Molecular Cancer Therapeutics
SCIE-ISI SCOPUS (2001-2025)
1535-7163
1538-8514
Mỹ
Cơ quản chủ quản: American Association for Cancer Research Inc. , AMER ASSOC CANCER RESEARCH
Lĩnh vực:
Cancer ResearchOncology
Các bài báo tiêu biểu
Tumor Mutational Burden as an Independent Predictor of Response to Immunotherapy in Diverse Cancers
Tập 16 Số 11 - Trang 2598-2608 - 2017
Abstract Immunotherapy induces durable responses in a subset of patients with
cancer. High tumor mutational burden (TMB) may be a response biomarker for
PD-1/PD-L1 blockade in tumors such as melanoma and non–small cell lung cancer
(NSCLC). Our aim was to examine the relationship between TMB and outcome in
diverse cancers treated with various immunotherapies. We reviewed data on 1,638
patients who ...
Cabozantinib (XL184), a Novel MET and VEGFR2 Inhibitor, Simultaneously Suppresses Metastasis, Angiogenesis, and Tumor Growth
Tập 10 Số 12 - Trang 2298-2308 - 2011
AbstractThe signaling pathway of the receptor tyrosine kinase MET and its ligand
hepatocyte growth factor (HGF) is important for cell growth, survival, and
motility and is functionally linked to the signaling pathway of VEGF, which is
widely recognized as a key effector in angiogenesis and cancer progression.
Dysregulation of the MET/VEGF axis is found in a number of human malignancies
and has bee...
Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity
Tập 7 Số 7 - Trang 1851-1863 - 2008
Abstract The phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of
rapamycin inhibitor (mTOR) pathway is often constitutively activated in human
tumor cells, providing unique opportunities for anticancer therapeutic
intervention. NVP-BEZ235 is an imidazo[4,5-c]quinoline derivative that inhibits
PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these
enzymes. In cellular s...
Antitumor Activity of the Glutaminase Inhibitor CB-839 in Triple-Negative Breast Cancer
Tập 13 Số 4 - Trang 890-901 - 2014
AbstractGlutamine serves as an important source of energy and building blocks
for many tumor cells. The first step in glutamine utilization is its conversion
to glutamate by the mitochondrial enzyme glutaminase. CB-839 is a potent,
selective, and orally bioavailable inhibitor of both splice variants of
glutaminase (KGA and GAC). CB-839 had antiproliferative activity in a
triple-negative breast can...
MK-2206, an Allosteric Akt Inhibitor, Enhances Antitumor Efficacy by Standard Chemotherapeutic Agents or Molecular Targeted DrugsIn vitroandIn vivo
Tập 9 Số 7 - Trang 1956-1967 - 2010
AbstractThe serine/threonine kinase Akt lies at a critical signaling node
downstream of phosphatidylinositol-3-kinase and is important in promoting cell
survival and inhibiting apoptosis. An Akt inhibitor may be particularly useful
for cancers in which increased Akt signaling is associated with reduced
sensitivity to cytotoxic agents or receptor tyrosine kinase inhibitors. We
evaluated the effect ...
Stereospecific PARP Trapping by BMN 673 and Comparison with Olaparib and Rucaparib
Tập 13 Số 2 - Trang 433-443 - 2014
Abstract Anti-PARP drugs were initially developed as catalytic inhibitors to
block the repair of DNA single-strand breaks. We recently reported that several
PARP inhibitors have an additional cytotoxic mechanism by trapping PARP–DNA
complexes, and that both olaparib and niraparib act as PARP poisons at
pharmacologic concentrations. Therefore, we have proposed that PARP inhibitors
should be evaluat...
Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma
Tập 6 Số 12 - Trang 3314-3322 - 2007
Abstract A t(2;5) chromosomal translocation resulting in expression of an
oncogenic kinase fusion protein known as nucleophosmin-anaplastic lymphoma
kinase (NPM-ALK) has been implicated in the pathogenesis of anaplastic
large-cell lymphoma (ALCL). PF-2341066 was recently identified as a p.o.
bioavailable, small-molecule inhibitor of the catalytic activity of c-Met kinase
and the NPM-ALK fusion pro...
Marine natural products as anticancer drugs
Tập 4 Số 2 - Trang 333-342 - 2005
Abstract The chemical and biological diversity of the marine environment is
immeasurable and therefore is an extraordinary resource for the discovery of new
anticancer drugs. Recent technological and methodologic advances in structure
elucidation, organic synthesis, and biological assay have resulted in the
isolation and clinical evaluation of various novel anticancer agents. These
compounds range...
Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor
Tập 11 Số 2 - Trang 317-328 - 2012
Abstract Following the discovery of NVP-BEZ235, our first dual pan-PI3K/mTOR
clinical compound, we sought to identify additional phosphoinositide 3-kinase
(PI3K) inhibitors from different chemical classes with a different selectivity
profile. The key to achieve these objectives was to couple a structure-based
design approach with intensive pharmacologic evaluation of selected compounds
during the ...
Cơ chế tác động chủ yếu của halichondrin tổng hợp E7389 là ức chế sự phát triển của vi ống Dịch bởi AI
Tập 4 Số 7 - Trang 1086-1095 - 2005
Tóm tắt E7389, hiện đang trong thử nghiệm lâm sàng giai đoạn I và II, là một dẫn
xuất ketone macrocyclic tổng hợp của sản phẩm tự nhiên halichondrin B từ bọt
biển biển. Trong khi cơ chế tác động của nó chưa được làm rõ hoàn toàn, mục tiêu
chính dường như là tubulin và/hoặc các vi ống có trách nhiệm với việc xây dựng
và chức năng đúng đắn của thoi phân bào. Giống như hầu hết các thuốc chống ung
thư...