Small molecules, big impact: 20 years of targeted therapy in oncology
The identification of molecular targets and the growing knowledge of their cellular functions
have led to the development of small molecule inhibitors as a major therapeutic class for …
have led to the development of small molecule inhibitors as a major therapeutic class for …
Lineage plasticity in cancer: a shared pathway of therapeutic resistance
Lineage plasticity, the ability of cells to transition from one committed developmental
pathway to another, has been proposed as a source of intratumoural heterogeneity and of …
pathway to another, has been proposed as a source of intratumoural heterogeneity and of …
Rapid non-uniform adaptation to conformation-specific KRAS (G12C) inhibition
JY Xue, Y Zhao, J Aronowitz, TT Mai, A Vides, B Qeriqi… - Nature, 2020 - nature.com
KRAS GTPases are activated in one-third of cancers, and KRAS (G12C) is one of the most
common activating alterations in lung adenocarcinoma,. KRAS (G12C) inhibitors, are in …
common activating alterations in lung adenocarcinoma,. KRAS (G12C) inhibitors, are in …
Clinical and biological features of neuroendocrine prostate cancer
Y Yamada, H Beltran - Current oncology reports, 2021 - Springer
Abstract Purpose of Review Neuroendocrine prostate cancer (NEPC) is an aggressive
histologic subtype of prostate cancer that most commonly arises in later stages of prostate …
histologic subtype of prostate cancer that most commonly arises in later stages of prostate …
Mechanisms of sensitivity and resistance to CDK4/6 inhibition
M Álvarez-Fernández, M Malumbres - Cancer cell, 2020 - cell.com
Inhibiting the cell-cycle kinases CDK4 and CDK6 results in significant therapeutic effect in
patients with advanced hormone-positive breast cancer. The efficacy of this strategy is …
patients with advanced hormone-positive breast cancer. The efficacy of this strategy is …
Binary pan-cancer classes with distinct vulnerabilities defined by pro-or anti-cancer YAP/TEAD activity
JD Pearson, K Huang, M Pacal, SR McCurdy, S Lu… - Cancer Cell, 2021 - cell.com
Cancer heterogeneity impacts therapeutic response, driving efforts to discover over-arching
rules that supersede variability. Here, we define pan-cancer binary classes based on distinct …
rules that supersede variability. Here, we define pan-cancer binary classes based on distinct …
The genomic landscape of intrinsic and acquired resistance to cyclin-dependent kinase 4/6 inhibitors in patients with hormone receptor–positive metastatic breast …
SA Wander, O Cohen, X Gong, GN Johnson… - Cancer discovery, 2020 - AACR
Mechanisms driving resistance to cyclin-dependent kinase 4/6 inhibitors (CDK4/6i) in
hormone receptor–positive (HR+) breast cancer have not been clearly defined. Whole …
hormone receptor–positive (HR+) breast cancer have not been clearly defined. Whole …
The CDK4/6 inhibitor revolution—A game-changing era for breast cancer treatment
L Morrison, S Loibl, NC Turner - Nature Reviews Clinical Oncology, 2024 - nature.com
Abstract Cyclin-dependent kinase (CDK) 4/6 inhibition in combination with endocrine
therapy is the standard-of-care treatment for patients with advanced-stage hormone receptor …
therapy is the standard-of-care treatment for patients with advanced-stage hormone receptor …
Synthetic lethality in cancer therapeutics: the next generation
Synthetic lethality (SL) provides a conceptual framework for tackling targets that are not
classically “druggable,” including loss-of-function mutations in tumor suppressor genes …
classically “druggable,” including loss-of-function mutations in tumor suppressor genes …
CDK/cyclin dependencies define extreme cancer cell-cycle heterogeneity and collateral vulnerabilities
ES Knudsen, V Kumarasamy, R Nambiar, JD Pearson… - Cell reports, 2022 - cell.com
Progression through G1/S phase of the cell cycle is coordinated by cyclin-dependent kinase
(CDK) activities. Here, we find that the requirement for different CDK activities and cyclins in …
(CDK) activities. Here, we find that the requirement for different CDK activities and cyclins in …