[HTML][HTML] Small molecules in targeted cancer therapy: advances, challenges, and future perspectives

L Zhong, Y Li, L Xiong, W Wang, M Wu… - Signal transduction and …, 2021 - nature.com
Due to the advantages in efficacy and safety compared with traditional chemotherapy drugs,
targeted therapeutic drugs have become mainstream cancer treatments. Since the first …

Small molecule kinase inhibitor drugs (1995–2021): medical indication, pharmacology, and synthesis

CC Ayala-Aguilera, T Valero… - Journal of Medicinal …, 2021 - ACS Publications
The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …

Long-term outcomes with frontline nilotinib versus imatinib in newly diagnosed chronic myeloid leukemia in chronic phase: ENESTnd 10-year analysis

HM Kantarjian, TP Hughes, RA Larson, DW Kim… - Leukemia, 2021 - nature.com
In the ENESTnd study, with≥ 10 years follow-up in patients with newly diagnosed chronic
myeloid leukemia (CML) in chronic phase, nilotinib demonstrated higher cumulative …

Response and resistance to BCR-ABL1-targeted therapies

TP Braun, CA Eide, BJ Druker - Cancer cell, 2020 - cell.com
Chronic myeloid leukemia (CML), caused by constitutively active BCR-ABL1 fusion tyrosine
kinase, has served as a paradigm for successful application of molecularly targeted cancer …

Conformational states dynamically populated by a kinase determine its function

T Xie, T Saleh, P Rossi, CG Kalodimos - Science, 2020 - science.org
INTRODUCTION Protein kinases mediate many cell signaling processes. Central to their
physiological function is the regulation of their binding and enzymatic activities, which is …

Next generation of fluorine-containing pharmaceuticals, compounds currently in phase II–III clinical trials of major pharmaceutical companies: new structural trends …

Y Zhou, J Wang, Z Gu, S Wang, W Zhu… - Chemical …, 2016 - ACS Publications
Fluoroorganic chemistry has become essential in the evolution of many different but
interconnected research fields. These include the development of new materials with a …

The leukaemia stem cell: similarities, differences and clinical prospects in CML and AML

D Vetrie, GV Helgason, M Copland - Nature Reviews Cancer, 2020 - nature.com
For two decades, leukaemia stem cells (LSCs) in chronic myeloid leukaemia (CML) and
acute myeloid leukaemia (AML) have been advanced paradigms for the cancer stem cell …

Chronic myeloid leukemia: 2018 update on diagnosis, therapy and monitoring

E Jabbour, H Kantarjian - American journal of hematology, 2018 - Wiley Online Library
Disease overview Chronic myeloid leukemia (CML) is a myeloproliferative neoplasm with an
incidence of 1‐2 cases per 100 000 adults. It accounts for approximately 15% of newly …

Kinase-targeted cancer therapies: progress, challenges and future directions

KS Bhullar, NO Lagarón, EM McGowan, I Parmar… - Molecular cancer, 2018 - Springer
The human genome encodes 538 protein kinases that transfer a γ-phosphate group from
ATP to serine, threonine, or tyrosine residues. Many of these kinases are associated with …

Discovery of COVID-19 inhibitors targeting the SARS-CoV-2 Nsp13 helicase

MA White, W Lin, X Cheng - The journal of physical chemistry …, 2020 - ACS Publications
The raging COVID-19 pandemic caused by SARS-CoV-2 has infected tens of millions of
people and killed several hundred thousand patients worldwide. Currently, there are no …