MX360932B - Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf. - Google Patents
Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf.Info
- Publication number
- MX360932B MX360932B MX2016003137A MX2016003137A MX360932B MX 360932 B MX360932 B MX 360932B MX 2016003137 A MX2016003137 A MX 2016003137A MX 2016003137 A MX2016003137 A MX 2016003137A MX 360932 B MX360932 B MX 360932B
- Authority
- MX
- Mexico
- Prior art keywords
- braf
- inhibitors
- conferring resistance
- mutations conferring
- mutations
- Prior art date
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- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/10—Transferases (2.)
- C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7088—Compounds having three or more nucleosides or nucleotides
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
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- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
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- C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
- C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
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- C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
- C12Y207/11—Protein-serine/threonine kinases (2.7.11)
- C12Y207/11001—Non-specific serine/threonine protein kinase (2.7.11.1), i.e. casein kinase or checkpoint kinase
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- G01N33/5011—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing antineoplastic activity
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- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
- G01N33/573—Immunoassay; Biospecific binding assay; Materials therefor for enzymes or isoenzymes
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- G01N2500/00—Screening for compounds of potential therapeutic value
- G01N2500/02—Screening involving studying the effect of compounds C on the interaction between interacting molecules A and B (e.g. A = enzyme and B = substrate for A, or A = receptor and B = ligand for the receptor)
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Abstract
La presente invención se refiere a un método para identificar un inhibidor de BRAF de segunda generación, que comprende; a) seleccionar un fármaco potencial utilizando un modelado asistido por computadora con una estructura tridimensional de cristal o de la solución de un polipéptido de BRAF mutante, en donde el polipéptido de BRAF mutante comprende una secuencia de aminoácidos que tiene al menos una sustitución de aminoácidos en comparación con un polipéptido de BRAF V600E que tiene una secuencia SEQ ID NO: 4, la al menos una sustitución de aminoácidos confiere resistencia a uno o más inhibidores de BRAF en el polipéptido de BRAF mutante, en donde la al menos una sustitución de aminoácidos se selecciona del grupo que consiste de A29, H72, S113, S124, P162, C194, L227, P231, C251, V291, Q329, K483, L495, T521, V528, D587, P655, S657, S683, P686, C696, L697, P722, F738 y C748; b) poner en contacto el fármaco potencial con el polipéptido de BRAF mutante; y c) detectar la interacción del fármaco potencial con el polipéptido de BRAF mutante; en donde un compuesto que es capaz de interactuar con el polipéptido de BRAF mutante se identifica como un inhibidor de BRAF de segunda generación.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US30827510P | 2010-02-25 | 2010-02-25 | |
PCT/US2011/025645 WO2011106298A1 (en) | 2010-02-25 | 2011-02-22 | Braf mutations conferring resistance to braf inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
MX360932B true MX360932B (es) | 2018-11-21 |
Family
ID=43769726
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2016003137A MX360932B (es) | 2010-02-25 | 2011-02-22 | Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf. |
MX2012009784A MX340392B (es) | 2010-02-25 | 2011-02-22 | Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf. |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2012009784A MX340392B (es) | 2010-02-25 | 2011-02-22 | Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf. |
Country Status (12)
Country | Link |
---|---|
US (2) | US8637246B2 (es) |
EP (2) | EP3028699B1 (es) |
JP (1) | JP5933459B2 (es) |
KR (1) | KR101814223B1 (es) |
CN (1) | CN103002894B (es) |
AU (1) | AU2011221227B2 (es) |
BR (1) | BR112012021411A2 (es) |
CA (1) | CA2789696C (es) |
ES (2) | ES2576061T3 (es) |
MX (2) | MX360932B (es) |
RU (1) | RU2571930C2 (es) |
WO (1) | WO2011106298A1 (es) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20130156768A1 (en) * | 2010-08-26 | 2013-06-20 | Bristol-Myers Squibb Company | Combination of anti-ctla4 antibody with braf inhibitors for the synergistic treatment of proliferative diseases |
US10077474B2 (en) | 2012-05-29 | 2018-09-18 | Abbott Molecular, Inc. | Method of designing primers, method of detecting single nucleotide polymorphisms (SNPs), method of distinguishing SNPs, and related primers, detectable oligonucleotides, and kits |
WO2015039107A1 (en) | 2013-09-16 | 2015-03-19 | The Johns Hopkins University | Activities of multiple cancer-related pathways are associated with braf mutation and predict the resistance to braf/mek inhibitors in melanoma cells |
EP3771745A1 (en) | 2013-12-28 | 2021-02-03 | Guardant Health, Inc. | Methods and systems for detecting genetic variants |
WO2019195959A1 (en) * | 2018-04-08 | 2019-10-17 | Cothera Biosciences, Inc. | Combination therapy for cancers with braf mutation |
WO2020145734A1 (ko) * | 2019-01-11 | 2020-07-16 | 주식회사 진캐스트 | Braf 돌연변이 검출을 위한 dna 중합효소 및 이를 포함하는 키트 |
WO2021003192A1 (en) * | 2019-07-02 | 2021-01-07 | Effector Therapeutics, Inc. | Methods of treating braf-mutated cancer cells |
CN111349704B (zh) * | 2020-03-17 | 2020-11-24 | 河北医科大学第三医院 | 肝癌的诊断产品和治疗组合物 |
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DE2220262C2 (de) | 1972-04-25 | 1979-11-22 | Siemens Ag, 1000 Berlin Und 8000 Muenchen | Verfahren zum Verbindungsaufbau in einem nichthierarchischen Fernmeldenetz |
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EP3028699B1 (en) | 2018-03-21 |
RU2012140726A (ru) | 2014-03-27 |
US20140155399A1 (en) | 2014-06-05 |
KR20120123141A (ko) | 2012-11-07 |
CN103002894A (zh) | 2013-03-27 |
ES2576061T3 (es) | 2016-07-05 |
AU2011221227B2 (en) | 2015-07-09 |
MX340392B (es) | 2016-07-06 |
MX2012009784A (es) | 2012-10-09 |
US9279144B2 (en) | 2016-03-08 |
EP2538943B1 (en) | 2016-03-30 |
EP2538943A1 (en) | 2013-01-02 |
CA2789696C (en) | 2017-11-07 |
JP5933459B2 (ja) | 2016-06-08 |
US20130004509A1 (en) | 2013-01-03 |
EP3028699A1 (en) | 2016-06-08 |
AU2011221227A1 (en) | 2012-08-23 |
BR112012021411A2 (pt) | 2017-04-18 |
KR101814223B1 (ko) | 2018-01-02 |
RU2571930C2 (ru) | 2015-12-27 |
US8637246B2 (en) | 2014-01-28 |
ES2674682T3 (es) | 2018-07-03 |
JP2013527747A (ja) | 2013-07-04 |
WO2011106298A1 (en) | 2011-09-01 |
CA2789696A1 (en) | 2011-09-01 |
CN103002894B (zh) | 2016-04-06 |
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