HuR-targeted agents: an insight into medicinal chemistry, biophysical, computational studies and pharmacological effects on cancer models

2021 ◽  
pp. 114088
Author(s):  
Giulia Assoni ◽  
Valeria La Pietra ◽  
Rosangela Digilio ◽  
Caterina Ciani ◽  
Nausicaa Valentina Licata ◽  
...  
Keyword(s):  
Medicinal Chemistry ◽  
Computational Studies ◽  
Pharmacological Effects ◽  
Targeted Agents ◽  
Cancer Models ◽  
Insight Into

Ultrastructure of neuromuscular relationships in the canine heartworm (dirofilaria immitis)

1986 ◽  
Vol 44 ◽  
pp. 278-279
Author(s):  
W. L. Steffens ◽  
Nancy B. Roberts ◽  
J. M. Bowen
Keyword(s):  
Dirofilaria Immitis ◽  
Domestic Dogs ◽  
Structural Description ◽  
Pharmacological Effects ◽  
Free Living ◽  
Canine Heartworm ◽  
The World ◽  
Synaptic Region ◽  
Muscle Innervation ◽  
Insight Into

The canine heartworm is a common and serious nematode parasite of domestic dogs in many parts of the world. Although nematode neuroanatomy is fairly well documented, the emphasis has been on sensory anatomy and primarily in free-living soil species and ascarids. Lee and Miller reported on the muscular anatomy in the heartworm, but provided little insight into the peripheral nervous system or myoneural relationships. The classical fine-structural description of nematode muscle innervation is Rosenbluth's earlier work in Ascaris. Since the pharmacological effects of some nematacides currently being developed are neuromuscular in nature, a better understanding of heartworm myoneural anatomy, particularly in reference to the synaptic region is warranted.

Insight into the Medicinal Chemistry of EGFR and HER-2 Inhibitors

2014 ◽  
Vol 21 (11) ◽  
pp. 1336-1350 ◽  
Author(s):  
C. Wang ◽  
H. Gao ◽  
J. Dong ◽  
F. Wang ◽  
P. Li ◽  
...  
Keyword(s):  
Medicinal Chemistry ◽  
Her 2 ◽  
Insight Into

Molecular targeted therapy: novel therapeutic approach for head and neck cancer

2020 ◽  
Vol 11 (10) ◽  
pp. 637-651 ◽  
Author(s):  
Swatantra Shrivastava ◽  
Ravleen Nagi ◽  
Saurabh Sharma ◽  
Sajid Ahmed Rasul Sanadi ◽  
Elbadri Taha Dafallah ◽  
...  
Keyword(s):  
Head And Neck ◽  
Head And Neck Cancers ◽  
Targeted Agents ◽  
Tumor Resistance ◽  
Therapeutic Approaches ◽  
Public Health Burden ◽  
Host Immune Responses ◽  
Alternative Treatment Option ◽  
Tumor Specificity ◽  
Insight Into

Cancer is a major public health burden worldwide, affecting millions of people each year. One of the major hallmarks of cancer is rapid growth and progression by evasion of host immune responses. Tumor resistance to conventional anticancer drugs by several mechanisms, such as drug inactivation, efflux pumps and enhanced toxicity to normal cells decreases their clinical efficacy. These limitations resulted in the development of new targeted agents, such as monoclonal antibodies and small molecule inhibitors that have high tumor specificity. This paper discusses the therapeutic applications of novel molecular targeted agents and immunotherapy as an alternative treatment option for head and neck cancers, as well as provides insight into future therapeutic approaches for advanced head and neck cancers.

scholarly journals ATRAID regulates the action of nitrogen-containing bisphosphonates on bone

