NATURE CHEMICAL BIOLOGY, ISSN 1552-4450, 01/2006, Volume 2, Issue 1, pp. 29 - 30
Hedgehog (Hh) signaling is an important regulator of embryonic patterning, tissue regeneration, stem cell renewal and cancer growth. A purine derivative named...
INHIBITION | SMALL-MOLECULE | BIOCHEMISTRY & MOLECULAR BIOLOGY | CYCLOPAMINE | OSTEOGENESIS
INHIBITION | SMALL-MOLECULE | BIOCHEMISTRY & MOLECULAR BIOLOGY | CYCLOPAMINE | OSTEOGENESIS
Journal Article
European Journal of Organic Chemistry, ISSN 1434-193X, 08/2018, Volume 2018, Issue 30, pp. 4147 - 4160
The design and diastereoselective synthesis of new C17 spiro‐lactam C‐nor‐D‐homo steroids is described. These constitute structurally simplified analogues of...
Amination | Diastereoselectivity | Cyclopamine | Spiro‐lactam | Rearrangement | Spiro-lactam | TERATOGENIC COMPOUNDS | ASYMMETRIC-SYNTHESIS | CHEMISTRY, ORGANIC | CELL LUNG | VERATRUM CALIFORNICUM DURAND | TERT-BUTANESULFINYL IMINES | POTENT | CYCLOPAMINE ANALOGS | PROSTATE-CANCER | INHIBITORS | HEDGEHOG SIGNALING PATHWAY
Amination | Diastereoselectivity | Cyclopamine | Spiro‐lactam | Rearrangement | Spiro-lactam | TERATOGENIC COMPOUNDS | ASYMMETRIC-SYNTHESIS | CHEMISTRY, ORGANIC | CELL LUNG | VERATRUM CALIFORNICUM DURAND | TERT-BUTANESULFINYL IMINES | POTENT | CYCLOPAMINE ANALOGS | PROSTATE-CANCER | INHIBITORS | HEDGEHOG SIGNALING PATHWAY
Journal Article
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 09/2017, Volume 8, Issue 9, pp. 953 - 957
The preparation of heteronanoparticles (NPs) with doxorubicin (DOXO) and cyclopamine (CYP) conjugates is presented. Biological evaluation on A431 cell lines...
cancer | doxorubicin | Self-assembled-nanoparticles | drug toxicity | cyclopamine | CHEMISTRY, MEDICINAL | BUILDING-BLOCKS | PODOPHYLLOTOXIN | CANCER STEM-CELLS | PACLITAXEL
cancer | doxorubicin | Self-assembled-nanoparticles | drug toxicity | cyclopamine | CHEMISTRY, MEDICINAL | BUILDING-BLOCKS | PODOPHYLLOTOXIN | CANCER STEM-CELLS | PACLITAXEL
Journal Article
Experimental Cell Research, ISSN 0014-4827, 12/2019, Volume 385, Issue 2, p. 111671
Aberrant activation of Sonic Hedgehog (SHH) pathway has been implicated in a variety of cancers including cholangiocarcinoma (CC); however, the influencing...
Epithelial to mesenchymal transition | Hypoxia | Sonic Hedgehog pathway | Cancer stem cells | Cholangiocarcinoma | Cyclopamine
Epithelial to mesenchymal transition | Hypoxia | Sonic Hedgehog pathway | Cancer stem cells | Cholangiocarcinoma | Cyclopamine
Journal Article
Cancer Research, ISSN 0008-5472, 08/2009, Volume 69, Issue 15, pp. 6007 - 6010
Ligand-dependent and ligand-independent activation of the Hedgehog (Hh) signaling pathway is involved in tumorigenesis. The importance of mutations in Hh...
STEM-CELLS | ONCOLOGY | SONIC HEDGEHOG | PATHWAY | PANCREATIC-CANCER | GROWTH | SELF-RENEWAL | CYCLOPAMINE | COMPARTMENT | MEDULLOBLASTOMA | REQUIREMENT | Neoplasms - metabolism | Hedgehog Proteins - metabolism | Animals | Signal Transduction | Humans
STEM-CELLS | ONCOLOGY | SONIC HEDGEHOG | PATHWAY | PANCREATIC-CANCER | GROWTH | SELF-RENEWAL | CYCLOPAMINE | COMPARTMENT | MEDULLOBLASTOMA | REQUIREMENT | Neoplasms - metabolism | Hedgehog Proteins - metabolism | Animals | Signal Transduction | Humans
Journal Article
Journal of drugs in dermatology : JDD, ISSN 1545-9616, 05/2018, Volume 17, Issue 5, pp. 506 - 508
Vismodegib (Erivedge, Genentech-Roche) is the first in class of Hedgehog pathway inhibitors approved for treatment of metastatic basal cell carcinoma (BCC), or...
