Publications by authors named "R Roskoski"

Breast cancer is the most commonly diagnosed malignancy and the fifth leading cause of cancer deaths worldwide. Surgery and radiation therapy are localized therapies for early-stage and metastatic breast cancer. The management of breast cancer is determined in large part by the HER2 (human epidermal growth factor receptor 2), HR (hormone receptor), ER (estrogen receptor), and PR (progesterone receptor) status.

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  • * Stage I/II NSCLC is typically treated with surgery, while other treatments like chemoradiotherapy, immune checkpoint inhibitors, and specific targeted therapies are available for various mutations present in NSCLC cases.
  • * SCLC, representing about 15% of lung cancer, has a poor prognosis; treatment for extensive-stage SCLC involves a combination of platinum-based chemotherapy and anti-PDL1 inhibitors.
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Kidney cancers comprise about 3% of all new malignancies in the United States. Renal cell carcinomas (RCCs) are the most common type of renal malignancy making up about 85% of kidney cancer cases. Signs and symptoms of renal cell carcinomas can result from local tumor growth, paraneoplastic syndromes, or distant metastases.

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  • Protein kinases are crucial drug targets for various diseases, particularly cancers, with 80 FDA-approved drugs that focus on them, including seven approved in 2023.
  • Among these drugs, a significant portion treats neoplasms, while others are aimed at inflammatory diseases, showcasing their versatility in treating multiple conditions.
  • The review highlights the key physicochemical properties of these 80 small molecule protein kinase inhibitors, covering aspects like potency, solubility, and ligand efficiency to aid in understanding their effectiveness.
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Because genetic alterations including mutations, overexpression, translocations, and dysregulation of protein kinases are involved in the pathogenesis of many illnesses, this enzyme family is the target of many drug discovery programs worldwide. The FDA has approved 80 small molecule protein kinase inhibitors with 77 drugs orally bioavailable. The data indicate that 69 of these medicinals are approved for the management of neoplasms including solid tumors such as breast and lung cancer as well as non-solid tumors such as leukemia.

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