JP2015531590A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2015531590A5 JP2015531590A5 JP2015524483A JP2015524483A JP2015531590A5 JP 2015531590 A5 JP2015531590 A5 JP 2015531590A5 JP 2015524483 A JP2015524483 A JP 2015524483A JP 2015524483 A JP2015524483 A JP 2015524483A JP 2015531590 A5 JP2015531590 A5 JP 2015531590A5
- Authority
- JP
- Japan
- Prior art keywords
- polypeptide
- amino acid
- nucleic acid
- isolated
- mutant
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 229920001184 polypeptide Polymers 0.000 claims description 85
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 85
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 85
- 150000001413 amino acids Chemical group 0.000 claims description 83
- 150000007523 nucleic acids Chemical class 0.000 claims description 60
- 102000039446 nucleic acids Human genes 0.000 claims description 59
- 108020004707 nucleic acids Proteins 0.000 claims description 59
- 230000035772 mutation Effects 0.000 claims description 39
- 238000006467 substitution reaction Methods 0.000 claims description 34
- 229940123407 Androgen receptor antagonist Drugs 0.000 claims description 29
- 210000004027 cell Anatomy 0.000 claims description 27
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims description 13
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims description 13
- 239000013598 vector Substances 0.000 claims description 12
- 206010060862 Prostate cancer Diseases 0.000 claims description 11
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 11
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims description 9
- 230000000694 effects Effects 0.000 claims description 7
- 238000012217 deletion Methods 0.000 claims description 6
- 230000037430 deletion Effects 0.000 claims description 6
- 108020004414 DNA Proteins 0.000 claims description 5
- 108091032973 (ribonucleotides)n+m Proteins 0.000 claims description 3
- 108020004705 Codon Proteins 0.000 claims description 2
- 241000238631 Hexapoda Species 0.000 claims description 2
- 102000007056 Recombinant Fusion Proteins Human genes 0.000 claims description 2
- 108010008281 Recombinant Fusion Proteins Proteins 0.000 claims description 2
- 230000001580 bacterial effect Effects 0.000 claims description 2
- 239000002299 complementary DNA Substances 0.000 claims description 2
- 210000003527 eukaryotic cell Anatomy 0.000 claims description 2
- 230000001939 inductive effect Effects 0.000 claims description 2
- 125000001909 leucine group Chemical group [H]N(*)C(C(*)=O)C([H])([H])C(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 210000004962 mammalian cell Anatomy 0.000 claims description 2
- 239000013600 plasmid vector Substances 0.000 claims description 2
- 210000001236 prokaryotic cell Anatomy 0.000 claims description 2
- 239000013603 viral vector Substances 0.000 claims description 2
- 210000005253 yeast cell Anatomy 0.000 claims description 2
- 108091028043 Nucleic acid sequence Proteins 0.000 claims 1
- 238000000034 method Methods 0.000 description 85
- 102100032187 Androgen receptor Human genes 0.000 description 83
- 108010080146 androgen receptors Proteins 0.000 description 83
- 235000001014 amino acid Nutrition 0.000 description 54
- 229940024606 amino acid Drugs 0.000 description 35
- 239000000523 sample Substances 0.000 description 19
- 206010028980 Neoplasm Diseases 0.000 description 16
- 201000011510 cancer Diseases 0.000 description 15
