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1. (WO2018006009) COMPOSITIONS, ASSAYS, AND METHODS FOR DIRECT MODULATION OF FATTY ACID METABOLISM
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/006009 International Application No.: PCT/US2017/040360
Publication Date: 04.01.2018 International Filing Date: 30.06.2017
IPC:
A61K 31/00 (2006.01) ,A61K 31/11 (2006.01) ,A61K 31/4045 (2006.01) ,A61K 31/495 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
11
Aldehydes
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403
condensed with carbocyclic rings, e.g. carbazole
404
Indoles, e.g. pindolol
4045
Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
Applicants: DANA-FARBER CANCER INSTITUTE, INC.[US/US]; 450 Brookline Avenue Boston, Massachusetts 02215-5450, US
Inventors: WALENSKY, Loren D.; US
ESCUDERO, Silvia; US
Agent: KOIPALLY, Joseph J.; US
ZHANG, Tony; US
Priority Data:
62/357,86601.07.2016US
Title (EN) COMPOSITIONS, ASSAYS, AND METHODS FOR DIRECT MODULATION OF FATTY ACID METABOLISM
(FR) COMPOSITIONS, TESTS ET PROCÉDÉS POUR LA MODULATION DIRECTE DU MÉTABOLISME DES ACIDES GRAS
Abstract:
(EN) This disclosure relates to the surprising and unexpected finding that the well-known cancer protein, Myeloid Cell Leukemia-1 (MCL-1), binds to and modulates the enzymatic activity of Very Long Chain Acyl CoA Dehydrogenase (VLCAD), thereby regulating fatty acid β-oxidation. This finding is employed in compositions and methods of treating cancer, metabolic diseases, or other conditions characterized by excessive fatty acid β-oxidation by blocking or reducing the energy production of cells (e.g., cancer) through inhibiting the MCL-1/VLCAD interaction and/or directly inhibiting VLCAD enzymatic activity. In addition, the disclosure features methods for identifying such agents that inhibit the interaction between MCL-1 and VLCAD or that inhibit VLCAD enzymatic activity.
(FR) Cette invention concerne la découverte surprenante et inattendue selon laquelle la protéine liée au cancer bien connue, MCL-1 (Myeloid Cell Leukemia-1), se lie à l'Acyl-CoA déshydrogénase à très longue chaîne (VLCAD) et module son activité enzymatique, régulant ainsi la ß-oxydation des acides gras. Cette découverte est utilisée dans des compositions et des procédés de traitement du cancer, de maladies métaboliques, ou d'autres affections caractérisées par une ß-oxydation excessive des acides gras par blocage ou réduction de la production d'énergie de cellules (par exemple, de cancer) par inhibition de l'interaction MCL-1/VLCAD et/ou par inhibition directe de l'activité enzymatique de VLCAD. De plus, l'invention concerne des procédés d'identification de tels agents qui inhibent l'interaction entre MCL-1 et VLCAD ou qui inhibent l'activité enzymatique de VLCAD.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)