G단백질결합수용체키나제5는 Ser /Thr단백질키나제스 의 G단백질결합수용체키나제 하위 계열의 구성원으로 GRK4 및 GRK6 와 가장 유사하다.[5] [6] [7] 단백질 은 G단백질 결합 수용체의 활성 형태를 만들어 신호를 조절 한다.
함수 G단백질결합수용체 키노리산 활성 G단백질결합수용체들은 수용체에 아레스틴 단백질의 결합을 촉진한다. 인광 활성 수용체에 대한 아레스틴 결합은 이질성 G 단백질 변환기 단백질의 수용체 자극을 방지하여 세포신호를 차단하고 수용체 감소 를 초래한다. 아레스틴 결합은 또한 수용체를 특정 세포 내분화 경로 로 유도하여 세포 표면에서 수용체를 제거하고 추가적인 활성화를 방지한다. 인산화 활성 수용체에 대한 아레스틴 결합도 아레스틴 파트너 단백질을 통한 수용체 신호 전달을 가능하게 한다. 따라서 GRK/arrestin 시스템은 G 단백질 결합 수용체에 대한 복잡한 신호 스위치 역할을 한다.[8]
GRK5 및 이와 밀접하게 연관된 GRK6 인산화 수용체들은 (반대의 효과가 있는 GRK2 와 GRK3 와는 대조적으로) 구속 매개 수용체 감소화, 내성화 및 인신매매보다는 구속 매개 신호를 장려하는 현장의 GRK6 인산화 수용체들이다.[9] [10] 이러한 차이는 수용체에 대한 약물 결합이 수용체가 그 수용체에 의해 자극된 작용의 특정 부분집합을 향해 신호를 보내는 편향될 수 있는 약리학적 편향 작용 (기능적 선택성이라고 도 함)의 한 가지 근거다.[11] [12]
GRK5는 몸 전체에 널리 표현되지만 폐, 심장, 태반에서 두드러지게 높은 발현을 가지고 있으며, 낮은 단계에서는 광범위한 발현을 하고 있다.[13] 인간에게 있어 아프리카 조상을 가진 개인에게 가장 많이 나타나는 잔류물 41(글루타민보다는 류신)에서 GRK5 염기서열 다형성은 천식 의 약물 표적인 기도 베타2-아드레날린 수용체 의 GRK5 매개 감소화 상승으로 이어진다.[14] 마우스에서는 GRK5가 기도와 뉴런에 있는 무스카린 아세틸콜린 수용체 의 M2 아형을 조절하고 있으며, GRK5가 부족한 생쥐는 알츠하이머병 모델 로 제안되어 왔다.[15] [16] [17] 제브라피쉬와 인간에서 GRK5 기능의 상실은 이단성 으로 인한 심장 결함과 연관되어 있는데, 이는 유기생식 중 부적절한 좌-우측 횡격으로 인해 발생하는 일련의 발달 결함이다.[18] 생쥐 심장에서 GRK5의 과다압박은 GRK5가 베타2-아드레날린 수용체를 조절하는 것으로 나타났으나 GRK5 과다압박 또는 삭제는 심장에서의 Angiotensin II AT1 수용체 에 의한 신호에 영향을 미치지 않는다.[19] [20]
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