- 238000011282 treatment Methods 0.000 description 14
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 8
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 description 7
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical compound NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 description 6
- 150000001875 compounds Chemical class 0.000 description 5
- 238000009115 maintenance therapy Methods 0.000 description 5
- 238000012360 testing method Methods 0.000 description 5
- 239000004471 Glycine Substances 0.000 description 4
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 4
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 description 4
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 description 4
- 108020004711 Nucleic Acid Probes Proteins 0.000 description 4
- 108091034117 Oligonucleotide Proteins 0.000 description 4
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 description 4
- 235000004279 alanine Nutrition 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 description 4
- 229960000310 isoleucine Drugs 0.000 description 4
- 239000002853 nucleic acid probe Substances 0.000 description 4
- 229940124597 therapeutic agent Drugs 0.000 description 4
- 239000004474 valine Substances 0.000 description 4
- 206010005003 Bladder cancer Diseases 0.000 description 3
- 206010006187 Breast cancer Diseases 0.000 description 3
- 208000026310 Breast neoplasm Diseases 0.000 description 3
- 239000000579 Gonadotropin-Releasing Hormone Substances 0.000 description 3
- 108700008625 Reporter Genes Proteins 0.000 description 3
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 description 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 3
- 239000000556 agonist Substances 0.000 description 3
- 239000003098 androgen Substances 0.000 description 3
- 239000005557 antagonist Substances 0.000 description 3
- 229940104302 cytosine Drugs 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 230000001747 exhibiting effect Effects 0.000 description 3
- XLXSAKCOAKORKW-AQJXLSMYSA-N gonadorelin Chemical group C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 XLXSAKCOAKORKW-AQJXLSMYSA-N 0.000 description 3
- 229940035638 gonadotropin-releasing hormone Drugs 0.000 description 3
- 206010073071 hepatocellular carcinoma Diseases 0.000 description 3
- 231100000844 hepatocellular carcinoma Toxicity 0.000 description 3
- 230000005764 inhibitory process Effects 0.000 description 3
- 239000002773 nucleotide Substances 0.000 description 3
- 125000003729 nucleotide group Chemical group 0.000 description 3
- 102000005962 receptors Human genes 0.000 description 3
- 108020003175 receptors Proteins 0.000 description 3
- 201000005112 urinary bladder cancer Diseases 0.000 description 3
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 description 2
- JPQFGMYHKSKKGW-UHFFFAOYSA-N 4-[7-[4-cyano-3-(trifluoromethyl)phenyl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl]-2-fluoro-n-methylbenzamide Chemical compound C1=C(F)C(C(=O)NC)=CC=C1N1C2(CCC2)C(=O)N(C=2C=C(C(C#N)=CC=2)C(F)(F)F)C1=S JPQFGMYHKSKKGW-UHFFFAOYSA-N 0.000 description 2
- 239000004475 Arginine Substances 0.000 description 2
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 description 2
- 208000005443 Circulating Neoplastic Cells Diseases 0.000 description 2
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 2
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 description 2