PROGENITORS | GENE | BASAL-CELL CARCINOMA | CYCLOPAMINE | MUTATIONS | HUMAN HOMOLOG | DERMATOLOGY
PROGENITORS | GENE | BASAL-CELL CARCINOMA | CYCLOPAMINE | MUTATIONS | HUMAN HOMOLOG | DERMATOLOGY
Journal Article
Medicinal Research Reviews, ISSN 0198-6325, 05/2019, Volume 39, Issue 3, pp. 1137 - 1204
Hedgehog (Hh) signaling is involved in the initiation and progression of various cancers and is essential for embryonic and postnatal development. This pathway...
Smoothened | SMO | Hedgehog inhibitor | nanomedicine | cancer | GDC‐0449 | cyclopamine | structure‐activity relationship (SAR) | GDC-0449 | structure-activity relationship (SAR) | A-RING ANALOGS | CHEMISTRY, MEDICINAL | SIDE-CHAIN ANALOGS | CELL-GROWTH | POTENT SMOOTHENED ANTAGONIST | IN-VITRO | SIGNALING PATHWAY | SMALL-MOLECULE INHIBITORS | CYCLOPAMINE ANALOGS | BIOLOGICAL EVALUATION | PHARMACOLOGY & PHARMACY | HIGHLY POTENT | Animals | Signal Transduction | Humans | Hedgehog Proteins - metabolism | Antineoplastic Agents - therapeutic use | Structure-Activity Relationship | Hedgehog Proteins - antagonists & inhibitors | Smoothened Receptor - metabolism | Antineoplastic Agents - chemistry | Neoplasms - drug therapy | Embryonic development | Care and treatment | Cancer
Smoothened | SMO | Hedgehog inhibitor | nanomedicine | cancer | GDC‐0449 | cyclopamine | structure‐activity relationship (SAR) | GDC-0449 | structure-activity relationship (SAR) | A-RING ANALOGS | CHEMISTRY, MEDICINAL | SIDE-CHAIN ANALOGS | CELL-GROWTH | POTENT SMOOTHENED ANTAGONIST | IN-VITRO | SIGNALING PATHWAY | SMALL-MOLECULE INHIBITORS | CYCLOPAMINE ANALOGS | BIOLOGICAL EVALUATION | PHARMACOLOGY & PHARMACY | HIGHLY POTENT | Animals | Signal Transduction | Humans | Hedgehog Proteins - metabolism | Antineoplastic Agents - therapeutic use | Structure-Activity Relationship | Hedgehog Proteins - antagonists & inhibitors | Smoothened Receptor - metabolism | Antineoplastic Agents - chemistry | Neoplasms - drug therapy | Embryonic development | Care and treatment | Cancer
Journal Article
Organic Letters, ISSN 1523-7060, 06/2016, Volume 18, Issue 12, pp. 3038 - 3040
Demissidine and solanidine, two steroidal alkaloids, are synthesized in eight steps from tigogenin acetate and diosgenin acetate, respectively, which involve...
METABOLITES | AZIDES | SCHMIDT REACTION | CARBOCATIONS | CHEMISTRY, ORGANIC | CYCLOPAMINE | SQUALAMINE | SOLANUM-TUBEROSUM | ALPHA-CHACONINE | GLYCOALKALOIDS | ALKALOIDS
METABOLITES | AZIDES | SCHMIDT REACTION | CARBOCATIONS | CHEMISTRY, ORGANIC | CYCLOPAMINE | SQUALAMINE | SOLANUM-TUBEROSUM | ALPHA-CHACONINE | GLYCOALKALOIDS | ALKALOIDS
Journal Article
International Journal of Cancer, ISSN 0020-7136, 02/2006, Volume 118, Issue 4, pp. 1022 - 1031
Journal Article
Molecular Cell, ISSN 1097-2765, 10/2018, Volume 72, Issue 2, pp. 316 - 327.e5
Primary cilia are required for Smoothened to transduce vertebrate Hedgehog signals, but how Smoothened accumulates in cilia and is activated is incompletely...
