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TherapeuticAdvances 2003 Archive
TherapeuticAdvances is up-dated twice-monthly highlighting 100's novel projects ready for development and commercialization.
To view the 2002 Therapeutic Advances Archive click here! - for the 2004 listings click here!
January-December 2003
Target of the Month: Janus tyrosine kinase 3 inhibition for the prevention of transplant rejection NVP-LAQ824 a novel histone deacetylase inhibitor Cx43 as a target for improved wound healing Development of GSK-3 inhibitors by GlaxoSmithKline and by Johnson & Johnson HDAC7: A novel target for autoimmune disorders Ki-67 as a target for anticancer strategies Successful gene therapy of pulmonary hypertension MAPK/ERK-kinase inhibitors as a promising strategy for the treatment of neuropathic pain Retinoids as candidate targets for alzheimer’s disease treatment PI3K inhibitors: Targeting multiple tumor progression pathways Gap junctions: The future of cancer therapy and prevention? Advances in Kv1.3 channel research Sigma(1) agonists offer hope to Alzheimer’s disease patients Target "Lifestyle" BAY 41-2272: A novel guanylate cyclase activator for the treatment of erectile dysfunction Expanding the therapeutic benefit of sildenafil to the treatment of premature ejaculation Oxytocin as a treatment of erectile dysfunction Stimulation of angiogenesis as an approach to erectile dysfunction The effect of PDE5 inhibition on patients with stable angina Focus on Airway disease: Effects of Phosphodiesterase 4 (PDE4) inhibition on host defense PDE4D: A target for the treatment of airway hyper-responsiveness in asthma IDEC-152 as a candidate treatment of asthma AWD 12-281, a PDE4 inhibitor with low emetic potential Syk tyrosine kinase as a target for asthma Suplatast tosilate: Anti-asthma properties Targeting NKT cells for the treatment of asthma The role of VEGF in emphysema Improved PDE4 inhibitors Potential benefits of retinoid treatment to COPD sufferers A small molecule inhibitor of VLA-4 for the treatment of allergic airway disease Treating corticosteroid resistant airway disease Steroid treatment of COPD: relationship to MMP-9 Targeting phosphodiesterases for the treatment of pulmonary hypertension Focus on Oncology: Targeting oncolytic viruses to colorectal tumors Increasing the anticancer efficacy of docetaxel by ERK inhibitors Advances in the development of histone deacetylase inhibitors siRNA blocking CXCR4 expression limits metastasis Development of an oncolytic virus targeted to the hypoxic tumor milieu Leptin and its role in tumor progression Cpd 5, a novel Cdc25A inhibitor with anticancer activi Aurora2 inhibitors for the treatment of cancer Oncolytic viruses as a means of improving radiation therapy ATN-161, and integrin antagonists that reduces angiogenesis and tumor progression Reintroducing retinoid sensitivity to breast cancer cells A-161906 a TGF-beta-like agonist that acts via histone deacetylase inhibition Advances in anticancer retinoids Combined use of histone deacetylase and methylation inhibitors for improved tumor control Focus on CardioVascular disease: PDE5 inhibition as a treatment of pulmonary hypertension The involvement of PDE4D in stroke Targeting PDE5 for the treatment of pulmonary hypertension Targeted delivery of thrombolytics to newly formed thrombi Lithium as a treatment for stroke A stable preparation of PGI2 as an effective treatment of stroke Recombinant VEGF improves angina HO-1 as a target for ischemic disease SSR69071: A highly potent elastase inhibitor Further benefits of targeting angiotensin for the prevention of stroke RWJ-58259 a PAR-1 antagonist with antithrombotic activity FGF-4 gene transfer as a treatment of limb ischemia Fractalkine:CX3CR1 binding as a target for coronary artery disease Focus on Metabolic Diseases: Alpha(v)beta(3) integrin antagonism as a treatment of osteoporosis 11beta-hydroxysteroid dehydrogenase inhibition reduces insulin resistance Stimulating Munc1-13 as a means of increasing