2020 ◽  
Vol 12 (544) ◽  
pp. eaav9166 ◽  
Author(s):  
Lauren E. Surface ◽  
Damon T. Burrow ◽  
Jinmei Li ◽  
Jiwoong Park ◽  
Sandeep Kumar ◽  
...  
Keyword(s):  
Osteonecrosis Of The Jaw ◽  
Pharmacological Effects ◽  
Protein Prenylation ◽  
Genome Wide ◽  
Cellular Factors ◽  
Osteoclast Function ◽  
Differential Responsiveness ◽  
Coding Variants ◽  
Deficient Mice ◽  
Insight Into

Nitrogen-containing bisphosphonates (N-BPs), such as alendronate, are the most widely prescribed medications for diseases involving bone, with nearly 200 million prescriptions written annually. Recently, widespread use of N-BPs has been challenged due to the risk of rare but traumatic side effects such as atypical femoral fracture (AFF) and osteonecrosis of the jaw (ONJ). N-BPs bind to and inhibit farnesyl diphosphate synthase, resulting in defects in protein prenylation. Yet, it remains poorly understood what other cellular factors might allow N-BPs to exert their pharmacological effects. Here, we performed genome-wide studies in cells and patients to identify the poorly characterized gene, ATRAID. Loss of ATRAID function results in selective resistance to N-BP–mediated loss of cell viability and the prevention of alendronate-mediated inhibition of prenylation. ATRAID is required for alendronate inhibition of osteoclast function, and ATRAID-deficient mice have impaired therapeutic responses to alendronate in both postmenopausal and senile (old age) osteoporosis models. Last, we performed exome sequencing on patients taking N-BPs that suffered ONJ or an AFF. ATRAID is one of three genes that contain rare nonsynonymous coding variants in patients with ONJ or an AFF that is also differentially expressed in poor outcome groups of patients treated with N-BPs. We functionally validated this patient variation in ATRAID as conferring cellular hypersensitivity to N-BPs. Our work adds key insight into the mechanistic action of N-BPs and the processes that might underlie differential responsiveness to N-BPs in people.

Abstract A194: OTX008, a small molecule that inhibits galectin-1, potentiates the in vitro effects of cytotoxic and targeted agents in several human cancer models.

2013 ◽  
Author(s):  
Lucile Astorgues-xerri ◽  
Maria Eugenia Riveiro ◽  
Kay Noel ◽  
Esteban Cvitkovic ◽  
Mohamed Bekradda ◽  
...  
Keyword(s):  
Small Molecule ◽  
Human Cancer ◽  
Targeted Agents ◽  
Cancer Models ◽  
In Vitro Effects

Classical Cancer Biology: Misconceptions and Limitations

2017 ◽  
Author(s):  
Abicumaran Uthamacumaran
Keyword(s):  
Cancer Cells ◽  
Cancer Biology ◽  
Expression Profiles ◽  
Gene Expression Profiles ◽  
Transformed Cells ◽  
Epigenetic Landscape ◽  
Normal Cells ◽  
Cancer Models ◽  
Stem Cell Division ◽  
Insight Into

Cancer is the co-evolution of cancer cells and their turbulent microenvironment, characterized by dynamical hyper-chaotic gene expression profiles. However, cancers should not be viewed as the result of random mutations and malfunctioning information processing systems. Rather, it is the selective advantages conferred by adaptive evolution of cellular biosystems. Although on a systemic scale, cancer is defined as a disease, on a cellular basis they outperform healthy (non-transformed cells) in terms of survival and reproductive success. Their enhanced longevity pathways, metastatic invasion, extended telomeres, dynamical morphogenesis, regenerative stem cell division and environment-specific metabolic cascades indicate they are adaptive evolutionary cell states that have surpassed the boundaries normal cells are confined to. Therefore, the paper presents a brief summary of currently existing classical cancer models in the field of mathematical biology and the misconceptions of cancer epimetabolomes to further advance cancer research beyond its current limits. Through an insight into the mathematical behaviors of cancer cells, a quantum adaptive epigenetic landscape is proposed to explain the selective evolutionary dominance of cancer cells.

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