A cewar wani bincike da aka buga aCell,masu bincike sun haɓaka takamaiman mai hanawa don KRASG12C da ake kira ARS-1602 wanda ya haifar da koma bayan ƙwayar cuta a cikin mice.
"Wannan binciken yana ba da shaida a cikin vivo cewa za a iya yin niyya na mutant KRAS, kuma ya bayyana ARS-1620 a matsayin wakiltar sabon ƙarni na KRASG12C-takamaiman hanawa tare da yiwuwar warkewa," in ji marubucin jagora, Matthew R Janes, PhD, daga Wellspring Biosciences in San Diego, CA, da abokan aiki.
Maye gurbi na KRAS shine mafi yawan maye gurbin oncogene kuma bincike da aka yi a baya ya nuna cewa kusan kashi 30% na ciwace-ciwacen ciwace-ciwacen ciwace-ciwacen ciwace-ciwacen ciwace-ciwacen ciwace-ciwacen ciwace-ciwacen ciwace-ciwacen ciwace-ciwacen ciwace-ciwacen ciwace-ciwacen ciwace-ciwacen ciwace-ciwacen ciwace-ciwacen ciwace-ciwace na RAS ya kunshi. Takamaiman maye gurbin KRAS sun mamaye takamaiman nau'ikan ƙari. Misali KRASG12C shine babban maye gurbi a cikin ciwon huhu mara kanana (NSCLC), kuma ana samunsa a cikin adenocarcinomas na pancreatic da colorectal.
Duk da yaɗuwar da shekarun da suka gabata na bincike da ke nuna KRAS mutant a matsayin babban direban tumorigenesis da juriya na asibiti, mutant KRAS ya kasance manufa mai taurin kai.
Daban-daban iri-iri sun yi ƙoƙarin gano ƙananan ƙwayoyin cuta waɗanda ke nufi KRAS, amma sun haifar da iyakancewar hana KRAS a cikin sel. Wannan ya zaburar da marubutan don tsara wani fili don haɓaka takamaiman masu hanawa KRAS, gami da masu hana masu hanawa 2 aljihu (S-IIP) KRASG12C waɗanda ke ɗaure da amsa tare da yanayin GDP na KRAS, suna kama shi a cikin rashin aiki.
Don yin tasiri, mai hanawa dole ne ya sami babban ƙarfi da saurin ɗaure motsin motsi. Hakanan dole ne ya sami mafi kyawun kaddarorin harhada magunguna don kiyaye fallasa da tsawon lokaci na dogon lokaci don kama yanayin rashin aiki na GDP na KRAS wanda ke fuskantar saurin sake zagayowar nucleotide.
Masu binciken sun tsara kuma suka haɗa ARS-1620 tare da kaddarorin ƙwayoyi, da ingantaccen ƙarfi akan mahaɗan ƙarni na farko. Inganci da motsin motsi a cikin layukan tantanin halitta tare da mutant allele sannan an tantance don sanin ko mazaunin da aka yi niyya don hana KRAS-GTP a cikin ciwace-ciwacen daji ya wadatar.
Hana haɓakar tantanin halitta, da kuma yiwuwar halayen da ba na musamman waɗanda zasu iya nuna yiwuwar guba, an kimanta su.
A ƙarshe, don tantance zama mai niyya a cikin vivo, an ba da ARS-1620 na baka ga beraye tare da ingantattun samfuran xenograft na subcutaneous waɗanda ke ɗauke da KRAS p.G12C azaman kashi ɗaya, ko yau da kullun don kwanaki 5.
Masu binciken sun ba da rahoton cewa ARS-1620 ta hana ci gaban ƙwayar cuta sosai a cikin kashi-da kuma dogaro da lokaci tare da alamar ƙwayar cuta.
A cikin nau'ikan xenograft guda biyar na layin salula na NSCLC a cikin mice, duk samfuran sun amsa bayan makonni biyu zuwa uku na jiyya, kuma huɗu daga cikin biyar sun nuna mahimmancin hana ci gaban ƙari. Bugu da ƙari, ARS-1620 an yarda da shi da kyau ba tare da lura da rashin lafiyar asibiti ba a lokacin lokacin jiyya.
"Tare, shaida a cikin vivo cewa ARS-1620 yana da tasiri sosai a matsayin wakili guda ɗaya a cikin tsarin NSCLC yana ba da tabbacin ra'ayi cewa wani muhimmin sashi na marasa lafiya tare da maye gurbin p.G12C KRAS na iya amfana daga hanyoyin kwantar da hankali na KRASG12C," in ji marubutan.
Sun kara da cewa ARS-1620 kai tsaye KRASG12C ƙananan ƙwayoyin ƙwayoyin cuta ne wanda ke da ƙarfi, zaɓi, mai yiwuwa na baka, kuma mai jurewa.
Lokacin aikawa: Mayu-22-2018