Targeting both BET and CBP/EP300 proteins with the novel dual inhibitors NEO2734 and NEO1132 leads to anti‐tumor activity in multiple myeloma

KR Ryan, F Giles, GJ Morgan - European Journal of …, 2021 - Wiley Online Library
Objectives Two promising epigenetic therapeutic targets have emerged for the treatment of
hematologic malignancies, BET and CBP/EP300 proteins. Several studies have shown that …

Development of REDX05358, a novel highly selective and potent pan RAF inhibitor and a potential therapeutic for BRAF and RAS mutant tumors

H Mason, S Scrace, R Testar, J Rainard, F Talab… - Cancer Research, 2017 - AACR
REDX05358 has been identified as a novel, highly selective and potent next generation pan
RAF inhibitor with improved therapeutic potential and predicted safety profile. Aberrant …

Synergistic activity of carfilzomib and panobinostat in multiple myeloma cells via modulation of ROS generation and ERK1/2

L Gao, M Gao, G Yang, Y Tao, Y Kong… - BioMed Research …, 2015 - Wiley Online Library
Relapse of disease and subsequent resistance to established therapies remain as major
challenges in the treatment of multiple myeloma (MM). New therapeutic options are needed …

Antitumor properties of RAF709, a highly selective and potent inhibitor of RAF kinase dimers, in tumors driven by mutant RAS or BRAF

W Shao, YM Mishina, Y Feng, G Caponigro, VG Cooke… - Cancer research, 2018 - AACR
Resistance to the RAF inhibitor vemurafenib arises commonly in melanomas driven by the
activated BRAF oncogene. Here, we report antitumor properties of RAF709, a novel ATP …

A first-in-human dose phase 1 study of LY3009120 in advanced cancer patients.

DS Hong, A Hollebecque, MS Gordon, KT Flaherty… - 2017 - ascopubs.org
2507 Background: LY3009120, a pan-Raf and dimer inhibitor, demonstrates inhibition of
phospho-Mek/Erk and tumor growth inhibition in several non-clinical cancer models with …

First-in-human, multicenter, dose-escalation, phase I study of the investigational drug TAK-733, an oral MEK inhibitor, in patients (pts) with advanced nonhematologic …

JA Sosman, AA Adjei, P LoRusso… - Journal of Clinical …, 2011 - ascopubs.org
TPS145 Background: The Ras/Raf/MEK/ERK cascade is frequently activated in human
cancers; MEK inhibition is an attractive therapeutic target for preventing tumor growth and …

Is B-Raf a good therapeutic target for melanoma and other malignancies?

SRV Madhunapantula, GP Robertson - Cancer research, 2008 - AACR
The RAF family members, A-Raf, B-Raf, and C-Raf (or Raf-1), are intermediate molecules in
the mitogen-activated protein (MAP) kinase [Ras/Raf/MAP kinase/extracellular signal …

A Phase 1 first-in-human trial to evaluate the safety and tolerability of CCT3833, an oral panRAF inhibitor, in patients with advanced solid tumours, including metastatic …

EJ Dean, U Banerji, R Girotti, I Niculescu-Duvaz… - 2016 - ascopubs.org
TPS9597 Background: Over 70,000 patients are diagnosed with malignant melanoma in the
USA every year with a high proportion occurring in young people. Although treatments …

[HTML][HTML] PF-04691502, a dual PI3K/mTOR inhibitor has potent pre-clinical activity by inducing apoptosis and G1 cell cycle arrest in aggressive B-cell non-Hodgkin …

D Chen, C Mao, Y Zhou, Y Su… - … Journal of Oncology, 2015 - spandidos-publications.com
The PI3K/Akt/mTOR pathway is activated in a variety of human tumors including B-cell non-
Hodgkin lymphoma (B-NHL). Targeting this pathway has been validated in solid and …

[HTML][HTML] Enhanced levels of apoptosis by combination of farnesyl transferase inhibition (tipifarnib) and proteasome inhibition (bortezomib) in myeloma cell lines and …

JL Kaufman, E David, C Torre, R Sinha, S Lonial - Blood, 2005 - Elsevier
Introduction: Despite significant advances in the treatment of myeloma, patients invariably
become resistant to therapy. Therefore, novel treatment strategies are needed to overcome …