insulin release Stearoyl-CoA desaturase (SCD) as a target for diabetes Bone hypoxia: A contributor to bone fracture Kv1.3 potassium channels as targets for the treatment of obesity Treatments for pulmonary hypertension A novel target for osteoporosis NO and NMDA in the control of osteoclast function Mitofusin 2: a regulator of energy expenditure that contributes to the development of obesity Targeting RXR receptors for the treatment of diabetes and obesity Matrix metalloproteinases, an emerging target for obesity Neuropeptide Y involvement in insulin resistance JNK1 as a promising target for obesity, diabetes and insulin resistance Focus on Immunology & Inflammatory disease: FR167653, a candidate p38 MAPK inhibitor for the treatment of rheumatoid arthritis VEGFR-1 as a target for rheumatoid arthritis therapies Blocking Tie-2 as a treatment of rheumatoid arthritis Ribozyme technology as an effective approach to HBV infection Kv1.3 potassium channel blockade as an immunomodulatory strategy FTY720 as a treatment for multiple sclerosis A pilot trial of SCH55700, a humanized monoclonal antibody to IL-5 The role of p-glycoprotein in intestinal damage IL-2 antibodies as an effective treatment of ulcerative colitis Clinical potential of retinoid RAR antagonists in arthritis SangStat’s RDP58 as a novel anti-inflammatory TNF anti-sense oligonucleotides for the treatment of chronic inflammation T-614 induces bone formation offering improved treatment of rheumatoid arthritis Focus on infectious disease: Advances in the treatment of HSV-1 infection Mechanisms underlying the respiratory symptomology of RSV infection P-glycoprotein inhibitors as adjuvants to antimicrobials Optimizing ribozyme therapeutics E5564: An emerging treatment of sepsis CS-758, an antifungal with activity in fluconazole-resistant candidiasis Advances in infectious disease Gene silencing as an approach to HIV infection Focus on Pain 5-HT3 receptor antagonists as analgesics T-type Ca2+ channel involvement in visceral pain Cannabinoid receptor ligands in the treament of pain HSV transfer of Glial cell-derived neurotrophic factor (GDNF) as a treatment of pain F 13640, a novel candidate analgesic A potent VR1 receptor antagonist blocks inflammatory and neuropathic pain F 13640, an exciting candidate analgesic H3 agonists as prophylactic treatments of migraine Newron’s NW-1029, a candidate for inflammatory and neuropathic pain Postsynaptic density protein-95 (PSD-95) as a target for neuropathic pain NaV1.8, a sodium channel target for the treatment of chronic pain Nociceptin:ORL-1 as a target for analgesia The involvement of 5-HT1B/1D receptors in trigeminal pain pathways Focus on CNS Disease: Novel corticotropin-releasing factor (CRF) receptor antagonists as effective anxiolytics Efficacy of the mixed 5-HT2 antagonist/SSRI, nefadozone in Parkinson’s disease RS-1259, a dual inhibitor of AChE and SERT for treating Alzheimers disease CB2 receptor agonists with anagesic activity Development of highly potent inhibitors of the cannabinoid transporter Muscarinic receptor activation reduces Abeta1-42 in Alzheimer’s disease Induction of NGF as a treatment of Alzheimer’s disease Astrocytes as a target for Alzheimers disease therapeutics GSK-3 in the etiology of schizophrenia Increasing central leptin levels reduces obesity Effects of ghrelin on memory and behavior Targeting the Inhibitor of Apoptosis family for the treatment of neurodegenerative disorders Further evidence linking GSK-3 to Alzheimer’s disease Advances in Alzheimer’s disease vaccine therapy Focus on Angiogenesis: Bisphosphonates as inhibitors of tumor angiogenesis Mutual regulation of angiogenesis and adipogenesis Combined radiation/SU11248 therapy for the treatment of cancer Arteriogenesis as a treatment of stroke Angiostatin gene transfer as an approach to the treatment of metastatic liver cancer An alpha(1)beta(1) integrin antagonist with anticancer activity RNAi technology for the development of improved VEGF therapeutics Small molecule