Clinical development of targeted and immune based anti-cancer therapies

NA Seebacher, AE Stacy, GM Porter… - Journal of Experimental & …, 2019 - Springer
Cancer is currently the second leading cause of death globally and is expected to be
responsible for approximately 9.6 million deaths in 2018. With an unprecedented …

Discovery of cysteine-targeting covalent protein kinase inhibitors

X Lu, JB Smaill, AV Patterson… - Journal of medicinal …, 2021 - ACS Publications
Small molecule covalent kinase inhibitors (CKIs) have entered a new era in drug discovery,
which have the advantage for sustained target inhibition and high selectivity. An increased …

Design, synthesis and anticancer evaluation of thieno [2, 3-d] pyrimidine derivatives as dual EGFR/HER2 inhibitors and apoptosis inducers

SA Elmetwally, KF Saied, IH Eissa, EB Elkaeed - Bioorganic chemistry, 2019 - Elsevier
Deregulation of many kinases is directly linked to cancer development and the tyrosine
kinase family is one of the most important targets in current cancer therapy regimens. In this …

New Benzimidazole-, 1,2,4-Triazole-, and 1,3,5-Triazine-Based Derivatives as Potential EGFRWT and EGFRT790M Inhibitors: Microwave-Assisted Synthesis …

HE Hashem, AEGE Amr, ES Nossier, MM Anwar… - ACS …, 2022 - ACS Publications
A new series of benzimidazole, 1, 2, 4-triazole, and 1, 3, 5-triazine derivatives were
designed and synthesized using a microwave irradiation synthetic approach utilizing 2 …

Quantitative Detection of EGFR Mutations in Circulating Tumor DNA Derived from Lung Adenocarcinomas

K Taniguchi, J Uchida, K Nishino, T Kumagai… - Clinical cancer …, 2011 - AACR
Purpose: Examination of somatic epidermal growth factor receptor (EGFR) mutations is now
a diagnostic routine for treatment of cancer using EGFR tyrosine kinase inhibitors (EGFR …

The oncolytic poxvirus JX-594 selectively replicates in and destroys cancer cells driven by genetic pathways commonly activated in cancers

KA Parato, CJ Breitbach, F Le Boeuf, J Wang… - Molecular Therapy, 2012 - cell.com
Oncolytic viruses are generally designed to be cancer selective on the basis of a single
genetic mutation. JX-594 is a thymidine kinase (TK) gene-inactivated oncolytic vaccinia virus …

Targeting EGFRL858R/T790M and EGFRL858R/T790M/C797S resistance mutations in NSCLC: Current developments in medicinal chemistry

X Lu, L Yu, Z Zhang, X Ren, JB Smaill… - Medicinal research …, 2018 - Wiley Online Library
Both the first‐generation reversible epidermal growth factor receptor (EGFR) inhibitors
gefitinib and erlotinib and the second‐generation covalent epidermal growth factor receptor …

Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments

C Jöst, C Nitsche, T Scholz, L Roux… - Journal of medicinal …, 2014 - ACS Publications
Covalent ligand-target interactions offer significant pharmacological advantages. However,
off-target reactivity of the reactive groups, which usually have electrophilic properties, must …

[HTML][HTML] EGFR-targeted therapy for non-small cell lung cancer: focus on EGFR oncogenic mutation

A Antonicelli, S Cafarotti, A Indini, A Galli… - … journal of medical …, 2013 - ncbi.nlm.nih.gov
The two essential requirements for pathologic specimens in the era of personalized
therapies for non-small cell lung carcinoma (NSCLC) are accurate subtyping as …

[HTML][HTML] Human papillomaviruses and cancer

J Haedicke, T Iftner - Radiotherapy and oncology, 2013 - Elsevier
Human papillomaviruses (HPV) are small oncogenic DNA viruses of which more than 200
types have been identified to date. A small subset of these is etiologically linked to the …