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 description 2
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 description 2
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 description 2
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 2
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 2
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 description 2
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 description 2
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 description 2
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 description 2
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 description 2
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 description 2
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 2
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 2
- 239000004472 Lysine Substances 0.000 description 2
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 description 2
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 2
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 description 2
- 239000004473 Threonine Substances 0.000 description 2
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 description 2
- 230000008485 antagonism Effects 0.000 description 2
- HJBWBFZLDZWPHF-UHFFFAOYSA-N apalutamide Chemical group C1=C(F)C(C(=O)NC)=CC=C1N1C2(CCC2)C(=O)N(C=2C=C(C(C#N)=NC=2)C(F)(F)F)C1=S HJBWBFZLDZWPHF-UHFFFAOYSA-N 0.000 description 2
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 2
- 235000009582 asparagine Nutrition 0.000 description 2
- 229960001230 asparagine Drugs 0.000 description 2
- 235000003704 aspartic acid Nutrition 0.000 description 2
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 2
- 230000002860 competitive effect Effects 0.000 description 2
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 description 2
- 235000018417 cysteine Nutrition 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- WXCXUHSOUPDCQV-UHFFFAOYSA-N enzalutamide Chemical compound C1=C(F)C(C(=O)NC)=CC=C1N1C(C)(C)C(=O)N(C=2C=C(C(C#N)=CC=2)C(F)(F)F)C1=S WXCXUHSOUPDCQV-UHFFFAOYSA-N 0.000 description 2
- 235000013922 glutamic acid Nutrition 0.000 description 2
- 239000004220 glutamic acid Substances 0.000 description 2
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 description 2
- 235000004554 glutamine Nutrition 0.000 description 2
- UYTPUPDQBNUYGX-UHFFFAOYSA-N guanine Chemical compound O=C1NC(N)=NC2=C1N=CN2 UYTPUPDQBNUYGX-UHFFFAOYSA-N 0.000 description 2
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 2
- 229930182817 methionine Natural products 0.000 description 2
- 238000002493 microarray Methods 0.000 description 2
- 238000012544 monitoring process Methods 0.000 description 2
- 239000008194 pharmaceutical composition Substances 0.000 description 2
- 238000003752 polymerase chain reaction Methods 0.000 description 2
- 108010042121 probasin Proteins 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- RWQNBRDOKXIBIV-UHFFFAOYSA-N thymine Chemical compound CC1=CNC(=O)NC1=O RWQNBRDOKXIBIV-UHFFFAOYSA-N 0.000 description 2
- 210000004881 tumor cell Anatomy 0.000 description 2
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 2
- 102100022089 Acyl-[acyl-carrier-protein] hydrolase Human genes 0.000 description 1
- 229930024421 Adenine Natural products 0.000 description 1
- GFFGJBXGBJISGV-UHFFFAOYSA-N Adenine Chemical compound NC1=NC=NC2=C1N=CN2 GFFGJBXGBJISGV-UHFFFAOYSA-N 0.000 description 1
