Fig. 9.1 CC chemokine receptor 4 (CCR4) and humanized anti-CCR4 monoclonal antibody, KW-0761. The CCR4 gene is located on chromosome 3p24. CCR4 is a seven-domain transmembrane G protein-coupled receptor, and…
Fig. 2.1 Timeline of BCR-ABL findings and development of imatinib 2.2 Molecular Biology of CML 2.2.1 Ph Chromosome The Ph chromosome results from a reciprocal translocation, which involves the BCR…
Response Definitions Hematologic response (HR) Complete hematologic response (CHR) WBC <10 × 109/L Platelet count <450 × 109/L Basophil <5% No immature cells Spleen nonpalpable Cytogenetic response (CyR) Complete cytogenetic…
Fig. 16.1 Structures of deoxyadenosine, cladribine, fludarabine, and clofarabine The basis of selectivity with antiviral agents usually involves selective activation by an enzyme expressed by the virus or selective inhibition…
Fig. 13.1 Timeline of the use of arsenic 13.2 Dosage, Schedule, and Pharmacokinetics of Arsenic Trioxide 13.2.1 Dosage and Administration For remission induction, ATO is administered by a 2-h infusion…
Fig. 4.1 Chemical structures of ABL tyrosine kinases. a Imatinib mesylate, b dasatinib, c nilotinib, d bosutinib, e bafetinib, f ponatinib Point mutations within the ABL kinase domain, which interfere…
Fig. 10.1 Type I and type II FLT3 inhibitors. The binding of FL to the extracellular domain of wild-type FLT3 leads to its dimerization, stabilizing a conformation in an active…
Fig. 15.1 Metabolism of purine nucleotides 15.2 Forodesine Forodesine [BCX-1777, immucillin-H, 7-[(2S,3S,4R,5R)-3,4-dihydroxy-5-hydroxymethyl-2-pyrrolidinyl]-1,5-dihydro-4H-pyrrolo-[3,2-d]-pyrimidin-4-one, monohydrochloride] is a transition-state analog that potently inhibits PNP enzyme activity (Fig. 15.2) [12–15]. Forodesine has shown anticancer…
Fig. 5.1 Chimeric structure of rituximab. Rituximab is a chimeric anti-CD20 monoclonal antibody containing human IgG1 heavy chain and human kappa light chain constant regions and murine immunoglobulin heavy and…
Fig. 14.1 The chemical structures of nelarabine and ara-G. (a) Nelarabine. (b) Ara-G 14.2 Mechanisms of Action 14.2.1 Mechanisms of Action (Fig. 14.2) In the blood, nelarabine is rapidly demethoxylated…
