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The resurgence of platinum-based cancer chemotherapy
- L. Kèlland
- Nature Reviews Cancer
- 1 August 2007
Key developments include the elucidation of mechanisms of tumour resistance to these drugs, the introduction of new platinum-based agents (oxaliplatin, satraplatin and picoplatin), and clinical combination studies using platinum drugs with resistance modulators or new molecularly targeted drugs. Expand
Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases.
Despite its rapid in vivo metabolism, PI103 is a valuable tool compound for exploring the biological function of class I PI3K and importantly represents a lead for further optimization of this novel class of targeted molecular cancer therapeutic. Expand
Discovery and development of anticancer aptamers
The most advanced aptamer in the cancer setting is AS1411, formerly known as AGRO100, which is being administered systemically in clinical trials and seems to involve initial binding to cell surface nucleolin and internalization, leading to an inhibition of DNA replication. Expand
In vitro and In vivo Pharmacokinetic-Pharmacodynamic Relationships for the Trisubstituted Aminopurine Cyclin-Dependent Kinase Inhibitors Olomoucine, Bohemine and CYC202
- F. Raynaud, S. Whittaker, +12 authors P. Workman
- Biology, Medicine
- Clinical Cancer Research
- 1 July 2005
YC202 showed therapeutic activity on human cancer cell lines in vitro and on xenografts and Pharmacodynamic markers are altered in vivo and in vivo, consistent with the inhibition of cyclin-dependent kinases. Expand
New platinum antitumor complexes.
- L. Kèlland
- Critical reviews in oncology/hematology
- 1 December 1993
Over the past two decades, platinum-based drugs (cisplatin and, latterly, the less toxic analogue carboplatin) have conferred significant therapeutic benefit to a large number of cancer sufferers.… Expand
DT-Diaphorase expression and tumor cell sensitivity to 17-allylamino, 17-demethoxygeldanamycin, an inhibitor of heat shock protein 90.
- L. Kèlland, S. Sharp, P. Rogers, T. Myers, P. Workman
- Biology, Medicine
- Journal of the National Cancer Institute
- 17 November 1999
The results suggest that the antitumor activity and possibly the toxicologic properties of 17AAG in humans may be influenced by the expression of DT-diaphorase. Expand
Platinum-Based Drugs in Cancer Therapy
The first € price and the £ and $ price are net prices, subject to local VAT. Prices indicated with * include VAT for books; the €(D) includes 7% for Germany, the €(A) includes 10% for Austria.… Expand
Phase II study of the efficacy and tolerability of two dosing regimens of the farnesyl transferase inhibitor, R115777, in advanced breast cancer.
- S. Johnston, T. Hickish, +8 authors A. Howes
- Journal of clinical oncology : official journal…
- 1 July 2003
The farnesyl transferase inhibitor R115777 has demonstrated clinical activity in patients with metastatic breast cancer, and the ID regimen has a significantly improved therapeutic index compared with the CD regimen. Expand
A G-quadruplex-interactive potent small-molecule inhibitor of telomerase exhibiting in vitro and in vivo antitumor activity.
The antitelomerase and antitumor properties of a small-molecule compound designed by computer modeling to interact with and stabilize human G-quadruplex DNA, a structure that may form with telomeric DNA, thereby inhibiting access to telomerase, are described. Expand
A G-quadruplex telomere targeting agent produces p16-associated senescence and chromosomal fusions in human prostate cancer cells.
- Christopher M Incles, C. Schultes, H. Kempski, H. Koehler, L. Kèlland, S. Neidle
- Medicine, Biology
- Molecular cancer therapeutics
- 1 October 2004
Evidence is presented showing that the inhibition of cell growth caused by BRACO-19 in DU145 prostate cancer cells occurs more rapidly than would be expected solely by the inhibitor of the catalytic function of telomerase, and that senescence is accompanied by an initial up-regulation of the cyclin-dependent kinase inhibitor p21. Expand