Molecular targeted therapy for anticancer treatment

HY Min, HY Lee - Experimental & molecular medicine, 2022 - nature.com
Since the initial clinical approval in the late 1990s and remarkable anticancer effects for
certain types of cancer, molecular targeted therapy utilizing small molecule agents or …

The role of quantum chemistry in covalent inhibitor design

LM Mihalovits, GG Ferenczy… - International Journal of …, 2022 - Wiley Online Library
The recent ascent of targeted covalent inhibitors (TCI) in drug discovery brings new
opportunities and challenges to quantum chemical reactivity calculations supporting …

Covalent proximity scanning of a distal cysteine to target PI3Kα

C Borsari, E Keles, JA McPhail… - Journal of the …, 2022 - ACS Publications
Covalent protein kinase inhibitors exploit currently noncatalytic cysteines in the adenosine
5′-triphosphate (ATP)-binding site via electrophiles directly appended to a reversible …

A sulfonyl fluoride derivative inhibits EGFRL858R/T790M/C797S by covalent modification of the catalytic lysine

F Ferlenghi, L Scalvini, F Vacondio, R Castelli… - European Journal of …, 2021 - Elsevier
The emergence of the C797S mutation in EGFR is a frequent mechanism of resistance to
osimertinib in the treatment of non-small cell lung cancer (NSCLC). In the present work, we …

The story of EGFR: from signaling pathways to a potent anticancer target

S Ramani, S Samant, SM Manohar - Future Medicinal Chemistry, 2022 - Future Science
EGFR is a member of the ERBB family. It plays a significant role in cellular processes such
as growth, survival and differentiation via the activation of various signaling pathways. EGFR …

Discovery of PLpro and Mpro Inhibitors for SARS-CoV-2

AC Puhl, AS Godoy, GD Noske, AM Nakamura… - ACS …, 2023 - ACS Publications
There are very few small-molecule antivirals for SARS-CoV-2 that are either currently
approved (or emergency authorized) in the US or globally, including remdesivir …

[HTML][HTML] Hype or hope–Can combination therapies with third-generation EGFR-TKIs help overcome acquired resistance and improve outcomes in EGFR-mutant …

F Papini, J Sundaresan, A Leonetti, M Tiseo… - Critical Reviews in …, 2021 - Elsevier
Three generations of epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-
TKIs) have been developed for treating advanced/metastatic non-small cell lung cancer …

Six‐Membered Aromatic Nitrogen Heterocyclic Anti‐Tumor Agents: Synthesis and Applications

J Li, A Gu, XM Nong, S Zhai, ZY Yue… - The Chemical …, 2023 - Wiley Online Library
Cancer stands as a serious malady, posing substantial risks to human well‐being and
survival. This underscores the paramount necessity to explore and investigate novel …

Dacomitinib for advanced non-small cell lung cancer patients harboring major uncommon EGFR alterations: a dual-center, single-arm, ambispective cohort study in …

HS Li, GJ Yang, Y Cai, JL Li, HY Xu, T Zhang… - Frontiers in …, 2022 - frontiersin.org
Objective: Dacomitinib has been approved for non-small-cell lung cancer (NSCLC) patients
harboring classical epidermal growth factor receptor (EGFR) mutations; however, clinical …

Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism

RL Du, N Sun, YH Fung, YY Zheng, YW Chen… - RSC Medicinal …, 2022 - pubs.rsc.org
Inhibition of bacterial cell division is a novel mechanistic action in the development of new
antimicrobial agents. The FtsZ protein is an important antimicrobial drug target because of its …