The Effects of Two Alkaloids Derived from Vinca rosea on the Malignant Cells of Hodgkin’s Disease, Lymphosarcoma and Acute Leukemia in Vivo Alberto M. Marmont and Eugenio E. Damasio 1 Studies of Lymphocyte Kinetics in Man Seymour Perry, George L. Irvin, 111, and Jacqueline Whang 22 The Effects of Allografts of Thymic Epithelial Reticular Cells on the Lymphoid Tissues of Neonatally Thymectomized...

Hechang Lei ( ),1 Emil S. Bozin,1 A. Llobet,2 V. Ivanovski,3 V. Koteski,3 J. Belosevic-Cavor,3 B. Cekic,3 and C. Petrovic1 1Condensed Matter Physics and Materials Science Department, Brookhaven National Laboratory, Uptown, New York 11973, USA 2Lujan Neutron Scattering Center, Los Alamos National Laboratory, MS H805, Los Alamos, New Mexico 87545, USA 3Institute of Nuclear Sciences Vinca, Univers...

We present a comparison of the energetics of spiral formation for two vinca alkaloids: a novel difluorinated vinorelbine derivative 20',20'-difluoro-3',4'-dihydrovinorelbine (F12158, or vinflunine) and the parent compound, vinorelbine. Vinca alkaloids are antineoplastic agents that halt cell division at metaphase by inhibiting microtubule assembly and inducing tubulin self-association into spir...

The continuous exposure of antimicrotubule drugs to tumors often results in the emergence of drug-resistant tumor cells with altered expression of several beta-tubulin isotypes. We found that Vinca alkaloid enhanced expression of class II beta-tubulin isotype (mTUBB2) in mouse B16F10 melanoma cells via alteration of the tumor suppressor p53 protein. Vincristine treatment stimulated an increase ...

BACKGROUND New treatment models are needed for the management of advanced stage head and neck carcinomas (HNSCC). Vinflunine is a novel vinca alkaloid which has shown remarkable improvement in efficiency and reduced side-effects in both in vitro and in vivo studies. Better locoregional control and prevention of distant metastasis in advanced HNSCC would be welcome and, with this new efficient c...

The plasticity and instability of the cancer genome is impressive and is characterized by gene amplifications and deletions, rearrangements, and many silent and active mutations. Although targeted therapeutics have had effect in some diseases, there remains a large role for new cytotoxic agents that have the potential to be broadly active across multiple cancers. Platinum-based regimens are the...

Antibodies reactive with human epidermal growth factor receptor (EGFr), such as 225 IgG1 (Masui et al., Cancer Res., 44: 1002-1007, 1984), are effective tumor-suppressive agents in xenograft models. In the present study an additional antibody reactive with EGFr was made and compared to 225 IgG1 for antitumor activity as an unmodified antibody or as a drug immunoconjugate. This IgG1 clone, desig...

Microtubule targeting drugs like taxanes, vinca alkaloids, and epothilones are widely-used and effective chemotherapeutic agents that target the dynamic instability of microtubules and inhibit spindle functioning. However, these drugs have limitations associated with their production, solubility, efficacy and unwanted toxicities, thus driving the need to identify novel antimitotic drugs that ca...

Farnesyl transferase (FTase) is an enzyme responsible for post-translational modification in proteins having a carboxy-terminal CaaX motif in human. It catalyzes the attachment of a lipid group in proteins of RAS superfamily, which is essential in signal transduction. FTase has been recognized as an important target for anti cancer therapeutics. In this work, we performed virtual screening agai...

Antibody-drug conjugates (ADC) are an emerging drug class that uses antibodies to improve cytotoxic drug targeting for cancer treatment. ADCs in current clinical trials achieve a compromise between potency and physicochemical/pharmacokinetic properties by conjugating potent cytotoxins directly to an antibody at a 4:1 or less stoichiometric ratio. Herein, we report a novel, polyacetal polymer-ba...