CBP | HSD11β2 | oxysterol | Hedgehog | primary cilium | Smoothened | sterol | medulloblastoma | cilia | lipid | OXIDATION | CELLS | BIOCHEMISTRY & MOLECULAR BIOLOGY | 7-DEHYDROCHOLESTEROL | TRAFFICKING | CYCLOPAMINE | PROTEINS | BINDING | LEMLI-OPITZ SYNDROME | HEDGEHOG | MODULATION | CELL BIOLOGY | Physiological aspects | Medical colleges | Lipids | Gliomas
CBP | HSD11β2 | oxysterol | Hedgehog | primary cilium | Smoothened | sterol | medulloblastoma | cilia | lipid | OXIDATION | CELLS | BIOCHEMISTRY & MOLECULAR BIOLOGY | 7-DEHYDROCHOLESTEROL | TRAFFICKING | CYCLOPAMINE | PROTEINS | BINDING | LEMLI-OPITZ SYNDROME | HEDGEHOG | MODULATION | CELL BIOLOGY | Physiological aspects | Medical colleges | Lipids | Gliomas
Journal Article
Chemical Science, ISSN 2041-6520, 2017, Volume 8, Issue 5, pp. 3427 - 3433
The development of novel therapeutic strategies allowing the destruction of tumour cells while sparing healthy tissues is one of the main challenges of cancer...
CYCLOPAMINE GLUCURONIDE PRODRUG | MONOTHERAPY | INHIBITION | ENDOGENOUS SERUM-ALBUMIN | EFFICACY | DOXORUBICIN | BETA-GLUCURONIDASE | RELEASE | ANTITUMOR-ACTIVITY | CHEMISTRY, MULTIDISCIPLINARY | CHEMOTHERAPY | Chemical Sciences | Catalysis
CYCLOPAMINE GLUCURONIDE PRODRUG | MONOTHERAPY | INHIBITION | ENDOGENOUS SERUM-ALBUMIN | EFFICACY | DOXORUBICIN | BETA-GLUCURONIDASE | RELEASE | ANTITUMOR-ACTIVITY | CHEMISTRY, MULTIDISCIPLINARY | CHEMOTHERAPY | Chemical Sciences | Catalysis
Journal Article
Journal of Chinese Pharmaceutical Sciences, ISSN 1003-1057, 04/2017, Volume 26, Issue 4
Journal Article
Anticancer Research, ISSN 0250-7005, 11/2018, Volume 38, Issue 11, pp. 6329 - 6332
Background: Hedgehog (HH), WNT, NOTCH, and mechanistic target of rapamycin (mTOR) signalling pathways are known to regulate the progression of cancer; however,...
NOTCH | Hedgehog | siRNA | WNT | Leukaemia | STEM-CELLS | PROLIFERATION | ONCOLOGY | PATHWAY | GROWTH | leukaemia | CYCLOPAMINE | DIFFERENTIATION | SONIC-HEDGEHOG
NOTCH | Hedgehog | siRNA | WNT | Leukaemia | STEM-CELLS | PROLIFERATION | ONCOLOGY | PATHWAY | GROWTH | leukaemia | CYCLOPAMINE | DIFFERENTIATION | SONIC-HEDGEHOG
Journal Article
Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 12/2017, Volume 114, Issue 52, pp. E11141 - E11150
Hedgehog signaling specifies tissue patterning and renewal, and pathway components are commonly mutated in certain malignancies. Although central to ensuring...
Hedgehog | Smoothened | Cholesterol | Patched | CELLS | ACTIVATION | MULTIDISCIPLINARY SCIENCES | TRAFFICKING | PROTEIN-COUPLED RECEPTORS | IDENTIFICATION | PRIMARY CILIUM | cholesterol | Na+ | CYCLOPAMINE | CANCER PROGRESSION | BINDING | MODULATION | Physiological aspects | Extracellular matrix | Biological assay | Observations | Cholesterol metabolism | Methods | Hedgehog proteins | Biological Sciences | PNAS Plus
Hedgehog | Smoothened | Cholesterol | Patched | CELLS | ACTIVATION | MULTIDISCIPLINARY SCIENCES | TRAFFICKING | PROTEIN-COUPLED RECEPTORS | IDENTIFICATION | PRIMARY CILIUM | cholesterol | Na+ | CYCLOPAMINE | CANCER PROGRESSION | BINDING | MODULATION | Physiological aspects | Extracellular matrix | Biological assay | Observations | Cholesterol metabolism | Methods | Hedgehog proteins | Biological Sciences | PNAS Plus
Journal Article
The Journal of Organic Chemistry, ISSN 0022-3263, 07/2017, Volume 82, Issue 14, pp. 7463 - 7469
A divergent synthesis of solanidine and 22-epi-solanidine, two 25S natural steroidal alkaloids, from 25R-configured diosgenin acetate, is described. Initially,...
