First Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Potent and Orally Active Antitumor Agents. 2. Lead Discovery†

2009 ◽  
Vol 52 (2) ◽  
pp. 293-307 ◽  
Author(s):  
Maria Menichincheri ◽  
Alberto Bargiotti ◽  
Jens Berthelsen ◽  
Jay A. Bertrand ◽  
Roberto Bossi ◽  
...  
Keyword(s):  
Kinase Inhibitors ◽  
Antitumor Agents ◽  
Lead Discovery ◽  
Cdc7 Kinase ◽  
Orally Active

scholarly journals First Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Potent and Orally Active Antitumor Agents. 2. Lead Discovery

2009 ◽  
Vol 52 (4) ◽  
pp. 1230-1230
Author(s):  
Maria Menichincheri ◽  
Alberto Bargiotti ◽  
Jens Berthelsen ◽  
Jay A. Bertrand ◽  
Roberto Bossi ◽  
...  
Keyword(s):  
Kinase Inhibitors ◽  
Antitumor Agents ◽  
Lead Discovery ◽  
Cdc7 Kinase ◽  
Orally Active

Cdc7 Kinase Inhibitors: 5-Heteroaryl-3-Carboxamido-2-Aryl Pyrroles as Potential Antitumor Agents. 1. Lead Finding

2010 ◽  
Vol 53 (20) ◽  
pp. 7296-7315 ◽  
Author(s):  
Maria Menichincheri ◽  
Clara Albanese ◽  
Cristina Alli ◽  
Dario Ballinari ◽  
Alberto Bargiotti ◽  
...  
Keyword(s):  
Kinase Inhibitors ◽  
Antitumor Agents ◽  
Cdc7 Kinase ◽  
Lead Finding ◽  
Potential Antitumor

Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Potential Antitumor Agents. 1. Synthesis and Structure–Activity Relationships

2008 ◽  
Vol 51 (3) ◽  
pp. 487-501 ◽  
Author(s):  
Ermes Vanotti ◽  
Raffaella Amici ◽  
Alberto Bargiotti ◽  
Jens Berthelsen ◽  
Roberta Bosotti ◽  
...  
Keyword(s):  
Kinase Inhibitors ◽  
Antitumor Agents ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Cdc7 Kinase ◽  
Potential Antitumor

scholarly journals Design, Synthesis, and Biological Activity of Sulfonamide Analogues of Antofine and Cryptopleurine as Potent and Orally Active Antitumor Agents

2015 ◽  
Vol 58 (19) ◽  
pp. 7749-7762 ◽  
Author(s):  
Yongseok Kwon ◽  
Jayoung Song ◽  
Honggu Lee ◽  
Eun-Yeong Kim ◽  
Kiho Lee ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Design Synthesis ◽  
Orally Active

Aminopyrimidinone Cdc7 Kinase Inhibitors

2012 ◽  
Vol 22 (5) ◽  
pp. 1940-1943 ◽  
Author(s):  
Keith W. Woods ◽  
Chunqiu Lai ◽  
Julie M. Miyashiro ◽  
Yunsong Tong ◽  
Alan S. Florjancic ◽  
...  
Keyword(s):  
Kinase Inhibitors ◽  
Cdc7 Kinase

Targeting HER2 Alterations in Non–Small-Cell Lung Cancer: A Comprehensive Review

2020 ◽  
pp. 411-425 ◽  
Author(s):  
Jing Zhao ◽  
Yang Xia
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
Kinase Inhibitors ◽  
Antitumor Agents ◽  
De Novo ◽  
Point Mutations ◽  
Small Cell ◽  
Small Cell Lung ◽  
Exon 20

PURPOSE HER2 is a critical gene that drives various solid tumors in addition to those of breast cancer. For example, HER2 plays a role in non–small-cell lung cancer (NSCLC). Overexpression, amplification, and point mutations in HER2 have been described in patients with NSCLC; however, the potential roles of these alterations remain unclear. METHODS We summarize the evidence regarding the distinct impacts of different HER2 aberrations on antitumor agents. Also, we update the therapeutic efficacy of HER2-targeted agents, including anti-HER2 antibodies, antibody-drug conjugates, and small-molecule tyrosine kinase inhibitors, tested in HER2-aberrant NSCLC. RESULTS Although these drugs are not yet standard treatments, certain patients may benefit from these therapies. In this review, we aim to provide an improved understanding of HER2 aberrations in NSCLC, including NSCLC biology and the impacts of each aberration on prognosis and standard treatment. We also highlight the potential of novel anti-HER2 therapies approved by regulatory bodies and those in clinical development. CONCLUSION Compared with HER2 amplification or overexpression, HER2 mutations, especially HER2 exon 20 mutations, are emerging as the most clear targetable driver for HER2-directed therapies in lung cancer. De novo and inducible HER2 pathway activation need to be differentially managed. Further investigations with new strategies are needed.

Hepatotoxicity of chemotherapeutic agents: current state of the problem

2016 ◽  
Vol 21 (6) ◽  
pp. 325-333
Author(s):  
M. T Vatutin ◽  
E. V Sklyannaya ◽  
Mariam A. El-Khatib ◽  
S. V Starchenko ◽  
M. V Makarova
Keyword(s):  
Kinase Inhibitors ◽  
Antitumor Agents ◽  
Opportunistic Infections ◽  
Alkylating Agents ◽  
Chemotherapeutic Agents ◽  
Protein Kinase Inhibitors ◽  
Drug Induced ◽  
Anthracycline Antibiotics ◽  
Current State ◽  
High Level

This review is devoted to the actual for the present day problem of the hepatotoxicity of chemotherapeutic agents. Liver is the most important organ essential for the maintaining of the body’s internal environment. For the present time there is observed the high level of the morbidity and mortality rate against the background of drug-induced liver lesions due to, in the first instance, the lack ofproper manner for the substitution of the liver function but transplantation. Liver deteriorations due to the administration of antitumor agents have no pathognomonic clinical or histological features that significantly embarrasses the execution of the differential diagnosis with liver disorders against the background of administration of other preparations, either associated with opportunistic infections or the progression of previously acquired pathology of the liver. In the article there is described the toxic influence on the liver of most often used in oncology chemotherapeutic agents - antimetabolites, alkylating agents, platinum compounds, epothilones, taxanes, vinca alkaloids, monoclonal antibodies, anthracycline antibiotics, topoisomerase and protein kinase inhibitors is described in this article. In the review there are summarized results of recent studies of etiology, pathogenesis, clinical features, diagnosis, prevention and treatment of chemotherapy induced hepatotoxicity. The special attention is given to recent discoveries in the area of pathogenesis of chemotherapy induced hepatotoxicity. However many moments remain to be still not studied completely, that offers perspectives for further research in this field.

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