- 102100022463 Alpha-1-acid glycoprotein 1 Human genes 0.000 description 1
- 108010037003 Buserelin Proteins 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 108010069236 Goserelin Proteins 0.000 description 1
- BLCLNMBMMGCOAS-URPVMXJPSA-N Goserelin Chemical compound C([C@@H](C(=O)N[C@H](COC(C)(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1[C@@H](CCC1)C(=O)NNC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 BLCLNMBMMGCOAS-URPVMXJPSA-N 0.000 description 1
- 102000003964 Histone deacetylase Human genes 0.000 description 1
- 108090000353 Histone deacetylase Proteins 0.000 description 1
- 108010033040 Histones Proteins 0.000 description 1
- 102100028092 Homeobox protein Nkx-3.1 Human genes 0.000 description 1
- 101000824278 Homo sapiens Acyl-[acyl-carrier-protein] hydrolase Proteins 0.000 description 1
- 101000678195 Homo sapiens Alpha-1-acid glycoprotein 1 Proteins 0.000 description 1
- 101000578249 Homo sapiens Homeobox protein Nkx-3.1 Proteins 0.000 description 1
- 101000880402 Homo sapiens Metalloreductase STEAP4 Proteins 0.000 description 1
- 101000638154 Homo sapiens Transmembrane protease serine 2 Proteins 0.000 description 1
- 229940127336 Hormone Receptor Agonists Drugs 0.000 description 1
- 229940123502 Hormone receptor antagonist Drugs 0.000 description 1
- 108010000817 Leuprolide Proteins 0.000 description 1
- 108060001084 Luciferase Proteins 0.000 description 1
- 239000005089 Luciferase Substances 0.000 description 1
- 108010047357 Luminescent Proteins Proteins 0.000 description 1
- 102000006830 Luminescent Proteins Human genes 0.000 description 1
- 108090000856 Lyases Proteins 0.000 description 1
- 102000004317 Lyases Human genes 0.000 description 1
- 102100037654 Metalloreductase STEAP4 Human genes 0.000 description 1
- 241000713333 Mouse mammary tumor virus Species 0.000 description 1
- 238000012408 PCR amplification Methods 0.000 description 1
- 108010072866 Prostate-Specific Antigen Proteins 0.000 description 1
- 102100038358 Prostate-specific antigen Human genes 0.000 description 1
- 239000013614 RNA sample Substances 0.000 description 1
- 108091027981 Response element Proteins 0.000 description 1
- 101100221606 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) COS7 gene Proteins 0.000 description 1
- 102100031989 Transmembrane protease serine 2 Human genes 0.000 description 1
- 229960000643 adenine Drugs 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 230000003321 amplification Effects 0.000 description 1
- 229940035676 analgesics Drugs 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 230000003474 anti-emetic effect Effects 0.000 description 1
- 229940124599 anti-inflammatory drug Drugs 0.000 description 1
- 229940125683 antiemetic agent Drugs 0.000 description 1
- 239000002111 antiemetic agent Substances 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 229940041181 antineoplastic drug Drugs 0.000 description 1
- 238000001574 biopsy Methods 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 210000001185 bone marrow Anatomy 0.000 description 1
- CUWODFFVMXJOKD-UVLQAERKSA-N buserelin Chemical compound CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](COC(C)(C)C)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H]1NC(=O)CC1)CC1=CC=C(O)C=C1 CUWODFFVMXJOKD-UVLQAERKSA-N 0.000 description 1
- 229960002719 buserelin Drugs 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 239000003246 corticosteroid Substances 0.000 description 1