HIGHLY ENANTIOSELECTIVE SYNTHESIS | STEROIDAL ALKALOIDS | METABOLITES | ANTICANCER | PROPARGYLAMINES | CHEMISTRY, ORGANIC | CYCLOPAMINE | DEMISSIDINE | ALPHA-CHACONINE | SOLASODINE | GLYCOALKALOIDS
HIGHLY ENANTIOSELECTIVE SYNTHESIS | STEROIDAL ALKALOIDS | METABOLITES | ANTICANCER | PROPARGYLAMINES | CHEMISTRY, ORGANIC | CYCLOPAMINE | DEMISSIDINE | ALPHA-CHACONINE | SOLASODINE | GLYCOALKALOIDS
Journal Article
ISSN 1359-7345, 12/2013, Volume 5, Issue 8, pp. 981 - 984
Interference of the Hedgehog (Hh) signaling pathway by cyclopamine leads to abnormal embryonic development. We monitor this dynamical drug effect in zebrafish...
Journal Article
Frontiers in Oncology, 06/2015, Volume 5
Rhabdomyosarcoma (RMS) are the most common soft tissue sarcoma in children and are divided into two major histological subgroups, i.e. embryonal (ERMS) and...
HHA | GDC-0449 | LDE225 | Rhabdomyosarcoma | Cyclopamine
HHA | GDC-0449 | LDE225 | Rhabdomyosarcoma | Cyclopamine
Journal Article
Clinical Cancer Research, ISSN 1078-0432, 09/2012, Volume 18, Issue 18, pp. 4883 - 4888
The Hedgehog (Hh) signaling pathway regulates embryonic development and may be aberrantly activated in a wide variety of human cancers. Efforts to target...
STEM-CELLS | INHIBITION | ONCOLOGY | TRANSCRIPTION | CYCLOPAMINE | MUTATIONS | PROTEINS | TUMOR-GROWTH | MEDULLOBLASTOMA | HUMAN HOMOLOG | PRIMARY CILIA | Neoplasms - metabolism | Receptors, G-Protein-Coupled - metabolism | Signal Transduction - drug effects | Humans | Smoothened Receptor | Translational Medical Research | Receptors, G-Protein-Coupled - antagonists & inhibitors | Hedgehog Proteins - metabolism | Neoplasms - drug therapy | Smoothened antagonists | basal cell carcinoma | Hedgehog | clinical trials
STEM-CELLS | INHIBITION | ONCOLOGY | TRANSCRIPTION | CYCLOPAMINE | MUTATIONS | PROTEINS | TUMOR-GROWTH | MEDULLOBLASTOMA | HUMAN HOMOLOG | PRIMARY CILIA | Neoplasms - metabolism | Receptors, G-Protein-Coupled - metabolism | Signal Transduction - drug effects | Humans | Smoothened Receptor | Translational Medical Research | Receptors, G-Protein-Coupled - antagonists & inhibitors | Hedgehog Proteins - metabolism | Neoplasms - drug therapy | Smoothened antagonists | basal cell carcinoma | Hedgehog | clinical trials
Journal Article
Experimental Cell Research, ISSN 0014-4827, 04/2013, Volume 319, Issue 7, pp. 1043 - 1053
Erythroleukemia is generally associated with a very poor response and survival to current available therapeutic agents. Cyclooxygenase-2 (COX-2) has been...
Erythroleukemia | Cyclooxygenase-2 | Jervine | Cyclopamine | Apoptosis | Acute leukemia | COX-2 inhibitors | Enzymes | Progesterone | Cellular biology | Leukemia | Steroids
Erythroleukemia | Cyclooxygenase-2 | Jervine | Cyclopamine | Apoptosis | Acute leukemia | COX-2 inhibitors | Enzymes | Progesterone | Cellular biology | Leukemia | Steroids
Journal Article
Chemical Science, ISSN 2041-6520, 05/2017, Volume 8, Issue 5, pp. 3427 - 3433
The development of novel therapeutic strategies allowing the destruction of tumour cells while sparing healthy tissues is one of the main challenges of cancer...
Covalence | Drug delivery systems | Side effects | Effectiveness | Strategy | Mice | Tumors | Cancer
Covalence | Drug delivery systems | Side effects | Effectiveness | Strategy | Mice | Tumors | Cancer
Journal Article
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