Past Issues: Cancer

October 2009

Targets and Mechanisms

Wnt it rains

by Steve Edelson, Executive Editor

Published online Oct. 29 2009; doi:10.1038/scibx.2009.1555

Dutch researchers have found a new target in the Wnt pathway called TNIK. The kinase could be druggable and may be a good target in colon and other cancers. But TNIK's general expression pattern will have to be analyzed to evaluate the potential side effects of inhibiting it.

Distillery: Therapeutics

B cell lymphoma

CD20

Published online Oct. 29 2009; doi:10.1038/scibx.2009.1560

In vitro and mouse studies identified a mutant variant of the anti-CD20 mAb Rituxan rituximab that could be used to treat B cell lymphomas.

Distillery: Therapeutics

Cancer

ATG3 autophagy-related 3 homolog (ATG3); viral FLICE-like inhibitory protein (FLIP)

Published online Oct. 29 2009; doi:10.1038/scibx.2009.1561

Studies in mice and in cell culture suggest that triggering cell death with FLIP-derived peptides could help prevent virus-induced cancers like Kaposi's sarcoma and primary effusion lymphoma.

Distillery: Therapeutics

Cancer

K-Ras (KRAS); NF-κB; TANK-binding kinase 1 (TBK1)

Published online Oct. 29 2009; doi:10.1038/scibx.2009.1562

A study in cell culture suggests that inhibiting TBK1 could help treat K-Ras-driven cancers.

Distillery: Therapeutics

Cancer

Mammalian target of rapamycin (mTOR; FRAP; RAFT1); mTOR complex 1 (mTORC1); mTORC2

Published online Oct. 29 2009; doi:10.1038/scibx.2009.1563

Studies in cell culture identified pyrazolopyrimidine analogs as mTOR inhibitors that could help treat cancer.

Distillery: Therapeutics

Cancer

T helper 17 (Th17) cells; IL-17; chemokine CC motif ligand 20 (CCL20; MIP3A); monocyte chemoattractant protein-1 (MCP-1; CCL2)

Published online Oct. 29 2009; doi:10.1038/scibx.2009.1564

Studies in mice suggest that adoptive transfer of tumor-specific Th17 cells could help treat cancer.

Distillery: Therapeutics

Cancer

TTK protein kinase (TTK; MPS1)

Published online Oct. 29 2009; doi:10.1038/scibx.2009.1565

A study in cell culture suggests that antagonizing MPS1 could increase the efficacy of paclitaxel in treating cancer.

Distillery: Therapeutics

Colon cancer

TRAF2 and NCK interacting kinase (TNIK)

Published online Oct. 29 2009; doi:10.1038/scibx.2009.1566

In vitro studies suggest that TNIK inhibitors could help treat colon cancer.

Distillery: Therapeutics

Non–small cell lung cancer (NSCLC)

Epidermal growth factor receptor 1 (HER1; ERBB1); HER2 (ERBB2; neu)

Published online Oct. 29 2009; doi:10.1038/scibx.2009.1567

Studies in cells and in rats suggest that a class of dual HER1 and HER2 inhibitors could help treat drug-resistant NSCLC.

Distillery: Therapeutics

Hydroxysteroid 17-β dehydrogenase 1 (HSD17B1)

Published online Oct. 22 2009; doi:10.1038/scibx.2009.1528

Studies in cell cultures suggest that thienopyrimidinone inhibitors of HSD17B1 could help treat hormone-dependent breast cancer.

Distillery: Therapeutics

Tumor protein p53 (TP53; p53); mdm2 p53 binding protein homolog (MDM2)

Published online Oct. 22 2009; doi:10.1038/scibx.2009.1529

A bee venom–derived peptide could provide a scaffold for p53 inhibitors to treat cancer.

Distillery: Therapeutics

Not applicable

Published online Oct. 22 2009; doi:10.1038/scibx.2009.1530

High throughput profiling suggests that activation of two or more canonical oncogenic pathways could help predict patient survival and guide patient selection in gastric cancer trials.

Distillery: Therapeutics

IKAROS family zinc finger 1 (IKZF1)

Published online Oct. 15 2009; doi:10.1038/scibx.2009.1495

Genetic association studies suggest that deletions in IKZF1 could be used as a prognostic marker for Philadelphia chromosome (Ph)-positive ALL.

Distillery: Therapeutics

v-myb myeloblastosis viral oncogene homolog (avian) (MYB; c-myb); nuclear factor I/B (NFIB)

Published online Oct. 15 2009; doi:10.1038/scibx.2009.1496

Studies in primary tumors and in cell cultures suggest that inhibiting the MYB-NFIB fusion gene could help treat adenoid cystic carcinomas of the breast and head and neck.

Distillery: Therapeutics

Annexin A1 (ANXA1)

Published online Oct. 15 2009; doi:10.1038/scibx.2009.1497

In vitro and mouse studies suggest that inhibiting ANXA1 could help treat cancer.

Distillery: Therapeutics

Cas-Br-M ecotropic retroviral transforming sequence b (CBLB)

Published online Oct. 15 2009; doi:10.1038/scibx.2009.1498

Studies in murine cells and in mice suggest that inhibiting CBLB could boost the activity of NK T cell agonists to treat cancer.