- 229960001334 corticosteroids Drugs 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 108091006047 fluorescent proteins Proteins 0.000 description 1
- 102000034287 fluorescent proteins Human genes 0.000 description 1
- 229960002913 goserelin Drugs 0.000 description 1
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- GFIJNRVAKGFPGQ-LIJARHBVSA-N leuprolide Chemical group CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)CC1=CC=C(O)C=C1 GFIJNRVAKGFPGQ-LIJARHBVSA-N 0.000 description 1
- 229960004338 leuprorelin Drugs 0.000 description 1
- 210000004880 lymph fluid Anatomy 0.000 description 1
- 108020004999 messenger RNA Proteins 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000003199 nucleic acid amplification method Methods 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 235000018102 proteins Nutrition 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 229940113082 thymine Drugs 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261676842P | 2012-07-27 | 2012-07-27 | |
| US61/676,842 | 2012-07-27 | ||
| US201361783763P | 2013-03-14 | 2013-03-14 | |
| US61/783,763 | 2013-03-14 | ||
| US201361829123P | 2013-05-30 | 2013-05-30 | |
| US61/829,123 | 2013-05-30 | ||
| PCT/US2013/052395 WO2014018926A1 (en) | 2012-07-27 | 2013-07-26 | Methods and compositions for determining resistance to androgen receptor therapy |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018028558A Division JP6592545B2 (ja) | 2012-07-27 | 2018-02-21 | アンドロゲン受容体治療に対する抵抗性を判定する方法及び組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015531590A JP2015531590A (ja) | 2015-11-05 |
| JP2015531590A5 true JP2015531590A5 (enExample) | 2016-09-08 |
| JP6297556B2 JP6297556B2 (ja) | 2018-03-20 |
Family
ID=48948536
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015524483A Expired - Fee Related JP6297556B2 (ja) | 2012-07-27 | 2013-07-26 | アンドロゲン受容体治療に対する抵抗性を判定する方法及び組成物 |
| JP2018028558A Expired - Fee Related JP6592545B2 (ja) | 2012-07-27 | 2018-02-21 | アンドロゲン受容体治療に対する抵抗性を判定する方法及び組成物 |
| JP2019171022A Ceased JP2020072655A (ja) | 2012-07-27 | 2019-09-20 | アンドロゲン受容体治療に対する抵抗性を判定する方法及び組成物 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018028558A Expired - Fee Related JP6592545B2 (ja) | 2012-07-27 | 2018-02-21 | アンドロゲン受容体治療に対する抵抗性を判定する方法及び組成物 |
| JP2019171022A Ceased JP2020072655A (ja) | 2012-07-27 | 2019-09-20 | アンドロゲン受容体治療に対する抵抗性を判定する方法及び組成物 |
Country Status (34)
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009128936A2 (en) | 2008-04-16 | 2009-10-22 | The Johns Hopkins University | Compositions and methods for treating or preventing prostate cancer and for detecting androgen receptor variants |
| PE20150099A1 (es) | 2011-12-16 | 2015-01-30 | Olema Pharmaceuticals Inc | Compuestos novedosos de benzopirano, composiciones y usos de los mismos |
| US10202653B2 (en) | 2012-04-20 | 2019-02-12 | Cepheid | Compositions and methods for detecting markers associated with bladder cancer |
| EP2912194B1 (en) | 2012-10-26 | 2019-05-08 | Memorial Sloan-Kettering Cancer Center | Androgen receptor variants and methods for making and using |
| CN105143463A (zh) * | 2013-02-25 | 2015-12-09 | 诺华股份有限公司 | 新的雄激素受体突变 |
| JP2016513961A (ja) | 2013-03-06 | 2016-05-19 | セファイド | 膀胱癌を検出する方法 |
| KR20150127720A (ko) | 2013-03-14 | 2015-11-17 | 유니버시티 오브 매릴랜드, 발티모어 | 안드로겐 수용체 하향 조절제 및 그의 용도 |