antagonists of FGF tyrosine kinase receptor binding CD146, a target for the inhibition of angiogenesis Phenylacetate-bisphosphonate as a new anticancer candidate Dual inhibition of Rho kinase and matrix metalloproteinases offers effective approach to cancer Cannabinoid agonists as anticancer agents Stem cell treatment of myocardial infarction Endorepellin, a novel anticancer target Focus on Cell Death: Mechanisms of apoptosis in Alzheimers disease Protein kinase C delta (PKC delta) inhibitors as a target for pro-apoptotic treatment of cancer CD271, a retinoid with potential for the treatment of colon cancer High throughput screening for stimulators of apoptosis ARMER, a novel regulator of apoptosis Ketotifen widens the therapeutic window of doxorubicin Retinoids as inhibitors of I-kappaB kinase (IKK) Pro-apoptotic effects of retinoid like molecules XIAP inhibitors as treatments for hormone resistant prostate cancer KRN5500 induces apoptosis in leukemia cells Histone deacetylase involvement in neuroprotection Histone deacetylase regulates survivin expression and apoptosis Lipoxygenase inhibitors as treatments of pancreatic cancer Reintroducing apoptosis into cancer cells by inhibiting specific tyrosine kinase activity Licensing Opportunities/Patent Update: ED-71: a vitamin D analogue with bone selective activity ONT-093: A P-glycoprotein inhibitor for use in patients with cancer, chronic pain, epilepsy and HIV infection Focus on industrial development: Strategies for improving high throughput screening Axokine: Phase II and III studies demonstrating anti-obesity efficacy Tryptase TC30, a novel target for influenza therapeutics Non-peptidic protein tyrosine phosphatase inhibitors Biochemical and pharmacological characterization of SSR69071, a novel orally active elastase inhibitor. Key advances in the development of glycogen synthase kinase-3 (GSK-3) inhibitors Targeting growth factors to prevent ischemic cell death following stroke Novel inhibitors of VEGFR-2 and VEGFR-3 kinase CXCR2 antagonism as an approach to rheumatoid arthritis Small molecule inhibition of caspase 3/7 as a treatment of cardiovascular disease
Target of the Month:
Janus tyrosine kinase 3 inhibition for the prevention of transplant rejection
NVP-LAQ824 a novel histone deacetylase inhibitor
Cx43 as a target for improved wound healing
Development of GSK-3 inhibitors by GlaxoSmithKline and by Johnson & Johnson
HDAC7: A novel target for autoimmune disorders
Ki-67 as a target for anticancer strategies
Successful gene therapy of pulmonary hypertension
MAPK/ERK-kinase inhibitors as a promising strategy for the treatment of neuropathic pain
Retinoids as candidate targets for alzheimer’s disease treatment
PI3K inhibitors: Targeting multiple tumor progression pathways
Gap junctions: The future of cancer therapy and prevention?
Advances in Kv1.3 channel research
Sigma(1) agonists offer hope to Alzheimer’s disease patients
Target "Lifestyle"
BAY 41-2272: A novel guanylate cyclase activator for the treatment of erectile dysfunction
Expanding the therapeutic benefit of sildenafil to the treatment of premature ejaculation
Oxytocin as a treatment of erectile dysfunction
Stimulation of angiogenesis as an approach to erectile dysfunction
The effect of PDE5 inhibition on patients with stable angina
Focus on Airway disease:
Effects of Phosphodiesterase 4 (PDE4) inhibition on host defense
PDE4D: A target for the treatment of airway hyper-responsiveness in asthma
IDEC-152 as a candidate treatment of asthma
AWD 12-281, a PDE4 inhibitor with low emetic potential
Syk tyrosine kinase as a target for asthma
Suplatast tosilate: Anti-asthma properties
Targeting NKT cells for the treatment of asthma
The role of VEGF in emphysema
Improved PDE4 inhibitors
Potential benefits of retinoid treatment to COPD sufferers
A small molecule inhibitor of VLA-4 for the treatment of allergic airway disease
Treating corticosteroid resistant airway disease
Steroid treatment of COPD: relationship to MMP-9
