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The Prostate, ISSN 0270-4137, 06/2018, Volume 78, Issue 9, pp. 655 - 663
Background The SH‐group at Cys‐34 of human serum albumin (HSA) is a unique and accessible functional group that can be exploited for efficient linkage of a... 
maleimide linkage | prostate cancer | albumin based drug uptake | EPR effect | CATABOLISM | PROTEIN | SERUM-ALBUMIN | STABILIZATION | TUMOR | FATTY-ACIDS | METABOLISM | MALEIMIDES | ENDOCRINOLOGY & METABOLISM | UROLOGY & NEPHROLOGY | CYSTEINE-34 | BINDING | Extracellular Fluid - chemistry | Antineoplastic Agents - chemical synthesis | Humans | Sesquiterpenes - pharmacokinetics | Maleimides - pharmacology | Male | Antineoplastic Agents - therapeutic use | Prodrugs - chemistry | Sesquiterpenes - chemical synthesis | Sesquiterpenes - therapeutic use | Prostatic Neoplasms, Castration-Resistant - secondary | Lactones - chemical synthesis | Cytotoxins - pharmacology | Maleimides - therapeutic use | Lactones - pharmacokinetics | Maleimides - chemical synthesis | Antineoplastic Agents - pharmacology | Prostate-Specific Antigen - metabolism | Lactones - chemistry | Cytotoxins - therapeutic use | Cytotoxins - chemical synthesis | Sesquiterpenes - chemistry | Prostatic Neoplasms, Castration-Resistant - drug therapy | Antineoplastic Agents - chemistry | Prostatic Neoplasms, Castration-Resistant - metabolism | Extracellular Fluid - drug effects | Lactones - therapeutic use | Serum Albumin, Human - therapeutic use | Serum Albumin, Human - pharmacology | Cytotoxins - chemistry | Cell Line, Tumor | Prodrugs - chemical synthesis | Prodrugs - therapeutic use | Maleimides - chemistry | Drug Delivery Systems - methods | Prodrugs - pharmacology | Albumin | Metastasis | Chemical synthesis | Prostate cancer | Analysis | Thapsigargin | Human serum albumin | Castration | Xenografts | Cytotoxicity | Prostate | Metastases | Ca2+-transporting ATPase | Index Medicus
Journal Article
Journal Article
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 08/2017, Volume 60, Issue 15, pp. 6678 - 6692
Porcupine is an O-acyltransferase that regulates Wnt secretion. Inhibiting porcupine may block the Wnt pathway which is often dysregulated in various cancers.... 
TARGET | CHEMISTRY, MEDICINAL | PATHWAY | MECHANISMS | BETA-CATENIN | WNT | CANCER | Acyltransferases - antagonists & inhibitors | Maleimides - administration & dosage | Cytochrome P-450 CYP3A Inhibitors - pharmacology | Antineoplastic Agents - chemical synthesis | Humans | Microsomes, Liver - metabolism | Maleimides - pharmacology | Cytochrome P-450 CYP3A Inhibitors - pharmacokinetics | Structure-Activity Relationship | Antineoplastic Agents - administration & dosage | Pyridazines - pharmacology | Pyridazines - chemical synthesis | Maleimides - pharmacokinetics | Cytochrome P-450 CYP1A2 Inhibitors - pharmacokinetics | Maleimides - chemical synthesis | HEK293 Cells | Pyridazines - administration & dosage | Female | Antineoplastic Agents - pharmacokinetics | Antineoplastic Agents - pharmacology | Cytochrome P-450 CYP2D6 Inhibitors - pharmacology | Wnt Signaling Pathway | Cytochrome P-450 CYP2D6 Inhibitors - pharmacokinetics | Cytochrome P-450 CYP3A Inhibitors - administration & dosage | Rats | Cytochrome P-450 CYP1A2 Inhibitors - chemical synthesis | Cytochrome P-450 CYP2D6 Inhibitors - administration & dosage | Cytochrome P-450 CYP3A Inhibitors - chemical synthesis | Xenograft Model Antitumor Assays | Animals | Cytochrome P-450 CYP1A2 Inhibitors - pharmacology | Cytochrome P-450 CYP2D6 Inhibitors - chemical synthesis | High-Throughput Screening Assays | Membrane Proteins - antagonists & inhibitors | Mice, Nude | Cytochrome P-450 CYP1A2 Inhibitors - administration & dosage | Cell Line, Tumor | Pyridazines - pharmacokinetics | Mice, Inbred BALB C
Journal Article
Biomaterials, ISSN 0142-9612, 2013, Volume 34, Issue 19, pp. 4602 - 4611
Journal Article
Journal Article
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 10/2013, Volume 68, pp. 361 - 371
A series of 7-azaindazolyl-indolyl-maleimides were designed, synthesized and evaluated for their GSK-3β inhibitory activity. Most compounds exhibited potent... 
Cellular activity | 7-Azaindazolyl-indolyl-maleimides | Enzymatic activity | GSK-3β inhibitors | Protein Kinase Inhibitors - chemical synthesis |