| WO2015023710A1 (en) | 2013-08-12 | 2015-02-19 | Tokai Pharmaceuticals, Inc. | Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies |
| HUE066137T2 (hu) | 2013-10-18 | 2024-07-28 | Novartis Ag | A prosztata-specifikus membrán antigén (PSMA) jelzett inhibitorai, alkalmazásuk képalkotásban és gyógyszerkészítmények prosztatarák kezelésére |
| MX386859B (es) * | 2014-02-05 | 2025-03-19 | Lek Pharmaceuticals | Composiciones farmacéuticas sólidas de antagonistas de los receptores de andrógenos. |
| US10774387B2 (en) | 2014-05-19 | 2020-09-15 | The Johns Hopkins University | Methods for identifying androgen receptor splice variants in subjects having castration resistant prostate cancer |
| CA2959336A1 (en) * | 2014-08-25 | 2016-03-03 | The Johns Hopkins University | Methods and compositions related to prostate cancer therapeutics |
| PL3435865T3 (pl) | 2016-03-29 | 2025-03-24 | F. Hoffmann-La Roche Ag | Sposób obsługi odbiornika do odbioru danych analitycznych, odbiornik i produkt w postaci programu komputerowego |
| US11702702B2 (en) * | 2016-04-15 | 2023-07-18 | Predicine, Inc. | Systems and methods for detecting genetic alterations |
| CN106198985B (zh) * | 2016-08-31 | 2018-03-27 | 天津市泌尿外科研究所 | 用于检测去势抵抗性前列腺癌的elisa试剂盒及使用方法 |
| CN106290919B (zh) * | 2016-08-31 | 2018-03-27 | 天津市泌尿外科研究所 | 用于检测去势抵抗性前列腺癌的elisa试剂盒及使用方法 |
| CN106405085B (zh) * | 2016-08-31 | 2018-03-27 | 天津市泌尿外科研究所 | 用于检测去势抵抗性前列腺癌的elisa试剂盒及使用方法 |
| CN106526185B (zh) * | 2016-10-28 | 2018-03-30 | 拜尔康(天津)医药科技有限公司 | 用于检测去势抵抗性前列腺癌的elisa试剂盒及检测方法 |
| KR102368555B1 (ko) * | 2016-12-16 | 2022-02-28 | 강푸 바이오파마슈티칼즈 리미티드 | 조성물, 이의 적용 및 치료 방법 |
| SG11202003122XA (en) * | 2017-10-19 | 2020-05-28 | Univ Yale | Inhibition of androgen receptor by extracts of medicinal herbs and compositions thereof |
| CN108018342A (zh) * | 2017-12-04 | 2018-05-11 | 合肥艾迪康临床检验所有限公司 | 检测ar基因突变的引物和方法 |
| CN109115742A (zh) * | 2018-09-05 | 2019-01-01 | 中国农业科学院农业质量标准与检测技术研究所 | 一种抗雄激素效应的检测方法 |
| CN109321569B (zh) * | 2018-10-29 | 2022-04-12 | 迈杰转化医学研究(苏州)有限公司 | 一种引物探针组合物及其应用 |
| KR102473989B1 (ko) | 2018-11-28 | 2022-12-07 | (주)바이오니아 | 안드로젠 수용체 특이적 서열을 포함하는 이중나선 올리고뉴클레오티드 구조체, 및 이를 포함하는 탈모 예방 및 발모용 조성물 |
| CN114761003B (zh) * | 2019-09-23 | 2023-12-29 | 冰洲石生物科技公司 | 具有雄激素受体降解活性的新型脲类及其用途 |
| GB201914296D0 (en) * | 2019-10-03 | 2019-11-20 | Univ Oxford Innovation Ltd | Treatment |
| WO2021110731A1 (en) * | 2019-12-03 | 2021-06-10 | Bayer Aktiengesellschaft | Method for determining the response of prostate cancer patients to treatment with androgen receptor antagonists based on gene expression changes or super-enhancer protein-binding profiles |
| CN113533730B (zh) * | 2021-07-23 | 2022-09-06 | 南方医科大学深圳医院 | 一种血浆外泌体标志物组合及其应用 |
| US20240400642A1 (en) * | 2022-06-27 | 2024-12-05 | Etern Therapeutics Inc. | Compositions and methods for modulating molecules |
| CN117860773B (zh) * | 2023-11-28 | 2024-07-16 | 四川大学华西医院 | 促进ar基因甲基化的药物及其在预防或治疗雄性激素脱发中的用途 |
| CN117778322B (zh) * | 2023-12-17 | 2025-02-07 | 苏州拓维生物技术有限公司 | 一种对恩杂鲁胺耐药的细胞系的筛选方法及其应用 |
| CN121065176A (zh) * | 2025-04-14 | 2025-12-05 | 羿美诚健(上海)生物医药有限公司 | 靶向雄激素受体的小核酸及其药物组合物和用途 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS57106673A (en) | 1980-12-24 | 1982-07-02 | Chugai Pharmaceut Co Ltd | Dibenzo(b,f)(1,4)oxazepin derivative |
| GB8607679D0 (en) | 1986-03-27 | 1986-04-30 | Winter G P | Recombinant dna product |
| US5223409A (en) | 1988-09-02 | 1993-06-29 | Protein Engineering Corp. | Directed evolution of novel binding proteins |
