530) in ovarian cancer [PDF]

, 2017
SRC tyrosine kinase is frequently overexpressed and activated in late-stage, poor prognosis ovarian tumours, and preclinical studies have supported the use of targeted SRC inhibitors in the treatment of this disease.
El-Helali, Aya, Kennedy, Richard D., McCabe, Nuala, McGivern, Niamh, Mcneish, Iain A., Mullan, Paul, Paul Harkin, D   +6 more
core   +2 more sources

Preconditioning of mesenchymal stromal cells with low-intensity ultrasound: influence on chondrogenesis and directed SOX9 signaling pathways [PDF]

, 2020
Background: Continuous low-intensity ultrasound (cLIUS) facilitates the chondrogenic differentiation of human mesenchymal stromal cells (MSCs) in the absence of exogenously added transforming growth factor-beta (TGFβ) by upregulating the expression of ...
A Argentaro, A Augello, A Katsumi, A Woods, A Woods, AD Miller, AH Huang, B Yang, BH Choi, C Huang, C Matta, CA Simmons, CB Little, CJ O’Conor, CY Huang, D Schumann, DR Haudenschild, EM Darling, F Dell'Accio, G Coricor, H Sim, H-C Hsu, HJ Kwon, HJ Lee, HJ Lee, J Li, J Puetzer, JC Sng, JD Kisiday, JH Cui, JH Cui, JW Choi, K Ebisawa, K Pelttari, L Bian, Li Ling, LJ Ng, M Shakibaei, M Tsuda, MA Corrigan, MB Mueller, N Fahy, N Thelin, NP Whitney, P Müller, R Ogawa, RL Mauck, RM Delaine-Smith, RS Tigli, S Murakami, S Noriega, S Noriega, S Yamaguchi, SD Cook, SD Cook, T Furumatsu, T Guo, T Ito, T Juhasz, T Nishida, T Sanjukta Guha, TM Louw, V Lefebvre, V Lefebvre, W Huang, W Huang, Z Li, ZJ Zhang   +67 more
core   +2 more sources

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

AurkA inhibitors enhance the effects of B-RAF and MEK inhibitors in melanoma treatment [PDF]

, 2014
Background: Aurora kinase A (AurkA) is over-expressed in melanoma and its inhibition has been observed to limit tumor growth, suggesting a potential role in melanoma treatment. Methods: A human melanoma cell line with the B-RAF (V600E) mutation (A375mel)
Ascierto, Paolo Antonio, Botti, Gerardo, Caputo, Emilia, Carriero, Maria Vincenza, Cavalcanti, Ernesta, Ciliberto, Gennaro, Fratangelo, Federica, Miceli, Roberta, Motti, Maria Letizia, Mozzillo, Nicola, Palmieri, Giuseppe, Pirozzi, Giuseppe, Taté, Rosarita   +12 more
core   +2 more sources

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

Harnessing autophagy to overcome mitogen‐activated protein kinase kinase inhibitor‐induced resistance in metastatic melanoma [PDF]

, 2019
Background Patients with malignant melanoma often relapse after treatment with BRAF and/or mitogen‐activated protein kinase kinase (MEK) inhibitors (MEKi) owing to development of drug resistance.
Alexander, M., Chaudhry, B., Edwards, N., Hill, David, Lovat, P.E., Plummer, R., Verykiou, S.   +6 more
core   +1 more source

Biology of advanced uveal melanoma and next steps for clinical therapeutics [PDF]

, 2014
Uveal melanoma is the most common intraocular malignancy although it is a rare subset of all melanomas. Uveal melanoma has distinct biology relative to cutaneous melanoma, with widely divergent patient outcomes.
Bastian, BC, Bowcock, AM, Carvajal, RD, Flaherty, KT, Gershenwald, JE, Gutkind, JS, Luke, JJ, McKenna, KC, Patel, PM, Sato, T, Selig, S, Sossman, JA, Streicher, HZ, Sznol, M, Thurin, M, Triozzi, PL, Van Meir, EG, Welch, J   +17 more
core   +1 more source