ANTICANCER

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ANTICANCER

ANTICANCER DRUG DEFINITION

Antineoplastics or Anticancer drugs are the drugs that prevent or inhibit the maturation and proliferation of neoplasms. 
Antineoplastic agents travel the body and destroy cancer cells. Many of the side effects associated with antineoplastic agents occur because treatment destroys the body's normal cells in addition to cancerous cells.

General Toxicities of Antineoplastic / Anticancer Drugs are:
Bone marrow depression
Lymphocytopenia
GIT Stomatitis
Diarrhoea
Nausea and Vomiting
Alopecia
Hyperuricaemia
Hair loss
Antineoplastic drugs / Anticancer Drugs are not only used prominently in different types of cancers but also in conjunction with surgery, radiotherapy and immunotherapy in the combined modality approach for many solid tumors, especially metastatic. 

Where are the anticancer drug binding sites in MRP1 protein? In order to define anticancer drug binding sites, we have made couple cysless MRP1 constructs (mutated all 25 cysteine residues to alanines), either full length or N-proximal half plus C-proximal half, and expressed in sf21 cells. We also made antibodies against MRP1 N-half or C-half. The cysless MRP1 protein is partially functional (to transport its substrate). Cysteine residues were introduced into the cysless MRP1 protein at the desired sites and will be utilized to screen anticancer drug binding sites by labeling with 14C-labeled N-ethylmaleimide.

How does the MRP1 protein couple ATP binding/hydrolysis to anticancer drug transport? Several papers have been published, regarding the ATP binding/hydrolysis at those two non-equivalent nucleotide binding domains and conformational changes of the MRP1 protein induced by the ATP binding/hydrolysis. The effects of drug binding on the ATP binding/hydrolysis were also studied. A lot of mutations affecting ATP binding or hydrolysis have been made and used to study the mechanism of ATP-dependent anticancer drug transport. This kind of research is still ongoing.

Of the 1.4 million Americans diagnosed with cancer this year, roughly 600,000 will die of this group of diseases. If current chemotherapy or immunotherapy were effective, these patients would be cured of their neoplasms. Our laboratory is attempting to gain insight into the limited efficacy of current therapies by investigating the biochemical basis for killing by effective chemotherapeutic agents and cytotoxic lymphocytes as well as the mechanisms by neoplastic cells evade this killing.

Apoptosis (programmed cell death) is a distinct form of cell death that occurs under a variety of physiological and pathological conditions. Building on earlier observations that a variety of chemotherapeutic agents induce apoptosis in susceptible cell types, members of my laboratory are investigating how the signaling by various components of apoptotic pathways is affected by changes in phosphorylation and other posttranslational modifications. At the same time, other members of my laboratory are using topoisomerase I poisons, which are used to treat a number of common cancers, as prototypic drugs to investigate changes further upstream that determine whether anticancer drugs are able to interact with their targets and trigger the signaling required to activate the cell death process. Finally, in conjunction with other members of the Developmental Therapeutics Program of the Mayo Clinic Cancer Center, we are examining the cytotoxic action of a number of novel anticancer agents in preclinical model systems and, in some cases, in the context of phase I and phase II clinical trials.

Classification of Antineoplastic Agents / Anticancer Drugs 2

  1. Alkylating Agents
    • Nitrogen mustards: Melphalan, Cyclophosphamide, Ifosfamide
    • Nitrosoureas
    • Alkylsulfonates
    • Ethyleneimines
    • Triazene
    • Methyl Hydrazines
    • Platinum Coordination complexes: Cisplatin, Carboplatin, Oxaliplatin
  2. Antimetabolites
    • Folate Antagonists: Methotrexate
    • Purine antagonists
    • Pyrimidine antagonists: 5-Fluorouracil, Cytarabibe
  3. Natural Products
    1. Plant Products
      • Vinca Alkaloids: Vincristine, Vinblastine
      • Taxanes: Paclitaxel, Docetaxel
      • Epipodophyllotoxins: Etoposide
      • Camptothecins: Irinotecan
    2. Microorganism Products
      • Antibiotics: Doxorubicin, Bleomycin
      • Enzymes: L-Asparaginase
  4. Miscellaneous
    • Hydroxyurea
    • Imatinib Mesylate
    • Rituximab
    • Epirubicin
    • Bortezomib
    • Zoledronic Acid
    • Geftinib
    • Leucovorin
    • Pamidronate
    • Gemcitabine
  5. Hormones and Antagonists
    • Corticosteroids: Prednisone, Dexamethasone
    • Estrogens: Ethinyloestradiol
    • Antiestrogens: Tamoxifen
    • Progesteron derivative: Megestrol Acetate
    • Androgen: Testosterone propionate
    • Antiandrogen: Flutamide , Bicalutamide
    • Aromatase inhibitor: Letrozole , Anastrazole
    • 5-alpha reductase inhibitor: Finasteride
    • GnRH Analogue: Leuprolide, Buserelin
    • Growth Hormone, glucagon and insulin inhibitor: Octreotide