Abstract 3901: Estrogen receptor conformation sensing small molecules as novel anti-cancer agents

Author(s):  
Bethany Rankin ◽  
Rajendram V. Rajnarayanan ◽  
Marc Koyack
Author(s):  
Lajos Gera ◽  
Daniel C. Chan ◽  
Laimute Taraseviciene-Stewart ◽  
Vitalija Simkeviciene ◽  
Paul A. Bunn ◽  
...  

Medicina ◽  
2019 ◽  
Vol 55 (8) ◽  
pp. 414 ◽  
Author(s):  
Crisci ◽  
Amitrano ◽  
Saggese ◽  
Muto ◽  
Sarno ◽  
...  

The upgraded knowledge of tumor biology and microenviroment provides information on differences in neoplastic and normal cells. Thus, the need to target these differences led to the development of novel molecules (targeted therapy) active against the neoplastic cells’ inner workings. There are several types of targeted agents, including Small Molecules Inhibitors (SMIs), monoclonal antibodies (mAbs), interfering RNA (iRNA) molecules and microRNA. In the clinical practice, these new medicines generate a multilayered step in pharmacokinetics (PK), which encompasses a broad individual PK variability, and unpredictable outcomes according to the pharmacogenetics (PG) profile of the patient (e.g., cytochrome P450 enzyme), and to patient characteristics such as adherence to treatment and environmental factors. This review focuses on the use of targeted agents in-human phase I/II/III clinical trials in cancer-hematology. Thus, it outlines the up-to-date anticancer drugs suitable for targeted therapies and the most recent finding in pharmacogenomics related to drug response. Besides, a summary assessment of the genotyping costs has been discussed. Targeted therapy seems to be an effective and less toxic therapeutic approach in onco-hematology. The identification of individual PG profile should be a new resource for oncologists to make treatment decisions for the patients to minimize the toxicity and or inefficacy of therapy. This could allow the clinicians to evaluate benefits and restrictions, regarding costs and applicability, of the most suitable pharmacological approach for performing a tailor-made therapy.


2010 ◽  
Vol 83 (Suppl_1) ◽  
pp. 293-293
Author(s):  
Susan Nagel ◽  
Joseph Beeman ◽  
Alison Ghormley ◽  
Bridget Niebruegge

2020 ◽  
Vol 56 (34) ◽  
pp. 4672-4675 ◽  
Author(s):  
Alexander R. Nödling ◽  
Emily M. Mills ◽  
Xuefei Li ◽  
Davide Cardella ◽  
Edward J. Sayers ◽  
...  

Conjugation of small molecules to a simple cyanine dye can lead to organelle-specific delivery.


2021 ◽  
Vol 22 (9) ◽  
pp. 4320
Author(s):  
Benjamin Caulier ◽  
Jorrit M. Enserink ◽  
Sébastien Wälchli

Chimeric antigen receptor (CAR) therapy is a promising modality for the treatment of advanced cancers that are otherwise incurable. During the last decade, different centers worldwide have tested the anti-CD19 CAR T cells and shown clinical benefits in the treatment of B cell tumors. However, despite these encouraging results, CAR treatment has also been found to lead to serious side effects and capricious response profiles in patients. In addition, the CD19 CAR success has been difficult to reproduce for other types of malignancy. The appearance of resistant tumor variants, the lack of antigen specificity, and the occurrence of severe adverse effects due to over-stimulation of the therapeutic cells have been identified as the major impediments. This has motivated a growing interest in developing strategies to overcome these hurdles through CAR control. Among them, the combination of small molecules and approved drugs with CAR T cells has been investigated. These have been exploited to induce a synergistic anti-cancer effect but also to control the presence of the CAR T cells or tune the therapeutic activity. In the present review, we discuss opportunistic and rational approaches involving drugs featuring anti-cancer efficacy and CAR-adjustable effect.


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