Covalent vs. Non‐Covalent Inhibition: Tackling Drug Resistance in EGFR–A Thorough Dynamic Perspective
FB Akher, A Farrokhzadeh… - Chemistry & …, 2019 - Wiley Online Library
A persistent challenge in the treatment of non‐small cell lung cancer (NSCLC) with EGFR is
the emergence of drug‐resistant caused by somatic mutations. The EGFR L858R/T790 M …
the emergence of drug‐resistant caused by somatic mutations. The EGFR L858R/T790 M …
[HTML][HTML] Therapeutic strategies of targeting non-apoptotic regulated cell death (RCD) with small-molecule compounds in cancer
X Jin, W Jin, L Tong, N Lin, L Zhang, J Zhao - Acta Pharmaceutica Sinica B, 2024 - Elsevier
Regulated cell death (RCD) is a controlled form of cell death orchestrated by one or more
cascading signaling pathways, making it amenable to pharmacological intervention. RCD …
cascading signaling pathways, making it amenable to pharmacological intervention. RCD …
[HTML][HTML] Targeted Synthesis and Analysis of Biologically Active Azomethine Derivatives of 2-amino-4, 5, 6, 7-tetrahydro-1-benzothiophene-3-carboxamide
AS Chiriapkin, IP Kodonidi… - Drug development & …, 2021 - pharmjournal.ru
Introduction. Azomethine derivatives of 2-amino-4, 5, 6, 7-tetrahydro-1-benzothiophene-3-
carboxamide are acyclic precursors of biologically active compounds derived from 5, 6, 7, 8 …
carboxamide are acyclic precursors of biologically active compounds derived from 5, 6, 7, 8 …
[HTML][HTML] 靶向beclin-1 小分子激动剂诱导三阴性乳腺癌细胞自噬性死亡和凋亡
赵荣演， 靳文珂， 姜星， 袁兆鑫， 刘博， 符雷蕾 - 药学学报, 2021 - html.rhhz.net
细胞自噬(autophagy) 是一种溶酶体降解途径, 在细胞内环境稳态, 细胞发育, 细胞免疫,
抑制肿瘤, 能量代谢, 预防神经退行性变和延长寿命方面起着至关重要的作用 …
抑制肿瘤, 能量代谢, 预防神经退行性变和延长寿命方面起着至关重要的作用 …
BRDT inhibitors for male contraceptive drug discovery: current status
As epigenetic readers, the bromodomain and extra-terminal domain (BET) protein family
binds to acetyl-lysine (KAc) residues and regulates chromatin structure and gene …
binds to acetyl-lysine (KAc) residues and regulates chromatin structure and gene …
Novel insights into epigenetic control of autophagy in cancer
The autophagy mechanism recycles the damaged and long-standing macromolecular
substrates and thus maintains cellular homeostatic and proteostatic conditions. Autophagy …
substrates and thus maintains cellular homeostatic and proteostatic conditions. Autophagy …
Design, synthesis and biological evaluation of novel pteridinone derivatives as potent dual inhibitors of PLK1 and BRD4
Y Qi, L Xu, Z Li, P Gong, T Hu, B Yin, M Qin… - New Journal of …, 2020 - pubs.rsc.org
To develop novel simultaneous inhibition of PLK1 and BRD4 bromodomain by a single
molecule, three series of novel pteridinone derivatives were designed, synthesized and …
molecule, three series of novel pteridinone derivatives were designed, synthesized and …
Applied Biophysics for Bromodomain Drug Discovery
WCK Pomerantz, JA Johnson, PD Ycas - Chemical Epigenetics, 2020 - Springer
The dynamic regulation of epigenetic processes is dictated by the addition, removal, and
recognition of posttranslational modifications on proteins and nucleic acids. These …
recognition of posttranslational modifications on proteins and nucleic acids. These …
Epigenetics in the Diagnosis, Prognosis, and Therapy of Cancer
L Fu, B Liu - Cancer Epigenetics, 2023 - Springer
As cancer is the leading cause of death worldwide, there is an urgent necessity to discover
novel diagnostic and prognostic biomarkers as well as therapeutic targets for this dreadful …
novel diagnostic and prognostic biomarkers as well as therapeutic targets for this dreadful …
Pharmacological regulation and functional significance of chromatin binding by BET tandem bromodomains
9.1. 1 H istone Acetylation and Transcription histoneswerethefirstacetylatedproteinsdisco…
16 andhistoneacetylationisgenerallyassociate…. 17, 18 Thiscorrelationwasfirstattributedtotheability …
16 andhistoneacetylationisgenerallyassociate…. 17, 18 Thiscorrelationwasfirstattributedtotheability …