| WO1995003335A1 (en) | 1993-07-26 | 1995-02-02 | K.O. Technology, Inc. | Inhibitors of alternative alleles of genes as a basis for cancer therapeutic agents |
| US6200754B1 (en) | 1998-03-19 | 2001-03-13 | Variagenics, Inc. | Inhibitors of alternative alleles of genes encoding products that mediate cell response to environmental changes |
| GB0005689D0 (en) * | 2000-03-09 | 2000-05-03 | Schering Ag | Crystal |
| AU8821301A (en) * | 2000-06-28 | 2002-01-08 | Bristol Myers Squibb Co | Selective androgen receptor modulators and methods for their identification, design and use |
| WO2005099693A2 (en) * | 2004-02-24 | 2005-10-27 | The Regents Of The University Of California | Methods and materials for assessing prostate cancer therapies and compounds |
| KR20100110298A (ko) * | 2007-11-26 | 2010-10-12 | 산타리스 팔마 에이/에스 | 안드로겐 수용체를 표적화하는 ｌｎａ 길항제 |
| EP2065474A1 (en) * | 2007-11-28 | 2009-06-03 | Siemens Healthcare Diagnostics GmbH | A method to assess prognosis and to predict therapeutic response to endocrine treatment |
| US8133724B2 (en) * | 2008-09-17 | 2012-03-13 | University Of Maryland, Baltimore | Human androgen receptor alternative splice variants as biomarkers and therapeutic targets |
| US9234098B2 (en) * | 2009-04-03 | 2016-01-12 | Basf Se | Method for the production of composite materials |
| CN102573472A (zh) * | 2009-10-23 | 2012-07-11 | 健康研究公司 | 治疗雄激素受体阳性癌症的方法 |
-
2013
- 2013-07-26 SM SM20190735T patent/SMT201900735T1/it unknown
- 2013-07-26 EP EP13745973.1A patent/EP2877599B1/en active Active
- 2013-07-26 SI SI201331612T patent/SI2877599T1/sl unknown
- 2013-07-26 PL PL13745973T patent/PL2877599T3/pl unknown
- 2013-07-26 NZ NZ704487A patent/NZ704487A/en not_active IP Right Cessation
- 2013-07-26 PE PE2015000095A patent/PE20150644A1/es active IP Right Grant
- 2013-07-26 CN CN201911199159.XA patent/CN110845626A/zh active Pending
- 2013-07-26 SG SG11201500184TA patent/SG11201500184TA/en unknown
- 2013-07-26 SG SG10201703254VA patent/SG10201703254VA/en unknown
- 2013-07-26 HR HRP20192342TT patent/HRP20192342T1/hr unknown
- 2013-07-26 DK DK13745973.1T patent/DK2877599T3/da active
- 2013-07-26 JP JP2015524483A patent/JP6297556B2/ja not_active Expired - Fee Related
- 2013-07-26 BR BR122017017921A patent/BR122017017921A2/pt not_active Application Discontinuation
- 2013-07-26 PT PT137459731T patent/PT2877599T/pt unknown
- 2013-07-26 WO PCT/US2013/052395 patent/WO2014018926A1/en not_active Ceased
- 2013-07-26 UA UAA201501717A patent/UA118178C2/uk unknown
- 2013-07-26 EA EA201792520A patent/EA035535B1/ru unknown
- 2013-07-26 EA EA201590290A patent/EA029563B1/ru unknown
- 2013-07-26 NZ NZ744288A patent/NZ744288A/en not_active IP Right Cessation
- 2013-07-26 CN CN201380050780.4A patent/CN104685072A/zh active Pending
- 2013-07-26 KR KR1020157004875A patent/KR102210183B1/ko not_active Expired - Fee Related
- 2013-07-26 PE PE2019001034A patent/PE20190845A1/es unknown
- 2013-07-26 CN CN201711405848.2A patent/CN108048567A/zh active Pending
- 2013-07-26 BR BR112015001801A patent/BR112015001801A2/pt not_active IP Right Cessation
- 2013-07-26 PE PE2019000439A patent/PE20190574A1/es unknown
- 2013-07-26 LT LTEP13745973.1T patent/LT2877599T/lt unknown
- 2013-07-26 NZ NZ742581A patent/NZ742581A/en not_active IP Right Cessation
- 2013-07-26 US US14/417,515 patent/US9617602B2/en not_active Expired - Fee Related
- 2013-07-26 AU AU2013295543A patent/AU2013295543B2/en not_active Ceased