Targeting phosphodiesterases for the treatment of pulmonary hypertension
Focus on Oncology:
Targeting oncolytic viruses to colorectal tumors
Increasing the anticancer efficacy of docetaxel by ERK inhibitors
Advances in the development of histone deacetylase inhibitors
siRNA blocking CXCR4 expression limits metastasis
Development of an oncolytic virus targeted to the hypoxic tumor milieu
Leptin and its role in tumor progression
Cpd 5, a novel Cdc25A inhibitor with anticancer activi
Aurora2 inhibitors for the treatment of cancer
Oncolytic viruses as a means of improving radiation therapy
ATN-161, and integrin antagonists that reduces angiogenesis and tumor progression
Reintroducing retinoid sensitivity to breast cancer cells
A-161906 a TGF-beta-like agonist that acts via histone deacetylase inhibition
Advances in anticancer retinoids
Combined use of histone deacetylase and methylation inhibitors for improved tumor control
Focus on CardioVascular disease:
PDE5 inhibition as a treatment of pulmonary hypertension
The involvement of PDE4D in stroke
Targeting PDE5 for the treatment of pulmonary hypertension
Targeted delivery of thrombolytics to newly formed thrombi
Lithium as a treatment for stroke
A stable preparation of PGI2 as an effective treatment of stroke
Recombinant VEGF improves angina
HO-1 as a target for ischemic disease
SSR69071: A highly potent elastase inhibitor
Further benefits of targeting angiotensin for the prevention of stroke
RWJ-58259 a PAR-1 antagonist with antithrombotic activity
FGF-4 gene transfer as a treatment of limb ischemia
Fractalkine:CX3CR1 binding as a target for coronary artery disease
Focus on Metabolic Diseases:
Alpha(v)beta(3) integrin antagonism as a treatment of osteoporosis
11beta-hydroxysteroid dehydrogenase inhibition reduces insulin resistance
Stimulating Munc1-13 as a means of increasing insulin release
Stearoyl-CoA desaturase (SCD) as a target for diabetes
Bone hypoxia: A contributor to bone fracture
Kv1.3 potassium channels as targets for the treatment of obesity
Treatments for pulmonary hypertension
A novel target for osteoporosis
NO and NMDA in the control of osteoclast function
Mitofusin 2: a regulator of energy expenditure that contributes to the development of obesity
Targeting RXR receptors for the treatment of diabetes and obesity
Matrix metalloproteinases, an emerging target for obesity
Neuropeptide Y involvement in insulin resistance
JNK1 as a promising target for obesity, diabetes and insulin resistance
Focus on Immunology & Inflammatory disease:
FR167653, a candidate p38 MAPK inhibitor for the treatment of rheumatoid arthritis
VEGFR-1 as a target for rheumatoid arthritis therapies
Blocking Tie-2 as a treatment of rheumatoid arthritis
Ribozyme technology as an effective approach to HBV infection
Kv1.3 potassium channel blockade as an immunomodulatory strategy
FTY720 as a treatment for multiple sclerosis
A pilot trial of SCH55700, a humanized monoclonal antibody to IL-5
The role of p-glycoprotein in intestinal damage
IL-2 antibodies as an effective treatment of ulcerative colitis
Clinical potential of retinoid RAR antagonists in arthritis
SangStat’s RDP58 as a novel anti-inflammatory
TNF anti-sense oligonucleotides for the treatment of chronic inflammation
T-614 induces bone formation offering improved treatment of rheumatoid arthritis
Focus on infectious disease:
Advances in the treatment of HSV-1 infection
Mechanisms underlying the respiratory symptomology of RSV infection
P-glycoprotein inhibitors as adjuvants to antimicrobials
Optimizing ribozyme therapeutics
E5564: An emerging treatment of sepsis
CS-758, an antifungal with activity in fluconazole-resistant candidiasis
Advances in infectious disease
Gene silencing as an approach to HIV infection
Focus on Pain
5-HT3 receptor antagonists as analgesics
T-type Ca2+ channel involvement in visceral pain
Cannabinoid receptor ligands in the treament of pain
HSV transfer of Glial cell-derived neurotrophic factor (GDNF) as a treatment of pain
F 13640, a novel candidate analgesic