Distillery: Therapeutics

DNA

Published online Oct. 15 2009; doi:10.1038/scibx.2009.1499

In vitro studies identified 1,4,5,8-naphthalentetracarboxylic diimide derivatives that could help treat cancer.

Distillery: Therapeutics

Heat shock protein 70 (Hsp70)

Published online Oct. 15 2009; doi:10.1038/scibx.2009.1500

In vitro and mouse studies suggest that 2-phenylethynesulfonamide (PES) inhibits Hsp70 and could help treat cancer.

Distillery: Therapeutics

MAP kinase 1 (MAPK1; ERK-2)

Published online Oct. 15 2009; doi:10.1038/scibx.2009.1501

SAR studies identified a pyrimidylpyrrole-based ERK-2 inhibitor that could help treat cancer.

Distillery: Therapeutics

DNA (cytosine-5-)-methyltransferase 1 (DNMT1)

Published online Oct. 15 2009; doi:10.1038/scibx.2009.1502

A study in mice suggests that inhibiting DNMT1 could help treat leukemia.

Distillery: Therapeutics

SOX2

Published online Oct. 15 2009; doi:10.1038/scibx.2009.1503

Genetic and in vitro studies suggest that inhibiting SOX2 could help treat lung and esophageal squamous cell carcinomas (SCC).

Targets and Mechanisms

Hitting HIF1 in cancer

by Tim Fulmer, Senior Writer

Published online Oct. 8 2009; doi:10.1038/scibx.2009.1461

Johns Hopkins researchers have identified the first compound that directly inhibits hypoxia-inducible factor 1, a central player in triggering angiogenesis and invasion in solid tumors. The compound, acriflavine, was used as an antibiotic nearly 100 years ago.

Distillery: Therapeutics

Kruppel-like factor 17 (KLF17)

Published online Oct. 8 2009; doi:10.1038/scibx.2009.1465

A study in human samples and in mice suggests that increasing KLF17 expression could help prevent breast cancer metastasis.

Distillery: Therapeutics

Hypoxia-inducible factor 1α (HIF1A; HIF1α); HIF1B (HIF1β)

Published online Oct. 8 2009; doi:10.1038/scibx.2009.1466

In vitro and mouse studies suggest that acriflavine, a small molecule antimicrobial, could help treat cancer.

Distillery: Therapeutics

Mitochondrial transporter

Published online Oct. 8 2009; doi:10.1038/scibx.2009.1467

In vitro and mouse studies suggest that an analog of GSAO could help treat cancer.

Distillery: Therapeutics

Dual specificity phosphatase 3 (DUSP3; VHR)

Published online Oct. 8 2009; doi:10.1038/scibx.2009.1468

In vitro studies identified inhibitors of VHR that could help treat cervical cancer.

Distillery: Therapeutics

Not applicable

Published online Oct. 8 2009; doi:10.1038/scibx.2009.1469

A study in mice suggests that CpG oligonucleotides can boost the CD8+ T cell response and help prevent lymphoma relapse.

Distillery: Therapeutics

Proteasome

Published online Oct. 8 2009; doi:10.1038/scibx.2009.1470

SAR and in vitro studies identified analogs of the proteasome inhibitor salinosporamide A that could help treat MM or mantle cell lymphoma.

Distillery: Therapeutics

Somatostatin receptor 2 (SSTR2); thrombospondin-1 (TSP-1; THBS1)

Published online Oct. 8 2009; doi:10.1038/scibx.2009.1471

A study in tissue culture suggests that increasing the activity of TSP-1 could help treat pancreatic cancer.

Distillery: Therapeutics

Atypical protein kinase C (aPKC); IL-6

Published online Oct. 8 2009; doi:10.1038/scibx.2009.1472

In vitro human and mouse studies suggest that inhibiting aPKC or IL-6 could help treat hormone refractory prostate cancer (HRPC).

Distillery: Therapeutics

Fibroblast growth factor receptor 4 (FGFR4; CD334)

Published online Oct. 8 2009; doi:10.1038/scibx.2009.1473

Studies in human cell culture and in mice suggest that inhibiting FGFR4 could help treat rhabdomyosarcoma.

Distillery: Therapeutics

Tumor protein p53 (TP53; p53)

Published online Oct. 1 2009; doi:10.1038/scibx.2009.1432

A study in mice suggests that p53 expression could help predict sensitivity of medulloblastomas to heat shock protein inhibitors.

Distillery: Therapeutics

BRAF

Published online Oct. 1 2009; doi:10.1038/scibx.2009.1433

Studies in mice identified BRAF inhibitors that could be optimized to help treat cancer.

Distillery: Therapeutics

Not applicable

Published online Oct. 1 2009; doi:10.1038/scibx.2009.1434

In vitro and mouse studies identified a series of Ellence–nitric oxide copolymer conjugates that could help treat cancer.

Distillery: Therapeutics

ABL tyrosine kinase (ABL; ABL1; c-ABL); tumor protein p63 (TP63; p63)

Published online Oct. 1 2009; doi:10.1038/scibx.2009.1435

In vitro and mouse studies suggest that inhibiting the ABL-p63 pathway during cisplatin treatment could help prevent chemotherapy-induced ovarian toxicity.