- 2013-07-26 RS RS20191677A patent/RS59812B1/sr unknown
- 2013-07-26 NZ NZ740700A patent/NZ740700A/en not_active IP Right Cessation
- 2013-07-26 EP EP19204705.8A patent/EP3653733A1/en not_active Withdrawn
- 2013-07-26 KR KR1020217002584A patent/KR20210012064A/ko not_active Ceased
- 2013-07-26 ES ES13745973T patent/ES2764381T3/es active Active
- 2013-07-26 CA CA2879926A patent/CA2879926A1/en not_active Abandoned
- 2013-07-26 HU HUE13745973A patent/HUE047781T2/hu unknown
- 2013-07-26 MX MX2015001209A patent/MX370507B/es active IP Right Grant
-
2015
- 2015-01-21 CR CR20150022A patent/CR20150022A/es unknown
- 2015-01-22 IL IL236844A patent/IL236844B/en active IP Right Grant
- 2015-01-26 MX MX2019015148A patent/MX2019015148A/es unknown
- 2015-01-26 CL CL2015000194A patent/CL2015000194A1/es unknown
- 2015-01-26 NI NI201500004A patent/NI201500004A/es unknown
- 2015-01-27 PH PH12015500175A patent/PH12015500175B1/en unknown
- 2015-01-28 GT GT201500019A patent/GT201500019A/es unknown
- 2015-02-04 CO CO15022272A patent/CO7280477A2/es unknown
- 2015-02-27 EC ECIEPI20157420A patent/ECSP15007420A/es unknown
-
2017
- 2017-03-01 US US15/446,341 patent/US20170196840A1/en not_active Abandoned
- 2017-05-19 AU AU2017203385A patent/AU2017203385B2/en not_active Ceased
-
2018
- 2018-02-21 JP JP2018028558A patent/JP6592545B2/ja not_active Expired - Fee Related
- 2018-11-26 PH PH12018502500A patent/PH12018502500A1/en unknown
-
2019
- 2019-03-13 AU AU2019201726A patent/AU2019201726B2/en not_active Expired - Fee Related
- 2019-03-25 IL IL265610A patent/IL265610B/en active IP Right Grant
- 2019-09-20 JP JP2019171022A patent/JP2020072655A/ja not_active Ceased
-
2020
- 2020-01-14 CY CY20201100029T patent/CY1122651T1/el unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2015531590A5 (enExample) | ||
| AU2019201726B2 (en) | Methods and compositions for determining resistance to androgen receptor therapy | |
| US20140005070A1 (en) | Markers associated with cyclin-dependent kinase inhibitors | |
| US20070243176A1 (en) | Human genes and gene expression products | |
| WO2014017491A1 (ja) | Ｃｅｐ５５遺伝子とｒｅｔ遺伝子との融合遺伝子 | |
| JP2017108751A5 (enExample) | ||
| JP6387001B2 (ja) | Ｃｄｋ阻害剤と関連するバイオマーカー | |
| KR20110014979A (ko) | 항바이러스 요법 | |
| WO2004047767A2 (en) | Methods for identifying risk of breast cancer and treatments thereof | |
| EP1507790A2 (en) | Human genes and gene expression products isolated from human prostate | |
| ES2347247T3 (es) | Regulacion de una quinasa, 'quinasa regulada en epoc' (quinasa rc). | |
| JP2008539742A (ja) | Ｇｉｐプロモーター多型の使用 | |
| CN110846416A (zh) | 一种检测dna非同源末端连接修复通路有效性的探针库、检测方法和试剂盒 | |
| US20240309453A1 (en) | Diagnosis of acute and chronic lung diseases by quantifying spink1 level | |
| WO2009103081A2 (en) | Glucocorticoid receptor polymorphisms | |
| US20100028867A1 (en) | LRRTM1 Compositions and Methods of Their Use for the Diagnosis and Treatment of Cancer | |
| US20220152071A1 (en) | Markers of efficacy of topoisomerase poisons | |
| WO2024197199A2 (en) | Targeting prac1 in steroid hormone driven cancer | |
| Akashi et al. | Frequent copy gain of the MET gene in hypopharyngeal and laryngeal cancer in the japanese population | |
| JP2006525782A5 (enExample) | ||
| CN1712541B (zh) | 肝细胞癌相关的蛋白质分子标记异种核糖核蛋白k的筛选及其应用 | |
| CN114949217A (zh) | 癌症靶标及其应用 | |
| US20120040938A1 (en) | Glucocorticoid receptor alleles and uses thereof | |
| JP2013226075A (ja) | 新規ａｕｒｋｃ融合体 |