A potent VR1 receptor antagonist blocks inflammatory and neuropathic pain
F 13640, an exciting candidate analgesic
H3 agonists as prophylactic treatments of migraine
Newron’s NW-1029, a candidate for inflammatory and neuropathic pain
Postsynaptic density protein-95 (PSD-95) as a target for neuropathic pain
NaV1.8, a sodium channel target for the treatment of chronic pain
Nociceptin:ORL-1 as a target for analgesia
The involvement of 5-HT1B/1D receptors in trigeminal pain pathways
Focus on CNS Disease:
Novel corticotropin-releasing factor (CRF) receptor antagonists as effective anxiolytics
Efficacy of the mixed 5-HT2 antagonist/SSRI, nefadozone in Parkinson’s disease
RS-1259, a dual inhibitor of AChE and SERT for treating Alzheimers disease
CB2 receptor agonists with anagesic activity
Development of highly potent inhibitors of the cannabinoid transporter
Muscarinic receptor activation reduces Abeta1-42 in Alzheimer’s disease
Induction of NGF as a treatment of Alzheimer’s disease
Astrocytes as a target for Alzheimers disease therapeutics
GSK-3 in the etiology of schizophrenia
Increasing central leptin levels reduces obesity
Effects of ghrelin on memory and behavior
Targeting the Inhibitor of Apoptosis family for the treatment of neurodegenerative disorders
Further evidence linking GSK-3 to Alzheimer’s disease
Advances in Alzheimer’s disease vaccine therapy
Focus on Angiogenesis:
Bisphosphonates as inhibitors of tumor angiogenesis
Mutual regulation of angiogenesis and adipogenesis
Combined radiation/SU11248 therapy for the treatment of cancer
Arteriogenesis as a treatment of stroke
Angiostatin gene transfer as an approach to the treatment of metastatic liver cancer
An alpha(1)beta(1) integrin antagonist with anticancer activity
RNAi technology for the development of improved VEGF therapeutics
Small molecule antagonists of FGF tyrosine kinase receptor binding
CD146, a target for the inhibition of angiogenesis
Phenylacetate-bisphosphonate as a new anticancer candidate
Dual inhibition of Rho kinase and matrix metalloproteinases offers effective approach to cancer
Cannabinoid agonists as anticancer agents
Stem cell treatment of myocardial infarction
Endorepellin, a novel anticancer target
Focus on Cell Death:
Mechanisms of apoptosis in Alzheimers disease
Protein kinase C delta (PKC delta) inhibitors as a target for pro-apoptotic treatment of cancer
CD271, a retinoid with potential for the treatment of colon cancer
High throughput screening for stimulators of apoptosis
ARMER, a novel regulator of apoptosis
Ketotifen widens the therapeutic window of doxorubicin
Retinoids as inhibitors of I-kappaB kinase (IKK)
Pro-apoptotic effects of retinoid like molecules
XIAP inhibitors as treatments for hormone resistant prostate cancer
KRN5500 induces apoptosis in leukemia cells
Histone deacetylase involvement in neuroprotection
Histone deacetylase regulates survivin expression and apoptosis
Lipoxygenase inhibitors as treatments of pancreatic cancer
Reintroducing apoptosis into cancer cells by inhibiting specific tyrosine kinase activity
Licensing Opportunities/Patent Update:
ED-71: a vitamin D analogue with bone selective activity
ONT-093: A P-glycoprotein inhibitor for use in patients with cancer, chronic pain, epilepsy and HIV infection
Focus on industrial development:
Strategies for improving high throughput screening
Axokine: Phase II and III studies demonstrating anti-obesity efficacy
Tryptase TC30, a novel target for influenza therapeutics
Non-peptidic protein tyrosine phosphatase inhibitors
Biochemical and pharmacological characterization of SSR69071, a novel orally active elastase inhibitor.
Key advances in the development of glycogen synthase kinase-3 (GSK-3) inhibitors
Targeting growth factors to prevent ischemic cell death following stroke
Novel inhibitors of VEGFR-2 and VEGFR-3 kinase
CXCR2 antagonism as an approach to rheumatoid arthritis
Small molecule inhibition of caspase 3/7 as a treatment of cardiovascular disease
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